Ethylene derivatives and pesticides containing said derivatives

Abstract

Ethylene derivatives of formula (I):

Description

BACKGROUND OF THE INVENTION

1. Field of the Art

The present invention relates to novel ethylene derivatives, and also to agricultural chemicals and agents for preventing the attachment of aquatic organisms containing said derivatives as an active ingredient. The agricultural chemicals as referred to herein include insecticides, acaricides, nematocides, herbicides and fungicides, etc., and are especially pesticides in the field of agriculture, horticulture, stock farming and sanitation. The agent for preventing the attachment of aquatic organisms are chemicals for preventing the attachment of harmful aquatic organisms such as shells and algae to fishing nets, the bottoms of ships, marine equipment such as buoys, marine constructions, circulating water systems in thermal and atomic power plants, inlet channels for heat exchanger cooling water in chemical industry, underwater constructions and reservoirs.

2. Description of the Related Art

For acrylonitrile derivatives, Japanese Patent Application Laid-Open No. Sho 53-92769 discloses the use of 2′-chloro-3-hydroxy-2-(4-phenyl-2-thiazolyl)-cinnamoyl nitrile as an insecticide; and International Patent Application Laid-Open No. WO-95/29591 discloses its use as an aquatic adhesion inhibitor. Japanese Patent Application Laid-open No. Sho 60-11452 discloses the use of 2-(4-chlorophenyl)-3-(3-pyridyl)-3-oxopropionitrile as a herbicide and Japanese Patent Application Laid-open No. Sho 60-11401 discloses its use as a fungicide.

With the long-term use of insecticides and fungicides, recently, some pests have become resistant to chemicals and are often difficult to exterminate with conventional insecticides and fungicides. In addition, some insecticides are highly toxic and are prone to remain long, without being decomposed, to destroy the ecosystem. Accordingly, it is always expected to develop novel, low-toxic and low-persistent insecticides and fungicides.

On the other hand, in order to prevent the adhesion and growth of marine and freshwater aquatics, it is used antifouling coatings comprising organic tin compounds such as bis(tributyltin) oxide or copper compounds such as copper sulfate and cuprous oxide. However, organic tin compounds are highly toxic, though being effective in preventing the adhesion of aquatics, and are especially prone to accumulate in the bodies of fishes and shellfishes. As so promoting the environmental pollution, the use of those compounds is now under legal controls. Copper compounds are widely used in antifouling coatings for inlet channels and for the bottoms of ships. However, like tin compounds, copper compounds contain a copper as a heavy metal. Therefore, the use of copper compounds will bring about the environmental pollution in future, and agents for preventing the attachment of aquatic organisms comprising such copper compounds are not preferred. Under the above-mentioned situation, it has been desired agents for preventing the attachment of aquatic organisms that have few influences on the ecosystem and bring about little secondary pollution.

SUMMARY OF THE INVENTION

In order to solve the above-mentioned problems, the present inventors have assiduously studied to develop agricultural chemicals and agents for preventing the attachment of aquatic organisms which can exhibit excellent pesticidal activities even when used in small amounts, and which have few negative influences on non-targeted organisms such as mammals, fishes and useful insects, and, as a result, have found that the compounds mentioned hereinunder are highly safe and have excellent pesticidal activities and activities for preventing the attachment of aquatic organisms. On the basis of these findings, the present inventors have completed the present invention.

DETAILED DESCRIPTION OF THE INVENTION

Specifically, the present invention provides the following [1] to [25]

[1] Ethylene derivatives of a formula (I):

[wherein;

Q represents a phenyl group optionally substituted by G, a naphthyl group optionally substituted by G, or a heterocyclic group optionally substituted by R (said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,4,5-tetrazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, imidazolinone, imidazolidinedione, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl; quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

A represents a phenyl group optionally substituted by W, a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y (said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

provided that, (a) when Q is a thienyl group optionally substituted by R, a furyl group optionally substituted by R, a quinolyl group optionally substituted by R, or an isoquinolyl group optionally substituted by R, then A is a phenyl group optionally substituted by W, a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y (said heterocyclic group being a pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(b) when Q is a 2-thiazolyl group optionally substituted by R, then A is a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y (said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(c) when Q is a pyridyl group optionally substituted by R, then A is a heterocyclic group optionally substituted by Y (said heterocyclic group being a pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyrazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(d) when Q is an isothiazolyl group optionally substituted by R, a 1,2,3-triazolyl group optionally substituted by R, or a benzoxazolyl group optionally substituted by R, then A is a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y (said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(e) when Q is a 1,2,4-triazolyl group optionally substituted by R, then A is a heterocyclic group optionally substituted by Y (said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(f) when Q is a benzothiazolyl group optionally substituted by R, then A is a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y (said heterocyclic group being a furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(g) when Q is a benzimidazolyl group optionally substituted by R, then A is a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y (said heterocyclic group being a pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyrazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(h) when Q is a phenyl group optionally substituted by G, then A is a heterocyclic group optionally substituted by Y (said heterocyclic group being a pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

(i) when Q is a naphthyl group optionally substituted by G, then A is a heterocyclic group optionally substituted by Y (said heterocyclic group being a thienyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl, 3(2H)-pyridazinone, benzothiazolyl, benzimidazolyl, indazolyl, benzoxazolyl, quinolyl, isoquinolyl, quinoxalinyl, phthalazinyl, cinnolinyl or quinazolinyl group);

B represents H, a C₁-C₄ alkyl group, a C₁-C₄ haloalkyl group, a C₂-C₄ alkoxyalkyl group, CH₃SCH₂, CH₃OC₂H₄OCH₂, a C₁-C₄ alkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₁-C₄ alkyl group substituted by a benzoyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a tetrahydropyranyl group, (CH₃)₃Si, a C₁-C₄ alkylsulfonyl group, a phenylsulfonyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, —SO₂CF₃, a C₁-C₄ monoalkylaminosulfonyl group, a C₂-C₈ dialkylaminosulfonyl group, a phenylaminosulfonyl group, a C₂-C₅ monoalkylaminothiocarbonyl group, a C₃-C₉ dialkylaminothiocarbonyl group, a C₂-C₅ cyanoalkyl group, a C₃-C₉ alkoxycarbonylalkyl group, —C(═O)T¹, —P(═O)T²T³, —P(═S)T²T³, an alkali metal atom, an alkaline earth metal atom, or NHT⁴T⁵T⁶;

provided that, when Q is a 2-thiazolyl or 2-benzothiazolyl group, then B is a C₁-C₄ alkyl group, a C₁-C₄ haloalkyl group, a C₂-C₄ alkoxyalkyl group, CH₃SCH₂, CH₃OC₂H₄OCH₂, a C₁-C₄ alkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₁-C₄ alkyl group substituted by a benzoyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a tetrahydropyranyl group, (CH₃)₃Si, a C₁-C₄ alkylsulfonyl group, a phenylsulfonyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, —SO₂CF₃, a C₁-C₄ monoalkylaminosulfonyl group, a C₂-C₈ dialkylaminosulfonyl group, a phenylaminosulfonyl group, a C₂-C₆ monoalkylaminothiocarbonyl group, a C₃-C₉ dialkylaminothiocarbonyl group, a C₂-C₅ cyanoalkyl group, a C₃-C₉ alkoxycarbonylalkyl group, —C(═O)T¹, —P(═O)T²T³, or —P(═S)T²T³;

E represents a heterocyclic group optionally substituted by a C₁-C₄ alkyl or C₁-C₄ haloalkyl group (said heterocyclic group being a 2-oxazolyl, 2-thiazolyl, 2-imidazolyl, 1,2,4-triazol-3-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-thiadiazol-3-yl, 1,3,4-oxadiazol-2-yl, 5-tetrazolyl, 2-oxazolinyl or 1,2,4,5-tetrazin-3-yl group)—or represents a halogen, a C₂-C₄ alkynyl group, a phenylethynyl group optionally substituted by Z, a C₁-C₄ haloalkyl group, CN, an isonitrile group, NO₂, N₃, CHO, a C₂-C₅ alkylcarbonyl group, a C₂-C₅ alkoxycarbonyl group, a C₃-C₅ alkenyloxycarbonyl group, a C₂-C₄ alkylaminocarbonyl group, a C₃-C₅ dialkylaminocarbonyl group, a benzoyl group optionally substituted by Z, an aminothiocarbonyl group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a phenylsulfenyl group optionally substituted by Z, a phenylsulfinyl group optionally substituted by Z, a phenylsulfonyl group optionally substituted by Z, —P(═O)T²T³, or —P(═S)T²T³.

G is a substituent freely selected from a halogen atom, a C₁-C₁₀ alkyl group, a C₂-C₄ cyanoalkyl group, a C₁-C₄ alkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₂-C₆ alkenyl group, a C₂-C₆ alkynyl group, a C₁-C₆ haloalkyl group, a C₂-C₆ haloalkenyl group, a C₂-C₆ haloalkynyl group, a C₃-C₆ halocycloalkyl group, a C₃-C₆ cycloalkyl group optionally substituted by a C₁-C₃ alkyl group, a C₁-C₁₀ alkoxy group, a C₂-C₆ alkenyloxy group, a C₂-C₆ alkynyloxy group, a C₁-C₄haloalkoxy group, a C₂-C₆ haloalkenyloxy group, a C₂-C₆ haloalkynyloxy group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a C₂-C₆ alkenylsulfenyl group, a C₂-C₆ alkenylsulfinyl group, a C₂-C₆ alkenylsulfonyl group, a C₂-C₆ alkynylsulfenyl group, a C₂-C₆ alkenylsulfinyl group, a C₂-C₆ alkynylsulfonyl group, a C₁-C₄ haloalkylsulfenyl group, a C₁-C₄ haloalkylsulfinyl group, a C₁-C₄ haloalkylsulfonyl group, a C₂-C₆ haloalkenylsulfenyl group, a C₂-C₆ haloalkenylsulfinyl group, a C₂-C₆ haloalkenylsulfonyl group, a C₂-C₆ haloalkynylsulfenyl group, a C₂-C₆ haloalkynylsulfinyl group, a C₂-C₆ haloalkynylsulfonyl group, CHO, NO₂, CN, —NU¹U², OH, a naphthyl group, a methoxy group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₂-C₇ alkoxycarbonyl group, a C₂-C₄ alkoxyalkyl group, a C₂-C₅ alkylcarbonyl group, a C₂-C₄ haloalkylcarbonyl group, a C₂-C₅ alkylcarbonyloxy group, a C₂-C₅ haloalkylcarbonyloxy group, a C₃-C₇ dialkylaminocarbonyloxy group, a phenyl group optionally substituted by Z, a phenoxy group optionally substituted by Z, a benzoyl group optionally substituted by Z, a pyridyl group optionally substituted by Z, a pyridyloxy group optionally substituted by Z, a thienyl group optionally substituted by Z, a methylenedioxy group as bonded at the adjacent substituting positions, a halomethylenedioxy group as bonded at the adjacent substituting positions, and —N═CT⁷T⁸ (in which T⁷ and T⁸ each independently represent H, or a phenyl, benzyl or C₁-C₆ alkyl group, or T⁷ and T⁸, together with the carbon atom to which they are bonded, form a 5-, 6-, 7- or 8-membered ring), (provided that when the the substituent is two or more, then said substituents may be the same or different), and the number of the substituent, G, is 1, 2, 3 or 4; or G is an alkylene group as bonded to the adjacent substituting positions to form a 5-, 6-, 7- or 8-membered ring;

R is a substituent freely selected from a halogen atom, a C₁-C₁₀ alkyl group, a C₁-C₄ alkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₂-C₆ alkenyl group, a C₂-C₆ alkynyl group, a C₁-C₆ haloalkyl group, a C₂-C₆ haloalkenyl group, a C₂-C₆ haloalkynyl group, a C₃-C₆ halocycloalkyl group, a C₃-C₆ cycloalkyl group optionally substituted by a C₁-C₃ alkyl group, a C₁-C₆ alkoxy group, a C₂-C₆ alkenyloxy group, a C₂-C₆ alkynyloxy group, a C₁-C₄ haloalkoxy group, a C₂-C₆ haloalkenyloxy group, a C₂-C₆ haloalkynyloxy group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a C₂-C₆ alkenylsulfenyl group, a C₂-C₆ alkenylsulfinyl group, a C₂-C₆ alkenylsulfonyl group, a C₂-C₆ alkynylsulfenyl group, a C₂-C₆ alkynylsulfinyl group, a C₂-C₆ alkynylsulfonyl group, a C₁-C₄ haloalkylsulfenyl group, a C₁-C₄ haloalkylsulfinyl, group, a C₁-C₄ haloalkylsulfonyl group, a C₂-C₆ haloalkenylsulfenyl group, a C₂-C₆ haloalkenylsulfinyl group, a C₂-C₆ haloalkenylsulfonyl group, a C₂-C₆ haloalkynylsulfenyl group, a C₂-C₆ haloalkynylsulfinyl group, a C₂-C₆ haloalkynylsulfonyl group, NO₂, CN, —NU¹U², a phenoxy group, OH, a naphthyl group, a C₂-C₇ alkoxycarbonyl group, a C₂-C₄ alkoxyalkyl group, a C₂-C₄ alkylcarbonyl group, a C₂-C₅ alkylcarbonyloxy group, a C₂-C₅ haloalkylcarbonyloxy group, a benzoyl group optionally substituted by X, a phenyl group optionally substituted by X, a pyridyl group optionally substituted by X, a thienyl group optionally substituted by X, and —N═CT⁷T⁸, (provided that when the substituent is two or more, then said substituents may be the same or different), and the number of the substituents, R, is 1, 2, 3 or 4; or R is an alkylene group as bonded to the adjacent substituting positions to form a 5-, 6-, 7- or 8-membered ring;

Y is a substituent freely selected from a halogen atom, a C₁-C₁₀ alkyl group, a C₁-C₆ haloalkyl group, a C₁-C₆ alkoxy group, a C₂-C₆ alkenyloxy group, a C₂-C₆ alkynyloxy group, a C₁-C₄-haloalkoxy group, a C₂-C₆ haloalkenyloxy group, a C₂-C₆ haloalkynyloxy group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a C₂-C₆ alkenylsulfenyl group, a C₂-C₆ alkenylsulfinyl group, a C₂-C₆ alkenylsulfonyl group, a C₂-C₆ alkynylsulfenyl group, a C₂-C₆ alkynylsulfinyl group, a C₂-C₆ alkynylsulfonyl group, a C₁-C₄ haloalkylsulfenyl group, a C₁-C₄ haloalkylsulfinyl group, a C₂-C₆ haloalkylsulfonyl group, a C₂-C₆ haloalkenylsulfenyl group, a C₂-C₆ haloalkenylsulfinyl group, a C₂-C₆ haloalkenylsulfonyl group, a C₂-C₆ haloalkynylsulfenyl group, a C₂-C₆ haloalkynylsulfinyl group, a C₂-C₆ haloalkynylsulfonyl group, NO₂, CN, —NU¹U², OH, a C₂-C₇ alkoxycarbonyl group, a C₂-C₄ alkoxyalkyl group, a C₂-C₅ alkylcarbonyloxy group, a C₂-C₅ haloalkylcarbonyloxy group, a C₃-C₇ dialkylaminocarbonyloxy group, a phenyl group optionally substituted by X, and —N═CT⁷T⁸ (in which T⁷ and T⁸ each independently represent H, or a phenyl, benzyl or C₁-C₆ alkyl group, or T⁷ and T⁸ may, together with the carbon atom to which they are bonded, form a 5-, 6-, 7- or 8-membered ring), (provided that when the substituent is two or more, then said substituents may be the same or different), and the number of the substituent, Y, is 1, 2, 3 or 4; or Y is an alkylene group as bonded to the adjacent substituting positions to form a 5-, 6-, 7- or 8-membered ring;

W is a substituent freely selected from a halogen atom, a C₁-C₆ alkyl group, a C₁-C₄ haloalkyl group, a C₁-C₄alkoxy group, a C₁-C₄ haloalkoxy group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a C₁-C₄ haloalkylsulfenyl group, a C₁-C₄ haloalkylsulfinyl group, a C₁-C₄ haloalkylsulfonyl group, a C₂-C₄ alkenyl group, a C₂-C₄ haloalkenyl group, a C₂-C₄ alkenyloxy group, a C₂-C₄ haloalkenyloxy group, a C₂-C₄ alkenylsulfenyl group, a C₂-C₄ alkenylsulfinyl group, a C₂-C₄ alkenylsulfonyl group, a C₂-C₄ haloalkenylsulfenyl group, a C₂-C₄ haloalkenylsulfinyl group, a C₂-C₄ haloalkenylsulfonyl group, a C₂-C₄ alkynyl group, a C₂-C₄ haloalkynyl group, a C₂-C₄ alkynyloxy group, a C₂-C₄ haloalkynyloxy group, a C₂-C₄ alkynylsulfenyl group, a C₂-C₄ alkynylsulfinyl group, a C₂-C₄ alkynylsulfonyl group, a C₂-C₄ haloalkynylsulfenyl group, a C₂-C₄ haloalkynylsulfinyl group, a C₂-C₄ haloalkynylsulfonyl group, NO₂, CN, a formyl group, a C₂-C₆ alkoxycarbonyl group, a C₂-C₆ alkylcarbonyl group, a C₂-C₆ haloalkylcarbonyl group, a C₂-C₆ alkylcarbonyloxy, group, and —NU¹U², (provided that when the substituent is two or more, then said substituents may be the same or different), and the number of the substituent, W, is 1, 2, 3 or 4;

T¹ represents a C₁-C₂₀ alkyl group, a C₂-C₆ alkenyl group, a C₁-C₆ haloalkyl group, a C₁-C₄ alkoxy-C₁-C₄ alkyl group, a C₃-C₆ halocycloalkyl group, a C₁-C₄ alkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₃-C₆ cycloalkyl group optionally substituted by a C₁-C₃ alkyl group, a cycloalkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a cyclopropyl group substituted by both a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group and a C₁-C₄ alkyl group, a C₃-C₄ cycloalkyl group substituted by both a phenyl group optionally substituted by a halogen or a C₁-C₄ alkoxy group, and a halogen, a cyclopropyl group substituted by both a C₂-C₄ alkenyl group optionally substituted by a halogen, and a C₁-C₄ alkyl group, a C₂-C₄ alkenyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₁-C₁₂ alkoxy group, a C₁-C₄ haloalkoxy group, a C₂-C₅ alkenyloxy group, a C₃-C₆ cycloalkoxy group optionally substituted by a C₁-C₃ alkyl group, a benzyloxy group, a C₂-C₅ alkoxycarbonyl group, —NU¹U², a phenylamino group, a phenyl group optionally substituted by Z, a phenoxy group optionally substituted by Z, a phenylthio group optionally substituted by Z, a naphthyl group optionally substituted by Z, or a 5-membered or 6-membered heterocyclic group optionally substituted by Z, (said heterocyclic group being selected from thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl, thiazolinyl and 3(2H)-pyridazinone groups);

T² and T³ each independently represent OH, a phenyl group, a C₁-C₆ alkyl group, a C₁-C₆ alkoxy group, or a C₁-C₄ alkylsulfenyl group;

T⁴, T⁵ and T⁵ each independently represent H, a C₁-C₆ alkyl group, a C₁-C₆ alkenyl group, a C₃-C₆ cycloalkyl group optionally substituted by a C₁-C₃ alkyl group, or a benzyl group; or any two of T⁴, T⁵ and T⁶ may, together with the nitrogen atom to which they are bonded, form a 5-, 6-, 7- or 8-membered cyclic group optionally containing oxygen, nitrogen and/or sulfur atoms;

X and Z are independently substituents as freely selected from a halogen atom, a C₁-C₄ alkyl group, a C₁-C₄haloalkyl group, a C₁-C₄ alkoxy group, a C₁-C₄ haloalkoxy group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a C₂-C₅ alkenylsulfenyl group, a C₂-C₅ alkenylsulfinyl group, a C₂-C₅ alkenylsulfonyl group, a C₁-C₄ haloalkylsulfenyl group, a C₁-C₄ haloalkylsulfinyl group, a C₁-C₄ haloalkylsulfonyl group, NO₂, CN, CHO, OH, —NU¹U², a phenyl group, a phenoxy group, and a C₂-C₅ alkoxycarbonyl group, (provided that when the substituent is two or more, then said substituents may be the same or different), and the number of the substituent, X and Z, is 1, 2, 3, 4 or 5 each;

T⁷ and T⁸ each independently represent H, or a phenyl, benzyl or C₁-C₆ alkyl group, or T⁷ and T⁸ may, together with the carbon atom to which they are bonded, form a 5-, 6-, 7- or 8-membered ring; and

U¹ and U² each independently represent H, a C₁-C₆ alkyl, C₂-C₅ alkylcarbonyl, phenyl or benzyl group, or U¹ and U² may, together with the nitrogen atom to which they are bonded, form a 5-, 6-, 7- or 8-membered ring.

[2] Ethylene derivatives of the above-mentioned [1], in which;

Q is a phenyl group optionally substituted by G, a naphthyl group optionally substituted by G, or a heterocyclic group optionally substituted by R, (said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,4,5-tetrazinyl, pyrazolinyl, imidazolinyl, imidazolinone or imidazolidinedione group;

A is a phenyl group optionally substituted by W, a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y, said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl or imidazolinyl group;

B is H, a C₁-C₄ alkyl group, a C₁-C₄ haloalkyl group, a C₂-C₄ alkoxyalkyl group, CH₃OC₂H₄OCH₂, a C₁-C₄ alkylsulfonyl group, a phenylsulfonyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, —SO₂CF₃, a C₂-C₈ dialkylaminosulfonyl group, a C₂-C₉ dialkylaminothiocarbonyl group, a C₃-C₉ alkoxycarbonylalkyl group, —C(═O)T¹, —P(═O)T²T³, —P(═S)T²T³, an alkali metal atom, an alkaline earth metal atom, or NHT⁴T⁵T⁶; and

T¹ is a C₁-C₂₀, alkyl group, a C₂-C₆ alkenyl group, a C₁-C₄ haloalkyl group, a C₁-C₄ alkoxy-C₁-C₄ alkyl group, a C₁-C₄ alkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₃-C₆ halocycloalkyl group, a C₃-C₆ cycloalkyl group optionally substituted by a C₁-C₃ alkyl group, a cycloalkyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a cyclopropyl group substituted by both a phenyl optionally substituted by a halogen or a C₁-C₄ alkyl group, and a C₁-C₄ alkyl group, a C₃-C₄ cycloalkyl group substituted by both a phenyl group optionally substituted by a halogen or a C₁-C₄ alkoxy group and a halogen, a cyclopropyl group substituted by both a C₂-C₄ alkenyl group optionally substituted by a halogen and a C₁-C₄ alkyl group, a C₂-C₄ alkenyl group substituted by a phenyl group optionally substituted by a halogen or a C₁-C₄ alkyl group, a C₁-C₁₂ alkoxy group, a C₁-C₄ haloalkoxy group, a C₂-C₅ alkenyloxy group, a C₃-C₆ cycloalkoxy group optionally substituted by a C₁-C₃ alkyl group, a benzyloxy group, a C₂-C₅ alkoxycarbonyl group, a phenyl group optionally substituted by Z, a phenoxy group optionally substituted by Z, a phenylthio group, a naphthyl group, or a heterocyclic group optionally substituted by Z, said heterocyclic group being selected from thienyl, furyl, oxazolyl, thiazolyl, pyrazolyl and pyridinyl groups.

[3] Ethylene derivatives of the above-mentioned [2], in which;

Q is a phenyl group optionally substituted by G, a naphthyl group optionally substituted by G, or a heterocyclic group optionally substituted by R, said heterocyclic group being

A is a phenyl group optionally substituted by W, a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y, said heterocyclic group being

provided that, when (a) Q is any of Q-1, Q-2, Q-3 or Q-4, then A is a phenyl group optionally substituted by W, a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y, (said heterocyclic group being any of A-5, A-6, A-7, A-8, A-9, A-10, A-11, A-12, A-13, A-14, A-15, A-16, A-17, A-18, A-19, A-20, A-21, A-22, A-23, A-24, A-25, A-26, A-27, A-28, A-29, A-30, A-31, A-32, A-33, A-34, A-35, A-36, A-37, A-38, A-39, A-40, A-41, A-42, A-43, A-44, A-45, A-46, A-47, A-48, A-49, A-50, A-51, A-52, A-53, A-57, A-58, A-59, A-60, A-61, A-62, A-63, A-64, A-65, A-66, A-67, A-68, A-69, A-70, A-71, A-72, A-73, A-74 or A-75),

(b) when Q is Q-12, then A is a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y, (said heterocyclic group being any of A-1, A-2, A-3, A-4, A-5, A-6, A-7, A-8, A-9, A-10, A-11, A-12, A-13, A-14, A-15, A-16, A-17, A-18, A-19, A-20, A-21, A-22, A-23, A-24, A-25, A-26, A-27, A-28, A-29, A-30, A-31, A-32, A-33, A-34, A-35, A-36, A-37, A-38, A-39, A-40, A-41, A-42, A-43, A-44, A-45, A-46, A-47, A-48, A-49, A-50, A-51, A-52, A-53, A-54, A-55, A-56, A-57, A-58, A-59, A-60, A-61, A-62, A-63, A-64, A-65, A-66, A-67, A-68, A-69, A-70, A-71, A-72, A-73, A-74 or A-75),

(c) when Q is any of Q-52, Q-53 or Q-54, then A is a heterocyclic group optionally substituted by Y, (said heterocyclic group being any of A-5, A-6, A-7, A-8, A-9, A-10, A-11, A-12, A-13, A-14, A-15, A-16, A-17, A-18, A-19, A-20, A-21, A-22, A-23, A-24, A-25, A-26, A-27, A-28, A-29, A-30, A-31, A-32, A-33, A-34, A-35, A-36, A-37, A-38, A-39, A-40, A-41, A-42, A-43, A-44, A-45, A-46, A-47, A-48, A-49, A-50, A-51, A-52, A-53, A-60, A-63, A-64, A-65, A-66, A-67, A-68, A-69, A-70, A-71, A-72, A-73, A-74 or A-75),

(d) when Q is any of Q-23, Q-24, Q-43, Q-44, Q-45, Q-46 or Q-49, then A is a naphthyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y, (said heterocyclic group being any of A-1, A-2, A-3, A-4, A-5, A-6, A-7, A-8, A-9, A-10, A-11, A-12, A-13, A-14, A-15, A-16, A-17, A-18, A-19, A-20, A-21, A-22, A-23, A-24, A-25, A-26, A-27, A-28, A-29, A-30, A-31, A-32, A-33, A-34, A-35, A-36, A-37, A-38, A-39, A-40, A-41, A-42, A-43, A-44, A-45, A-46, A-47, A-48, A-49, A-50, A-51, A-52, A-53, A-54, A-55, A-56, A-57, A-58, A-59, A-60, A-61, A-62, A-63, A-64, A-65, A-66, A-67, A-68, A-69, A-70, A-71, A-72, A-73, A-74 or A-75),

(e) when Q is any of Q-37, Q-38, Q-39, Q-40, Q-41 or Q-42, then A is a heterocyclic group optionally substituted by Y, (said heterocyclic group being any of A-1, A-2, A-3, A-4, A-5, A-6, A-1, A-8, A-9, A-10, A-11, A-12, A-13, A-14, A-15, A-16, A-17, A-18, A-19, A-20, A-21, A-22, A-23, A-24, A-25, A-26, A-27, A-28, A-29, A-30, A-31, A-32, A-33, A-34, A-35, A-36, A-37, A-38, A-39, A-40, A-41, A-42, A-43, A-44, A-45, A-46, A-47, A-48, A-49, A-50, A-51, A-52, A-53, A-57, A-58, A-59, A-60, A-61, A-62, A-63, A-64, A-65, A-66, A-67, A-68, A-69, A-70, A-71, A-72, A-73, A-74 or A-75),

(f) when Q is a phenyl group optionally substituted by G, then A is a heterocyclic group optionally substituted by Y, said heterocyclic group being any of A-5, A-6, A-7, A-8, A-9, A-10, A-11, A-12, A-13, A-14, A-19, A-20, A-21, A-22, A-23, A-24, A-25, A-26, A-27, A-28, A-29, A-30, A-31, A-32, A-33, A-34, A-35, A-36, A-37, A-38, A-39, A-40, A-41, A-42, A-43, A-44, A-45, A-46, A-47, A-48, A-49, A-50, A-51, A-52, A-53, A-60, A-61, A-62, A-63, A-64, A-65, A-66, A-67, A-68, A-69, A-70, A-71, A-72, A-73, A-74 or A-75,

(g) when Q is a naphthyl group optionally substituted by G, then A is a heterocyclic group optionally substituted by Y, (said heterocyclic group being any of A-1, A-2, A-5, A-6, A-7, A-8, A-9, A-10, A-11, A-12, A-13, A-14, A-15, A-16, A-17, A-18, A-19, A-20, A-21, A-22, A-23, A-24, A-25, A-26, A-27, A-28, A-29, A-30, A-31, A-32, A-33, A-34, A-35, A-36, A-37, A-38, A-39, A-40, A-41, A-42, A-43, A-44, A-45, A-46, A-47, A-48, A-49, A-50, A-51, A-52, A-53, A-54, A-55, A-56, A-57, A-58, A-59, A-60, A-61, A-62, A-63, A-64, A-65, A-66, A-67, A-68, A-69, A-70, A-71, A-72, A-73, A-74 or A-75,

R¹ is selected from a halogen atom, a C₁-C₁₀ alkyl group, a C₂-C₆ alkenyl group, a C₂-C₆ alkynyl group, a C₁-C₆ haloalkyl group, a C₁-C₆ alkoxy group, a C₂-C₆ alkenyloxy group, NO₂, CN, —NU¹U², OH, a C₂-C₇ alkoxycarbonyl group, a C₂-C₄ alkoxyalkyl group, a C₂-C₄ alkylcarbonyl group, a phenyl group optionally substituted by X, a pyridyl group optionally substituted by X, a thienyl group optionally substituted by X, and —N═CT⁷T⁸ (in which T⁷ and T⁸ each independently represent H, a phenyl, benzyl or C₁-C₆ alkyl group, or T⁷ and T⁸ may, together with the carbon atom to which they are bonded, form a 5-, 6-, 7- or 8-membered ring); or may, together with the adjacent R, form a 5-, 6-, 7- or 8-membered ring as an alkylene group

Y¹ is selected from a halogen atom, a C₁-C₁₀ alkyl group, a C₁-C₆ haloalkyl group, a C₁-C₆ alkoxy group, a C₂-C₆ alkenyloxy group, NO₂, CN, —NU¹U², OH, a C₂-C₇ alkoxycarbonyl group, a C₂-C₄ alkoxyalkyl group, a phenyl group optionally substituted by X, and —N═CT⁷T⁸ (in which T⁷ and T⁸ each independently represent H, or a phenyl, benzyl or C₁-C₆ alkyl group, or T⁷ and T⁸ may, together with the carbon atom to which they are bonded), form a 5-, 6-, 7- or 8-membered ring); or may, togeher with the adjacent Y¹, form a 5-, 6-, 7- or 8-membered ring an alkylene group;

X is a substituent of which the number is from 1 to 4 and which is freely selected from a halogen atom, a C₁-C₄ alkyl group, a C₁-C₄ haloalkyl group, a C₁-C₄ alkoxy group, a C₁-C₄ haloalkoxy group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a C₂-C₅alkenylsulfenyl group, a C₂-C₅ alkenylsulfinyl group, a C₂-C₅alkenylsulfonyl group, a C₁-C₄ haloalkylsulfenyl group, a C₁-C₄ haloalkylsulfinyl group, a C₁-C₄ haloalkylsulfonyl group, NO₂, CN, CHO, OH, —NU¹U², a phenyl group, a phenoxy group, and a C₂-C₅ alkoxycarbonyl group, (provided that when the number of the substituent, X, is two or more then said substituents may be the same or different);

Z is a substituent of which the number is from 1 to 4 and which is freely selected from a halogen atom, a C₁-C₄ alkyl group, a C₁-C₄ haloalkyl group, a C₁-C₄ alkoxy group, a C₁-C₄ haloalkoxy group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a C₁-C₄ alkenylsulfenyl group, a C₁-C₄ alkenylsulfinyl group, a C₁-C₄ alkenylsulfonyl group, NO₂, CN, —NU¹U², a phenyl group, a phenoxy group, and a C₂-C₅ alkoxycarbonyl group, (provided that when the number of the substituent, Z, is two or more, then said substituents may be the same or different);

m indicates the number of the substituents, and is 0, 1, 2 or 3;

n indicates the number of the substituents, and is 0, 1, 2, 3, or 4;

p indicates the number of the substituents, and is 0, 1 or 2;

q indicates the number of the substituents, and is 0 or 1;

(provided that when m, n and p each are an integer of 2 or more, the substituents may be the same or different).

[4] Ethylene derivatives of the above-mentioned [2], in which E is CN.

[5] Ethylene derivatives of the above-mentioned [3], in which E is CN.

[6] Ethylene derivatives of the above-mentioned [2], in which E is a heterocyclic group optionally substituted by a C₁-C₄ alkyl or C₁-C₄ haloalkyl group—(said heterocyclic group being a 2-oxazolyl, 2-thiazolyl, 2-imidazolyl, 1,2,4-triazol-3-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-thiadiazol-3-yl or 1,3,4-oxadiazol-2-yl group)—or is a halogen atom, a C₂-C₄ alkynyl group, a phenylethynyl group optionally substituted by Z, a C₁-C₄ haloalkyl group, CN, NO₂, N₃, CHO, a C₂-C₅ alkylcarbonyl group, a C₂-C₅ alkoxycarbonyl group, a C₂-C₄ alkylaminocarbonyl group, a C₃-C₉ dialkylaminocarbonyl group, a benzoyl group optionally substituted by Z, an aminothiocarbonyl group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a phenylsulfenyl group optionally substituted by Z, a phenylsulfinyl group optionally substituted by Z, a phenylsulfonyl group optionally substituted by Z, —P(═O)T²T³, or —P(═S)T²T³.

[7] Ethylene derivatives of the above-mentioned [3], in which E is a heterocyclic group optionally substituted by a C₁-C₄ alkyl or C₁-C₄ haloalkyl group—(said heterocyclic group being a 2-oxazolyl, 2-thiazolyl, 2-imidazolyl, 1,2,4-triazol-3-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-thiadiazol-3-yl or 1,3,4-oxadiazol-2-yl group)—or is a halogen atom, a C₂-C₄ alkynyl group, a phenylethynyl group optionally substituted by Z, a C₁-C₄ haloalkyl group, CN, NO₂, N₃, CHO, a C₂-C₅ alkylcarbonyl group, a C₂-C₅ alkoxycarbonyl group, a C₂-C₄ alkylaminocarbonyl group, a C₃-C₉ dialkylaminocarbonyl group, a benzoyl group optionally substituted by Z, an aminothiocarbonyl group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a phenylsulfenyl group optionally substituted by Z, a phenylsulfinyl group optionally substituted by Z, a phenylsulfonyl group optionally substituted by Z, —P(═O)T²T³, or —P(═S)T²T³.

[8] Ethylene derivatives of the above-mentioned [4], in which Q is a phenyl group optionally substituted by G, an oxazolyl group optionally substituted by R, a thiazolyl group optionally substituted by R, a pyrazolyl group optionally substituted by R, a 1,2,3-triazolyl group optionally substituted by R, a pyridinyl group optionally substituted by R, or a pyrimidinyl group optionally substituted by R.

[9] Ethylene derivatives of the above-mentioned [8], in which Q is a phenyl group optionally substituted by G.

[10] Ethylene derivatives of the above-mentioned [8], in which Q is an oxazolyl group optionally substituted by R or a 1,2,3-triazolyl group optionally substituted by R.

[11] Ethylene derivatives of the above-mentioned [8], in which Q is a thiazolyl group optionally substituted by R.

[12] Ethylene derivatives of the above-mentioned [8], in which Q is a pyrazolyl group optionally substituted by R.

[13] Ethylene derivatives of the above-mentioned [5], in which Q is a phenyl group optionally substituted by G, or is Q-9, Q-10, Q-11, Q-12, Q-13, Q-14, Q-25, Q-26, Q-27, Q-28, Q-29, Q-30, Q-44, Q-45, Q-46, Q-47, Q-52, Q-53, Q-54, Q-55, Q-56 or Q-57.

[14] Ethylene derivatives of the above-mentioned [7], in which Q is a phenyl group optionally substituted by G, or is Q-9, Q-10, Q-11, Q-12, Q-13, Q-14, Q-25, Q-26, Q-27, Q-28, Q-29, Q-30, Q-44, Q-45, Q-46, Q-47, Q-52, Q-53, Q-54, Q-55, Q-56 or Q-57.

[15] Ethylene derivatives of the above-mentioned [13], in which Q is Q-10, Q-44, Q-45, Q-46 or Q-47.

[16] Ethylene derivatives of the above-mentioned [13], in which Q is Q-12, Q-13 or Q-14.

[17] Ethylene derivatives of the above-mentioned [13], in which Q is Q-25, Q-26, Q-27, Q-28, Q-29 or Q-30.

[18] Ethylene derivatives of the above-mentioned [13], in which Q is a phenyl group optionally substituted by G.

[19] Ethylene derivatives of the above-mentioned [2], in which A is a phenyl group optionally substituted by W, a thiazolyl group optionally substituted by Y, a pyrazolyl group optionally substituted by Y, a pyridinyl group optionally substituted by Y, or a pyrimidinyl group optionally substituted by Y.

[20] Ethylene derivatives of the above-mentioned [3], in which;

Q is a phenyl group optionally substituted by G, a naphthyl group, Q-31, Q-32, Q-33, Q-34, Q-35, Q-36, Q-37, Q-44, Q-45, Q-46, Q-49,

Y² is a halogen atom, a C₁-C₄ alkyl group, a C₁-C₄ haloalkyl group, a C₁-C₄ alkoxy group, NO₂, CN, or a C₂-C₅ alkoxycarbonyl group; and

Y³ is a halogen atom, a C₁-C₄ alkyl group, a C₁-C₆ haloalkyl group, a C₂-C₄ alkoxyalkyl group, or a phenyl group optionally substituted by X.

[21] Ethylene derivatives of the above-mentioned [20], in which E is CN.

[22] Ethylene derivatives of the above-mentioned [20], in which E is a heterocyclic group optionally substituted by a C₁-C₄ alkyl or C₁-C₄ haloalkyl group—(said heterocyclic group being a 2-oxazolyl, 2-thiazolyl, 2-imidazolyl, 1,2,4-triazol-3-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-thiadiazol-3-yl or 1,3,4-oxadiazol-2-yl group)—or is a halogen atom, a C₂-C₄ alkynyl group, a phenylethynyl group optionally substituted by Z, a C₁-C₄ haloalkyl group, CN, NO₂, N₃, CHO, a C₂-C₅ alkylcarbonyl group, a C₂-C₆ alkoxycarbonyl group, a C₂-C₄ alkylaminocarbonyl group, a C₃-C₉ dialkylaminocarbonyl group, a benzoyl group optionally substituted by Z, an aminothiocarbonyl group, a C₁-C₄ alkylsulfenyl group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, a phenylsulfenyl group optionally substituted by Z, a phenylsulfinyl group optionally substituted by Z, a phenylsulfonyl group optionally substituted by Z, —P(═O)T²T³, or —P(═S)T²T³.

[23] Ethylene derivatives of the above-mentioned [1], which are selected from the following:

[24] An agricultural chemical comprising, as the active ingredient, one or more ethylene derivatives of the above-mentioned [1] to [23]

[25] An agent for preventing the attachment of aquatic organisms containing, as an active ingredient, one or more ethylene derivatives of the above-mentioned [1] to [23].

MODES OF CARRYING OUT THE INVENTION

The moiety —C(E)=C(OB)— of the compounds (I) of the present invention includes two isomers of E-form and Z-form, both of which are within the scope of the invention.

It will be understood that the compounds of formula (I) of the present invention where the substituent B is a hydrogen atom exist as tautomers to be represented by the following:

Although the compounds (I) will exist essentially as the enol-form (1′), they could be as the tautomer form (2) under some conditions. It should be understood that the present invention includes all these three tautomers and their mixtures.

Now, preferred embodiments of Q, A, B, E, G, R, R¹, Y, Y¹, Y², W, X, Z, T¹, T², T³, T⁴, T⁵, T⁶, T⁷, T⁸, U¹, U², m, n, p and q are referred to hereinunder.

The heterocyclic group for Q, A and B indicates the following meanings.

Specifically, thienyl is thiophen-2-yl or thiophen-3-yl; furyl is furan-2-yl or furan-3-yl; pyrrolyl is pyrrol-1-yl, pyrrol-2-yl or pyrrol-3-yl; oxazolyl is oxazol-2-yl, oxazol-3-yl, oxazol-4-yl or oxazol-5-yl; thiazolyl is thiazol-2-yl, thiazol-4-yl or thiazol-5-yl; imidazolyl is imidazol-1-yl, imidazol-2-yl or imidazol-4-yl; isoxazolyl is isoxazol-3-yl, isoxazol-4-yl or isoxazol-5-yl; isothiazolyl is isothiazol-3-yl, isothiazol-4-yl or isothiazol-5-yl; pyrazolyl is pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl or pyrazol-5-yl; 1,3,4-oxadiazolyl is 1,3,4-oxadiazol-2-yl; 1,3,4-thiadiazolyl is 1,3,4-thiadiazol-2-yl; 1,2,4-oxadiazolyl is 1,2,4-oxadiazol-3-yl or 1,2,4-oxadiazol-5-yl; 1,2,4-thiadiazolyl is 1,2,4-thiadiazol-3-yl or 1,2,4-thiadiazol-5-yl; 1,2,4-triazolyl is 1,2,4-triazol-1-yl, 1,2,4-triazol-3-yl or 1,2,4-triazol-4-yl; 1,2,3-thiadiazolyl is 1,2,3-thiadiazol-4-yl or 1,2,3-thiadiazol-5-yl; 1,2,3-triazolyl is 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl or 1,2,3-triazol-4-yl; 1,2,3,4-tetrazolyl is 1,2,3,4-tetrazol-1-yl, 1,2,3,4-tetrazol-2-yl or 1,2,3,4-tetrazol-5-yl; pyridinyl is pyridin-2-yl, pyridin-3-yl or pyridin-4-yl; pyrimidinyl is pyrimidin-2-yl, pyrimidin-4-yl or pyrimidin-5-yl; pyrazinyl is pyrazin-2-yl; pyridazinyl is pyridazin-3-yl or pyridazin-4-yl; 1,3,5-triazinyl is 1,3,5-triazin-2-yl; 1,2,4-triazinyl is 1,2,4-triazin-3-yl, 1,2,4-triazin5-yl or 1,2,4-triazin-6-yl; 1,2,4,5-tetrazinyl is 1,2,4,5-tetrazin-3-yl; pyrazolinyl is 3-pyrazolin-1-yl, 3-pyrazolin-3-yl, 3-pyrazolin-4-yl or 3-pyrazolin-5-yl; imidazolinyl is 1-imidazolin-3-yl, 1-imidazolin-2yl, 1-imidazolin-4-yl or 4-imidazolin-2-yl; oxazolinyl is 2-oxazolin-2-yl, 2-oxazolin-4-yl or 2-oxazolin-5-yl; isoxazolinyl is 2-isoxazolin-3-yl, 2-isoxazolin-4-yl or 2-isoxazolin-5-yl; thiazolinyl is 2-thiazolin-2-yl, 2-thiazolin-4-yl or 3-thiazolin-2-yl; imidazolidinon-yl is imidazolidin-2-on-1-yl; imidazolinon-yl is 2-imidazolinon-1-yl; and 3(2H)-pyridazinon-yl is 3(2H)-pyridazinon-2-yl, 3(2H)-pyridazinon-4-yl, 3(2H)-pyridazinon-5-yl or 3(2H)-pyridazinon-6-yl.

Preferred scope of Q is the following groups.

QI: phenyl, thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,4,5-tetrazinyl.

QII: phenyl, thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl.

QIII: phenyl, thienyl, oxazolyl, thiazolyl, pyrazolyl, pyridinyl, pyrimidinyl, 1,2,3-triazolyl.

QIV: phenyl.

QV: oxazolyl.

QVI: thiazolyl.

QVII: pyrazolyl.

QVIII: pyrimidinyl.

QIX: 1,2,3-triazolyl.

Preferred scope of A is the following groups.

AI: phenyl, thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl.

AII: phenyl, thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolyl, imidazolyl, 1,2,3-triazolyl, 1,2,3-thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl.

AIII: phenyl, thiazolyl, pyrazolyl, pyridinyl, pyrimidinyl.

AIV: thiazolyl, pyrazolyl, pyridinyl.

AV: thiazolyl.

AVI: pyrazolyl.

AVII: pyridinyl

Preferred scope of B is the following groups.

BI: H, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₂-C₄ alkoxyalkyl, CH₃OC₂H₄ OCH₂, C₁-C₄ alkylsulfonyl, phenylsulfonyl optionally substituted by halogen or C₁-C₄ alkyl, —SO₂CF₃, C₂-C₈ dialkylaminosulfonyl, C₃-C₉ dialkylaminothiocarbonyl, C₃-C₉ alkoxycarbonylalkyl, —C(═O)T¹, —P(═O)T²T³, —P(═S)T²T³, alkali metal, alkaline earth metal or NHT⁴T⁵T⁶.

BII: H, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₂-C₄ alkoxyalkyl, CH₃ OC₂H₄OCH₂, C₁-C₄ alkylsulfonyl, —SO₂ CF₃, —C(═O)T¹, alkali metal, alkaline earth metal or NHT⁴T⁵T⁶.

BIII: H, C₂-C₄ alkoxyalkyl, C₁-C₄ alkylsulfonyl, —SO₂CF₃, —C(═O)T¹, alkali metal, alkaline earth metal, NHT⁴T⁵T⁶.

BIV: C₂-C₄ alkoxyalkyl, C₁-C₄ alkylsulfonyl, —SO₂CF₃, —C(═O)T¹, alkali metal, alkaline earth metal or NHT⁴T⁵T⁶.

Preferred scope of E is the following groups.

EI: halogen, C₂-C₄ alkynyl, phenylethynyl optionally substituted by Z, C₁-C₄ haloalkyl, CN, NO₂, N₃, CHO, C₃-C₆ alkylcarbonyl, C₂-C₆ alkoxycarbonyl, C₂-C₄ alkylaminocarbonyl, C₃-C₉ dialkylaminocarbonyl, benzoyl optionally substituted by Z, aminothiocarbonyl, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, phenylsulfenyl optionally substituted by Z, phenylsulfinyl optionally substituted by Z, phenylsulfonyl optionally substituted by Z, —P(═O)T²T³, —P(═S)T²T³.

EII: halogen, C₂-C₄ alkynyl, phenylethynyl optionally substituted by Z, CN, C₂-C₅ alkylcarbonyl, C₂-C₆ alkoxycarbonyl, C₂-C₄ alkylaminocarbonyl, C₃-C₉ dialkylaminocarbonyl, benzoyl optionally substituted by Z, aminothiocarbonyl, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, phenylsulfenyl optionally substituted by Z, phenylsulfinyl optionally substituted by Z, phenylsulfonyl optionally substituted by Z or —P(═O)T²T³.

EIII: CN.

Preferred scope of G is the following groups.

GI: substituents freely selected from halogen, C₁-C₆ alkyl, C₂-C₄ alkenyl, C₂-C₄ alkynyl, C₁-C₄ haloalkyl, C₂-C₄ haloalkenyl, C₂-C₄ haloalkynyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, C₁-C₆ alkoxy, C₂-C₄ alkenyloxy, C₂-C₄ alkynyloxy, C₁-C₄ haloalkoxy, C₂-C₄ haloalkenyloxy, C₂-C₄ haloalkynyloxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₄ alkenylsulfenyl, C₂-C₄ alkenylsulfinyl, C₂-C₄ alkenylsulfonyl, C₂-C₄ alkynylsulfenyl, C₂-C₄ alkynylsulfinyl, C₂-C₄ alkynylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, C₂-C₄ haloalkenylsulfenyl, C₂-C₄ haloalkenylsulfinyl, C₂-C₄ haloalkenylsulfonyl, C₂-C₄ haloalkynylsulfenyl, C₂-C₄ haloalkynylsulfinyl, C₂-C₄ haloalkynylsulfonyl, NO₂, CN, —NU¹U², methoxy substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₂-C₆ alkoxycarbonyl, C₂-C₄ alkoxyalkyl, C₂-C₄ alkylcarbonyl, C₂-C₄ haloalkylcarbonyl, C₂-C₅ alkylcarbonyloxy, C₂-C₅ haloalkylcarbonyloxy, C₃-C₇ dialkylaminocarbonyloxy, phenyl optionally substituted by Z, phenoxy optionally substituted by Z, benzoyl optionally substituted by Z, pyridyl optionally substituted by Z, and pyridyloxy optionally substituted by Z (provided that when the substituent is two or more, said substituents may be the same or different) and the number of the substituent, G, is 1, 2, 3 or 4, or G is an alkylene group as bonded to the adjacent substituting positions to form a 5-, 6-, 7- or 8-membered ring.

GII: substituents freely selected from halogen, C₁-C₆ alkyl, C₂-C₄ alkenyl, C₂-C₄ alkynyl, C₁-C₄ haloalkyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, C₁-C₆ alkoxy, C₂-C₄ alkenyloxy, C₂-C₄ alkynyloxy, C₁-C₄ haloalkoxy, C₂-C₄ haloalkenyloxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₄ alkenylsulfenyl, C₂-C₄ alkenylsulfinyl, C₂-C₄ alkenylsulfonyl, C₁-C₄ alkynylsulfenyl, C₂-C₄ alkynylsulfinyl, C₂-C₄ alkynylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, C₂-C₄ haloalkenylsulfenyl, C₂-C₄ haloalkenylsulfinyl, C₂-C₄ haloalkenylsulfonyl, methoxy substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₂-C₅ alkoxycarbonyl, C₂-C₅ alkylcarbonyloxy, C₂-C₅ haloalkylcarbonyloxy, phenoxy optionally substituted by Z, and pyridyloxy optionally substituted by Z (provided that the number of the substituent is two or more, said substituents may be the same or different), and the number of the substituent, G, is 1, 2 or 3.

GIII: substituents freely selected from halogen, C₁-C₆ alkyl, C₁-C₄ haloalkyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, C₁-C₆ alkoxy, C₂-C₄ alkenyloxy, C₂-C₄ alkynyloxy, C₁-C₄ haloalkoxy, C₂-C₄ haloalkenyloxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₄ alkenylsulfenyl, C₂-C₄ alkenylsulfinyl, C₂-C₄ alkenylsulfonyl, C₂-C₄ alkynylsulfenyl, C₂-C₄ alkynylsulfinyl, C₂-C₄ alkynylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, C₂-C₄ haloalkenylsulfenyl, C₂-C₄ haloalkenylsulfinyl, C₂-C₄ haloalkenylsulfonyl, methoxy substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₂-C₅ alkoxycarbonyl, C₂-C₅ alkylcarbonyloxy, phenoxy optionally substituted by Z, and pyridyloxy optionally substituted by Z (provided that when the substituent is two or more, said substituents may be the same or different), and the number of the substituent, G, is 1 or 2.

Preferred scope of R is the following group.

RI: substituents freely selected from halogen, C₁-C₆ alkyl, C₁-C₃ alkyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₁-C₆ haloalkyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, C₁-C₄ alkoxy, C₂-C₄ alkenyloxy, C₂-C₄ alkynyloxy, C₁-C₄ haloalkoxy, C₂-C₄ haloalkenyloxy, C₂-C₄ haloalkynyloxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₄ alkenylsulfenyl, C₂-C₄ alkenylsulfinyl, C₂-C₄ alkenylsulfonyl, C₂-C₄ alkynylsulfenyl, C₂-C₄ alkynylsulfinyl, C₂-C₄ alkynylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, C₂-C₄ haloalkenylsulfenyl, C₂-C₄ haloalkenylsulfinyl, C₂-C₄ haloalkenylsulfonyl, NO₂, CN, —NU¹U², naphthyl, C₂-C₄ alkoxycarbonyl, C₂-C₄ alkoxyalkyl, phenyl optionally substituted by X, pyridyl optionally substituted by X, and thienyl optionally substituted by X (provided that when the substituent is two or more, said substituents may be the same or different), and the number of the substituent, R, is 1, 2 or 3, or R is an alkylene group as bonded to the adjacent substituting positions to form a 5-, 6-, 7- or 8-membered ring.

RII: substituents freely selected from halogen, C₁-C₆ alkyl, C₁-C₃ alkyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, NO₂, CN, —NU¹U², naphthyl, C₂-C₄ alkoxycarbonyl, C₂-C₄ alkoxyalkyl, phenyl optionally substituted by X, and pyridyl optionally substituted by X (provided that when the substituents is two or more, said substituents may be the same or different), and the number of the substituent, R, is 1, 2 or 3.

RIII: substituents freely selected from halogen, C₁-C₆ alkyl, C₁-C₃ alkyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, NO₂, CN, —NU¹U², naphthyl, C₂-C₄ alkoxycarbonyl, phenyl optionally substituted by X, and pyridyl optionally substituted by X (provided that when the substituent is two or more, said substituents may be the same or different), and the number of the substituent, R, is 1 or 2.

Depending on the type of the heterocyclic group to be substituted by R, the number of R differs. For the group of 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,3-oxadiazolyl, 1,2,3-thiadiazolyl or 1,2,3,4-tetrazolyl, the number of R is 0 or 1, preferably 1. For the group of thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, 1,3,4-triazolyl, 1,2,4-triazolyl, 1,2,3-triazolyl, 1,3,5-triazinyl, 1,2,4-triazinyl or 1,2,4-triazinyl, the number of R is an integer of from 0 to 2, preferably 1 or 2. For the group of thienyl, furyl, pyrazolyl, imidazolyl, pyrimidinyl, pyrazinyl or pyridazinyl, the number of R is an integer of from 0 to 3, preferably an integer of from 0 to 2, more preferably 1 or 2. For the group of pyrrolyl, pyridinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl or thiazolinyl, the number of R is an integer of from 0 to 4, preferably an integer of from 0 to 3, more preferably 1 or 2.

Preferred scope of Y is the following groups.

YI: substituents freely selected from halogen, C₁-C₅ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₂-C₄ alkenyloxy, C₂-C₄ alkynyloxy, C₁-C₄ haloalkoxy, C₂-C₄ haloalkenyloxy, C₂-C₄ haloalkynyloxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₄ alkenylsulfenyl, C₂-C₄ alkenylsulfinyl, C₂-C₄ alkenylsulfonyl, C₂-C₄ alkynylsulfenyl, C₂-C₄ alkynylsulfinyl, C₂-C₄ alkynylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₂-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, C₂-C₄ haloalkenylsulfenyl, C₂-C₄ haloalkenylsulfinyl, C₂-C₄ haloalkenylsulfonyl, C₂-C₄ haloalkynylsulfenyl, C₂-C₄ haloalkynylsulfinyl, C₂-C₄ haloalkynylsulfonyl, NO₂, CN, —NU¹U², C₂-C₄ alkoxycarbonyl, C₂-C₄ alkoxyalkyl, C₂-C₄ alkylcarbonyloxy, C₂-C₄ haloalkylcarbonyloxy, and phenyl optionally substituted by X (provided that the substituent is two or more, said substituents may be the same or different) and the number of the substituent, Y, is 1, 2 or 3.

YII: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, NO₂, CN, C₂-C₄ alkoxycarbonyl, and phenyl optionally substituted by X (provided that when the substituent is two or more, said substituents may be the same or different) and the number of the substituent, Y, is 1, 2 or 3.

Depending on the type of the heterocyclic group to be substituted by Y, the number of Y differs. For the group of 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,3-thiadiazolyl or 1,2,3,4-tetrazolyl, the number of Y is 0 or 1, preferably 1. For the group of thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, 1,3,4-triazolyl, 1,2,4-triazolyl, 1,2,3-triazolyl, 1,3,5-triazinyl, 1,2,4-triazinyl or 1,2,4-triazinyl, the number of Y is an integer of from 0 to 2, preferably 1 or 2. For the group of thienyl, furyl, pyrazolyl, imidazolyl, pyrimidinyl, pyrazinyl or pyridazinyl, the number of Y is an integer of from 0 to 3, preferably an integer of from 0 to 2, more preferably 1 or 2. For the group of pyrrolyl, pyridinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl or thiazolinyl, the number of Y is an integer of from 0 to 4, preferably an integer of from 0 to 3, more preferably 1 or 2.

Preferred scope of W is the following group.

WI: substituents freely selected from halogen, C₁-C₆ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, C₂-C₄ alkenyloxy, C₂-C₄ haloalkenyloxy, C₂-C₄ alkenylsulfenyl, C₂-C₄ alkenylsulfinyl, C₂-C₄ alkenylsulfonyl, C₂-C₄ haloalkenylsulfenyl, C₂-C₄ haloalkenylsulfinyl, C₂-C₄ haloalkenylsulfonyl, C₂-C₄ alkynyloxy, C₂-C₄ alkynylsulfenyl, C₂-C₄ alkynylsulfinyl, C₂-C₄ alkynylsulfonyl, NO₂, CN, C₂-C₄ alkoxycarbonyl, C₂-C₄ alkylcarbonyl, C₂-C₄ haloalkylcarbonyl, C₂-C₄ alkylcarbonyloxy, and —NU¹U² (provided that when the substituent is two or more, said substituents are the same or different) and the number of the substituent, W, is 1, 2, 3 or 4.

WII: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, C₁-C₄ alkenyloxy, C₂-C₄ haloalkenyloxy, C₂-C₄ alkenylsulfenyl, C₂-C₄ alkenylsulfinyl, C₂-C₄ alkenylsulfonyl, C₂-C₄ alkynyloxy, C₂-C₄ alkynylsulfenyl, C₂-C₄ alkynylsulfinyl, C₂-C₄ alkynylsulfonyl, NO₂, and CN (provided that the substituent is two or more, said substituents may be the same or different) and the number of the substituent, W, is 1, 2 or 3.

WIII: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, NO₂, and CN (provided that when the substituent is two or more, the substituents may be the same or different) and the number of the substituent, W, is 1 or 2.

Preferred scope of T¹ is the following groups.

T¹I: C₁-C₁₈ alkyl, C₂-C₈ alkenyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy-C₁-C₄ alkyl, C₁-C₄ alkyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₃-C₆ halocycloalkyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, cycloalkyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₂-C₄ alkenyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₁-C₁₀ alkoxy, C₁-C₄ haloalkoxy, C₂-C₅ alkenyloxy, C₃-C₅ cycloalkoxy optionally substituted by C₁-C₃ alkyl, benzyloxy, C₂-C₅ alkoxycarbonyl, —NU¹U², phenyl optionally substituted by Z, phenoxy optionally substituted by Z, phenylthio optionally substituted by Z, naphthyl, and heterocyclic group optionally substituted by Z, (said heterocyclic group being selected from thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl and 1,2,4-triazinyl groups).

T¹II: C₁-C₁₈ alkyl, C₂-C₆ alkenyl, C₁-C₄ haloalkyl, C₂-C₄ alkoxyalkyl, C₁-C₄ alkyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₃-C₆ cycloalkyl optionally substituted by C₁-C₃ alkyl, cycloalkyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₂-C₄ alkenyl substituted by phenyl optionally substituted by halogen or C₁-C₄ alkyl, C₁-C₁₀ alkoxy, C₁-C₄ haloalkoxy, C₂-C₅ alkenyloxy, C₃-C₆ cycloalkoxy, benzyloxy, C₂-C₅ alkoxycarbonyl, phenyl optionally substituted by Z, phenoxy optionally substituted by Z, phenylthio, naphthyl, and heterocyclic group optionally substituted by Z (said heterocyclic group being selected from thienyl, furyl, oxazolyl, thiazolyl, pyrazolyl and pyridinyl groups).

T¹III: C₁-C₁₇ alkyl, C₂-C₆ alkenyl, C₁-C₄ haloalkyl, C₃-C₄ alkoxyalkyl, C₁-C₄ alkyl substituted by phenyl, C₃-C₆ cycloalkyl optionally substituted C₁-C₃ alkyl, cycloalkyl substituted by phenyl, C₂-C₄ alkenyl substituted by phenyl, C₁-C₈ alkoxy, C₁-C₄ haloalkoxy, C₂-C₅ alkenyloxy, C₃-C₆ cycloalkoxy, benzyloxy, C₂-C₆ alkoxycarbonyl, phenyl optionally substituted by Z, phenoxy optionally substituted by Z, phenylthio, naphthyl, pyrazolyl optionally substituted by Z or pyridinyl optionally substituted by Z.

Preferred scope of T² is the following groups.

T²I: phenyl, C₁-C₄ alkyl, C₁-C₄ alkoxy or C₁-C₄ alkylsulfenyl.

Preferred scope of T³ is the following groups.

T³I: phenyl, C₁-C₆ alkyl, C₁-C₆ alkoxy or C₁-C₄ alkylsulfenyl.

Preferred scope of T⁴ is the following groups.

T⁴I: H, C₁-C₄ alkyl, C₃-C₆ cycloalkyl or benzyl. Also preferred is such that any two of T⁴, T⁵ and T⁶, together with the nitrogen atom to which they are bonded, forms a 5-, 6- or 7-membered ring optionally having oxygen, nitrogen and/or sulfur atoms.

Preferred scope of T⁵ is the following groups.

T⁵I: H, C₁-C₄ alkyl, C₃-C₆ cycloalkyl or benzyl. Also, preferred is such that any two of T⁴, T⁵ and T⁶, together with the nitrogen atom to which they are bonded, forms a 5-, 6- or 7-membered ring optionally having oxygen, nitrogen and/or sulfur atoms.

Preferred scope of T⁶ is the following groups.

T⁶I: H, C₁-C₄ alkyl, C₃-C₆ cycloalkyl or benzyl. Also, preferred is such that any two of T⁴, T⁵ and T⁶, together with the nitrogen atom to which they are bonded, forms a 5-, 6- or 7-membered ring optionally having oxygen, nitrogen and/or sulfur atoms.

Preferred scope of X is the following groups.

XI: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₅ alkenylsulfenyl, C₂-C₅ alkenylsulfinyl, C₂-C₅ alkenylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, NO₂, CN, —NU¹U² and C₂-C₅ alkoxycarbonyl (provided that the substituent is two or more, said substituents may be the same or different) and the substituent, X, is 1, 2 or 3.

XII: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₅ alkenylsulfenyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, and NO₂ (provided that when the substituent is two or more, said substituents may be the same or different) and the number of the substituent, X, is 1, 2 or 3.

XIII: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, and C₁-C₄ alkoxy (provided that when the substituent is two or more, said substituents may be the same or different) and the number of the substituent, X, is 1 or 2.

Depending on the type of the ring to be substituted by X, the number of X differs. For phenyl, the number of X is an integer of from 0 to 5, preferably an integer of from 0 to 3, more preferably an integer of from 0 to 2. For pyridyl, the number of X is an integer of from 0 to 4, preferably 0, 1 or 2, more preferably 0′, or 1. For thienyl, the number of X is an integer of from 0 to 3, preferably 0 or 1.

Preferred scope of Z is the following groups.

ZI: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₅ alkenylsulfenyl, C₂-C₅ alkenylsulfinyl, C₂-C₅ alkenylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl, C₁-C₄ haloalkylsulfonyl, NO₂, CN, —NU¹U² and C₂-C₆ alkoxycarbonyl (provided that when the substituent is two or more, said substituents may be the same or different) and the number of the substituent, Z, is 1, 2, 3 or 4.

ZII: substituents freely selected from halogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkoxy, C₁-C₄ alkylsulfenyl, C₁-C₄ alkylsulfinyl, C₁-C₄ alkylsulfonyl, C₂-C₄ alkenylsulfenyl, C₂-C₅ alkenylsulfinyl, C₂-C₅ alkenylsulfonyl, C₁-C₄ haloalkylsulfenyl, C₁-C₄ haloalkylsulfinyl and C₁-C₄ haloalkylsulfonyl (provided that when the substituent is two or more, said substituents may be the same or different) and the substituent, Z, is 1, 2, 3 or 4.

Depending on the type of the ring to be substituted by Z, the number of Z differs. For phenyl, the number of Z is an integer of from 0 to 5, preferably an integer of from 0 to 4, more preferably 0, 1, 2 or 3, even more preferably 0, 1 or 2. For naphthyl, the number of Z is an integer of from 0 to 7, preferably 0. Where the ring to be substituted by Z is a heterocyclic group, the number of the substituents of Z also differs depending on the type of the heterocyclic group. For the group of 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,3-oxadiazolyl, 1,2,3-thiadiazolyl, 1,2,3,4-tetrazolyl or 1,2,3,5-tetrazolyl, the number of Z is 0 or 1. For the group of thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, 1,3,4-triazolyl, 1,2,4-triazolyl, 1,2,3-triazolyl, 1,3,5-triazinyl, 1,2,4-triazinyl or 1,2,4-triazinyl, the number of z is an integer of from 0 to 2, preferably 1 or 2. For the group of thienyl, furyl, pyrazolyl, imidazolyl, pyrimidinyl, pyrazinyl or pyridazinyl, the number of Z is an integer of from 0 to 3, preferably an integer of from 0 to 2, more preferably 1 or 2. For the group of pyrrolyl, pyridinyl, pyrazolinyl, imidazolinyl, oxazolinyl, isoxazolinyl or thiazolinyl, the number of Z is an integer of from 0 to 4, preferably an integer of from 0 to 2, more preferably 1 or 2.

Preferred scope of T⁷ is the following groups.

T⁷: H, phenyl, benzyl or C₁-C₄ alkyl. Also preferred is such that T⁷ and T⁸, together with the carbon atom to which they are bonded, form a 5-membered or 6-membered ring.

Preferred scope of T⁸ is the following groups.

T⁸I: phenyl, benzyl or C₁-C₄ alkyl. Also preferred is such that T⁷ and T⁸, together with the carbon atom to which they are bonded, form a 5-membered or 6-membered ring.

Preferred scope of U¹ is the following groups.

U¹I: H, C₁-C₄ alkyl or C₂-C₅ alkylcarbonyl. Also preferred is such that U¹ and U², together with nitrogen atom to which they are bonded, form a 5-, 6- or 7-membered ring.

Preferred scope of U² is the following groups.

U²I: H, C₁-C₄ alkyl or C₂-C₅ alkylcarbonyl. Also preferred is such that U¹ and U², together with the carbon atom to which they are bonded, form a 5-, 6- or 7-membered ring.

Preferably, m is 1, 2, or 3, more preferably 1 or 2.

Preferably n is 0, 1, 2 or 3, more preferably 1 or 2.

Preferably, p is 1 or 2.

The above-mentioned preferred groups in the scopes of the preferred substituents can be optionally combined and show the scopes of the preferred compounds of the present invention. Hereinunder mentioned are especially preferred scopes.

Compounds of the invention comprising preferred substituents of QI, AI, BI, EI, GI, RI, YI, WI, T¹I, T²I, T³I, T⁴I, T⁵I, T⁶I, XI, ZI, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QI, AI, BI, EIII, GI, RI, YI, WI, T¹I, T²I, T³I, T⁴I, T⁵I, T⁶I, XI, ZI, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QII, AII, BI, EII, GI, RI, YI, WI, T¹I, T², T³I, T⁴I, T⁵I, T⁶I, XI, ZI, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QII, AII, BI, EIII, GI, RI, YI, WI, T¹I, T²I, T³I, T⁴I, T⁵I, T⁶I, XI, ZI, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIII, AIII, BI, EIII, GI, RI, YI, WI, T¹I, T²I, T³I, T⁴I, T⁵I, T⁶I, XI, ZI, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIII, AIII, BII, EIII, GII, RII, YII, WII, T¹II, T²I, T³I, T⁴I, T⁵I, T⁶I, XII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIII, AIII, BII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIII, AIV, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIV, AIV, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QV, AIII, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QVI, AIII, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QVI, AIV, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QVII, AIII, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QVIII, AIII, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIX, AIII, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIII, AV, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIII, AVI, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T⁵I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Compounds of the invention comprising preferred substituents of QIII, AVII, BIII, EIII, GIII, RIII, YII, WII, T¹III, T²I, T³I, T⁴I, T⁵I, T⁶I, XIII, ZII, T⁷I, T⁸I, U¹I and U²I.

Now, specific examples of Q, A, B, E, G, R, R¹, Y, Y¹, Y², W, X, Z, T¹, T², T³, T⁴, T⁵, T⁶, T⁷, T⁸, U¹ and U² are mentioned below.

The halogen atom for E, G, R, R¹, W, X, Y, Y¹, Y², Y³ and Z includes a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom. Preferred are a fluorine atom, a chlorine atom and a bromine atom.

The alkyl group for B, G, R, R¹, T¹, T², T³, T⁴, T⁵, T⁶, T⁷, T⁸, U¹, U², W, X, Y, Y¹, Y², Y³ and Z may be a straight chain or branched alkyl group having indicated carbon atoms, which includes, for example, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, pentyl-1, pentyl-2, pentyl-3,2-methylbutyl-1, 2-methylbutyl-2,2-methylbutyl-3,3-methylbutyl-1, 2,2-dimethylpropyl-1, hexyl-1, hexyl-2, hexyl-3, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl, 1-ethyl-2-methylpropyl, n-heptyl, n-octyl, n-nonyl, n-undecyl, n-dodecyl, n-tridecyl, n-tetradecyl, n-pentadecyl, n-hexadecyl, n-heptadecyl, n-octadecyl, n-nonadecyl and n-eicosyl groups.

The alkenyl group for G, R, R¹, T¹, T⁴, T⁵, T⁶, Y¹ and W may be a straight chain or branched alkenyl group having indicated carbon atoms, which includes, for example, ethenyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-methyl-2-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-methyl-2-butenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl, 1-methyl-3-butenyl, 2-methyl-3-butenyl, 3-methyl-3-butenyl, 1,1-dimethyl-2-propenyl, 1,2-dimethyl-2-propenyl, 1-ethyl-2-propenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-methyl-2-pentenyl, 4-methyl-2-pentenyl, 1-methyl-3-pentenyl, 2-methyl-3-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4-pentenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,1-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-dimethyl-2-butenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl-2-butenyl, 1,3-dimethyl-3-butenyl, 2,3-dimethyl-2-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-2-butenyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 2-ethyl-2-butenyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl and 1-ethyl-1-methyl-2-propenyl groups.

The alkynyl group for E, G, R, R¹, Y¹ and W may be a straight chain or branched alkynyl group having indicated carbon atoms, which includes, for example, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-methyl-2-propynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-methyl-2-butynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, hexynyl, 1-methyl-3-pentynyl, 1-methyl-4-pentynyl, 2-methyl-3-pentynyl, 2-methyl-4-pentynyl, 3-methyl-4-pentynyl, 4-methyl-2-pentynyl, 1,1-dimethyl-2-butynyl, 1,1-dimethyl-3-butynyl, 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl, 1-ethyl-2-butynyl, 1-ethyl-3-butynyl and 2-ethyl-3-butynyl groups.

The haloalkyl group for B, E, G, R, R¹, T¹, W, X, Y, Y¹, Y², Y³ and Z may be a straight chain or branched haloalkyl group having indicated carbon atoms, which includes, for example, fluoromethyl, chloromethyl, bromomethyl, fluoroethyl, chloroethyl, bromoethyl, fluoro-n-propyl, chloro-n-propyl, difluoromethyl, chlorodifluoromethyl, trifluoromethyl, dichloromethyl, trichloromethyl, difluoroethyl, trifluoroethyl, trichloroethyl, chlorodifluoromethyl, bromodifluoromethyl, trifluorochloroethyl, hexafluoro-n-propyl, chlorobutyl, fluorobutyl, chloro-n-pentyl, fluoro-n-pentyl, chloro-n-hexyl and fluoro-n-hexyl groups.

The C₃-C₆ cycloalkyl group optionally substituted by a C₁-C₃ alkyl group for G, R, T¹, T⁴, T⁵ and T⁶ includes, for example, cyclopropyl, 1-methylcyclopropyl, 2,2,3,3-tetramethylcyclopropyl, cyclobutyl, 1-ethylcyclobutyl, 1-n-butylcyclobutyl, cyclopentyl, 1-methylcyclopentyl, cyclohexyl, 1-methylcyclohexyl and 4-methylcyclohexyl groups.

The C₁-C₄ alkyl group substituted by a phenyl group optionally substituted by a halogen atom or a C₁-C₄ alkyl group for B, G, R and T¹ includes, for example, benzyl, 2-chlorobenzyl, 3-bromobenzyl, 4-chlorobenzyl, 4-methylbenzyl, 4-tert-butylbenzyl, 1-phenylethyl, 1-(3-chlorophenyl)ethyl, 2-phenylethyl, 1-methyl-1-phenylethyl, 1-(4-chlorophenyl)-1-methylethyl, 1-(3-chlorophenyl)-1-methylethyl, 1-phenylpropyl, 2-phenylpropyl, 3-phenylpropyl, 1-phenylpropyl, 2-phenylbutyl, 3-phenylbutyl, 4-phenylbutyl, 1-methyl-1-phenylpropyl, 1-methyl-2-phenylpropyl, 1-methyl-3-phenylpropyl, 2-methyl-2-phenylpropyl, 2-(4-chlorophenyl)-2-methyl-propyl and 2-methyl-2-(3-methylphenyl)propyl groups.

For T¹, the C₃-C₆ cycloalkyl group substituted by a phenyl group optionally substituted by a halogen atom or a C₁-C₄ alkyl group includes, for example, 1-phenylcyclopropyl, 1-(3-chlorophenyl)cyclopropyl, 1-(4-chlorophenyl)cyclopropyl, 1-(4-bromophenyl)cyclopropyl, 1-(4-fluorophenyl)cyclopropyl, 1-(4-ethylphenyl)cyclopropyl, 1-(4-propylphenyl)cyclopropyl, 2-phenylcyclopropyl, 1-phenylcyclobutyl, 2-phenylcyclobutyl, 1-phenylcyclopentyl, 1-(4-chlorophenyl)cyclopentyl, 2-phenylcyclopentyl, 3-phenylcyclopentyl, 1-phenylcyclohexyl, 1-(3-fluorophenyl)cyclohexyl, 1-(4-chlorophenyl)cyclohexyl, 1-(4-tert-butylphenyl)cyclohexyl, 2-phenylcyclohexyl, 3-phenylcyclohexyl and 4-phenylcyclohexyl groups.

For T¹, the cyclopropyl group substituted by both a phenyl group optionally substituted by a halogen atom or a C₁-C₄ alkyl group and a C₁-C₄ alkyl group includes, for example, 2,2-dimethyl-1-phenylcyclopropyl, 1-(4-chlorophenyl)-2,2-dimethylcyclopropyl, 2,2-dimethyl-3-phenylcyclopropyl, 3-(3-chlorophenyl)-2,2-dimethylcyclopropyl, (4-chlorophenyl)-2,2-dimethyl-3-phenylcyclopropyl, (4-bromophenyl)-2,2-dimethyl-3-phenylcyclopropyl; 2,2-dimethyl-3-(4-methylphenyl)cyclopropyl and (4-tert-butylphenyl)-2,2-dimethyl-3-phenylcyclopropyl groups.

For T¹, the C₃-C₄ cycloalkyl group substituted by both a phenyl group optionally substituted by a halogen atom or a C₁-C₄ alkoxy group and a halogen atom includes, for example, 2,2-dichloro-1-phenylcyclopropyl, 2,2-dichloro-1-(3-chlorophenyl)cyclopropyl, 2,2-dichloro-1-(4-methoxyphenyl)cyclopropyl, 2,2-dichloro-1-(4-ethoxyphenyl)cyclopropyl, 2,2-dichloro-(4-i-propyloxyphenyl)cyclopropyl, 2,2-dichloro-1-(4-t-butylphenyl)cyclopropyl, 2,2-dichloro-1-(4-methoxyphenyl)-3-phenylcyclopropyl and 1-(4-ethoxyphenyl)-2,2,3,3-tetrafluorobutyl groups.

For T¹, the cyclopropyl group substituted by both a C₂-C₄ alkenyl group optionally substituted by a halogen atom, and a C₁-C₄ alkyl group includes, for example, 2,2-dimethyl-3-(2,2-dimethylethenyl)cyclopropyl, 3-(2,2-dibromoethenyl)-2,2-dimethylcyclopropyl, 3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropyl and 3-(2,2-chlorotrifluoroethenyl)-2,2-dimethylcyclopropyl groups.

For T¹, the C₃-C₆ cycloalkoxy group optionally substituted by a C₁-C₃ alkyl group includes, for example, cyclopropoxy, cyclobutoxy, cyclopentoxy, cyclohexyloxy and 1-methylcyclopropoxy groups.

For T¹, the C₂-C₄ alkenyl group substituted by a phenyl group optionally substituted by a halogen atom or a C₁-C₄ alkyl group includes, for example, 1-phenylethenyl, 2-phenylethenyl, 2-(2-chlorophenyl)ethenyl, 2-(3-chlorophenyl)ethenyl, 2-(4-chlorophenyl)ethenyl, 2-(4-methylphenyl)ethenyl, 2-(2,6-difluorophenyl)ethenyl, 2-(2,5-dimethylphenyl)ethenyl, 1-methyl-2-phenylethenyl, 2-phenyl-1-propenyl, 2-(4-bromophenyl)-1-propenyl and 2-(2,4,6-trimethylphenyl)-1-propenyl groups.

The alkoxy group for G, R, T¹, T², T³, R¹, W, X, Y, Y¹, Y² and Z may be a straight chain or branched alkoxy group having indicated carbon atoms, which includes, for example, methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentyloxy, 1-methylbutyloxy, 2-methylbutyloxy, 3-methylbutyloxy, 1,1-dimethylpropoxy, 1,2-dimethylpropoxy, 2,2-dimethylpropoxy, 1-ethylpropyloxy, n-hexyloxy, 1-methylpentyloxy, 2-methylpentyloxy, 3-methylpentyloxy, 4-methylpentyloxy, 1,1-dimethylbutyloxy, 1,2-dimethylbutyloxy, 1,3-dimethylbutyloxy, 2,2-dimethylbutyloxy, 2,3-dimethylbutyloxy, 3,3-dimethylbutyloxy, 1-ethylbutyloxy, 2-ethylbutyloxy, 1,1,2-trimethylpropyloxy, 1,2,2-trimethylpropyloxy, 1-ethyl-1-methylpropyloxy, 1-ethyl-2-methylpropyloxy, n-heptyloxy, n-octyloxy, n-nonyloxy and n-decyloxy groups.

The C₃-C₆ halocycloalkyl group for G, R and T¹ includes, for example, fluorocyclopropyl, difluorocyclopropyl, chlorocyclopropyl, dichlorocyclopropyl, 1-methyl-2,2-dichlorocyclopropyl, chlorocyclobutyl, dichlorocyclobutyl, chlorocyclopentyl, dichlorocyclopentyl, chlorocyclohexyl, dichlorocyclohexyl and tetrafluorocyclobutyl groups.

The group —NU¹U² for G, R, R¹, T¹, W, X, Y, Y¹ and Z includes, for example, methylamino, ethylamino, n-propylamino, isopropylamino, n-butylamino, isobutylamino, sec-butylamino, tert-butylamino, n-pentylamino, 1-methylbutylamino, 2-methylbutylamino, 3-methylbutylamino, 1,1-dimethylpropylamino, 1,2-dimethylpropylamino, 2,2-dimethylpropylamino, 1-ethylpropylamino, n-hexylamino, 1-methylpentylamino, 2-methylpentylamino, 3-methylpentylamino, 4-methylpentylamino, 1,1-dimethylbutylamino, 1,2-dimethylbutylamino, 1,3-dimethylbutylamino, 2,2-dimethylbutylamino, 2,3-dimethylbutylamino, 3,3-dimethylbutylamino, 1-ethylbutylamino, 2-ethylbutylamino, 1,1,2-trimethylpropylamino, 1,2,2-trimethylpropylamino, 1-ethyl-1-methylpropylamino, 1-ethyl-2-methylpropylamino, dimethylamino, diethylamino, di-n-propylamino, diisopropylamino, di-n-butylamino, di-sec-butylamino, diisobutylamino, di-n-pentylamino, di-n-hexylamino, methylethylamino, methylpropylamino, methylisopropylamino, methylbutylamino, methyl-sec-butylamino, methyl-isobutylamino, methyl-tert-butylamino, methylpentylamino, methylhexylamino, ethylpropylamino, ethylisopropylamino, ethylbutylamino, ethyl-sec-butylamino, ethyl-isobutylamino, ethylpentylamino, ethylhexylamino, phenylamino, benzylamino, N-methylacetamido, N-ethylacetamido, N-phenylacetamido and N-acetylacetamido groups, to which is applied the indicated scope of the carbon atoms constituting it.

The C₂-C₅ alkoxycarbonyl group for E, G, R, R¹, T¹, W, X, Y, Y¹, Y² and Z includes, for example, methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, iso-propoxycarbonyl, n-butoxycarbonyl, sec-butoxycarbonyl, iso-butoxycarbonyl and tert-butoxycarbonyl groups.

The C₁-C₄ haloalkoxy group for G, R, T¹, W, X, Y and Z may be a straight chain or branched C₁-C₄ haloalkoxy group, including, for example, fluoromethoxy, difluoromethoxy, trifluoromethoxy, chlorodifluoromethoxy, bromodifluoromethoxy, dichlorofluoromethoxy, chloromethoxy, dichloromethoxy, trichloromethoxy, bromomethoxy, fluoroethoxy, chloroethoxy, bromoethoxy, difluoroethoxy, trifluoroethoxy, tetrafluoroethoxy, pentafluoroethoxy, trichloroethoxy, trifluorochloroethoxy, fluoropropoxy, chloropropoxy, bromopropoxy, fluorobutoxy, chlorobutoxy, fluoro-iso-propoxy and chloro-iso-propoxy groups.

The C₁-C₄ alkylsulfenyl group for E, G, R, T², T³, W, X, Y and Z includes, for example, methylthio, ethylthio, n-propylthio, iso-propylthio, n-butylthio, iso-butylthio, sec-butylthio and tert-butylthio groups.

The C₁-C₄ alkylsulfinyl group for E, G, R, X, W, Y and z includes, for example, methylsulfinyl, ethylsulfinyl, n-propylsulfinyl, iso-propylsulfinyl, n-butylsulfinyl, iso-butylsulfinyl, sec-butylsulfinyl and tert-butylsulfinyl groups.

The C₁-C₄ alkylsulfonyl group for B, E, G, R, W, X, Y and Z includes, for example, methylsulfonyl, ethylsulfonyl, n-propylsulfonyl, iso-propylsulfonyl, n-butylsulfonyl, iso-butylsulfonyl, sec-butylsulfonyl and tert-butylsulfonyl groups.

The C₂-C₄ alkoxyalkyl group for B, G, R, R¹, T¹, Y, Y¹ and Y² includes, for example, C₁-C₃ alkoxy-methyl, C₁-C₂ alkoxy-ethyl, methoxyethoxymethyl and methoxypropyl groups.

The C₂-C₄ alkylcarbonyl group for E, G, R, R¹, U¹, U², Y¹, Y² and W includes, for example, acetyl, propionyl, butanoyl and iso-butanoyl groups.

The C₂-C₆ haloalkylcarbonyl group for G and W includes, for example, chloroacetyl, trifluoroacetyl, 3,3,3-trifluoropropionyl and pentafluoropropionyl groups.

The C₂-C₅ haloalkylcarbonyloxy group for G, R and Y includes, for example, chloroacetyloxy, trifluoroacetyloxy, 3,3,3-trifluoropropionyloxy and pentafluoropropionyloxy groups.

The C₃-C₇ dialkylaminocarbonyloxy group for G and Y includes, for example, dimethylaminocarbonyloxy, diethylaminocarbonyloxy and di-i-propylaminocarbonyloxy groups.

The naphthyl group for R, Y, Z and T¹ includes, for example, 1-naphthyl and 2-naphthyl groups.

The pyridyl group optionally substituted by Z for G and T¹ includes, for example, 2-pyridyl, 3-pyridyl and 4-pyridyl groups all optionally substituted by Z. Preferred are 2-pyridyl and 3-pyridyl groups both optionally substituted by Z; and more preferred is a 2-pyridyl group optionally substituted by Z.

The pyridyloxy group optionally substituted by Z for G and T¹ includes, for example, 2-pyridyloxy, 3-pyridyloxy and 4-pyridyloxy groups all optionally substituted by Z.

The pyridyl group optionally substituted by X for R and R¹ includes, for example, 2-pyridyl, 3-pyridyl and 4-pyridyl groups all optionally substituted by X. Preferred are 2-pyridyl and 3-pyridyl groups both optionally substituted by X; and more preferred is a 2-pyridyl group optionally substituted by X.

The pyridyloxy group optionally substituted by X for R and R¹ includes, for example, 2-pyridyloxy, 3-pyridyloxy and 4-pyridyloxy groups all optionally substituted by X.

The thienyl group optionally substituted by X for R and R¹ includes, for example, 2-thienyl and 3-thienyl groups both optionally substituted by X.

The thienyl group optionally substituted by Z for G and Y¹ includes, for example, 2-thienyl and 3-thienyl groups both optionally substituted by Z.

The group —N═CT⁷T⁸ for G, R, R¹, Y and Y¹ indicates an alkylidenamino group, a benzylidenamino group, an arylidenamino group or a cycloalkylidenamino group, including, for example, methylidenamino, ethylidenamino, propylidenamino, isopropylidenamino, 4-methyl-2-pentylidenamino, cyclopentylidenamino and cyclohexylidenamino groups.

The C₂-C₄ alkylaminocarbonyl group for E includes, for example, methylaminocarbonyl, ethylaminocarbonyl and n-propylaminocarbonyl groups.

The C₃-C₉ dialkylaminocarbonyl group for E includes, for example, dimethylaminocarbonyl, diethylaminocarbonyl, di-n-propylaminocarbonyl, di-isopropylaminocarbonyl and di-n-butylaminocarbonyl groups.

The C₁-C₄ alkylaminosulfonyl group for B includes, for example, methylaminosulfonyl, ethylaminosulfonyl, n-ptopylaminosulfonyl, isopropylaminosulfonyl and n-butylaminosulfonyl groups.

The C₂-C₈ dialkylaminosulfonyl group for B includes, for example, dimethylaminosulfonyl, diethylaminosulfonyl, di-n-propylaminosulfonyl, di-isopropylaminosulfonyl and di-n-butylaminosulfonyl groups.

The C₂-C₆ alkylaminothiocarbonyl group for B includes, for example, methylaminothiocarbonyl, ethylaminothiocarbonyl, n-propylaminothiocarbonyl, isopropylaminothiocarbonyl and n-butylaminothiocarbonyl groups.

The C₃-C₉ dialkylaminothiocarbonyl group for B includes, for example, dimethylaminothiocarbonyl, diethylaminothiocarbonyl, di-n-propylaminothiocarbonyl, di-isopropylaminothiocarbonyl and di-n-butylaminothiocarbonyl groups.

The C₁-C₄ alkyl group substituted by a benzoyl group optionally substituted by a halogen atom or a C₁-C₄ alkyl group for B includes, for example, phenacyl, 2-fluorophenacyl, 3-chlorophenacyl, 4-bromophenacyl, 2-methylphenacyl, 3-ethylphenacyl, 4-i-propylphenacyl and 4-t-butylphenacyl groups.

The phenylsulfonyl group optionally substituted by a halogen atom or a C₁-C₄ alkyl group for B includes, for example, 2-fluorophenylsulfonyl, 4-fluorophenylsulfonyl, 2-chlorophenylsulfonyl, 4-chlorophenylsulfonyl, 4-bromophenylsulfonyl, 2,5-dichlorophenylsulfonyl, pentafluorophenylsulfonyl, 4-methylphenylsulfonyl, 2-methylphenylsulfonyl, 4-t-butylphenylsulfonyl, 2,5-dimethylphenylsulfonyl, 2,4-dimethylphenylsulfonyl, 2,4,6-trimethylphenylsulfonyl and 2,4,6-tri-i-propylphenylsulfonyl groups.

The C₂-C₆ cyanoalkyl group for G and B includes, for example, cyanomethyl, 2-cyanoethyl, 3-cyanopropyl and 1-cyano-1-methylethyl groups.

The C₃-C₉ alkoxycarbonylalkyl group for B may be a straight chain or branched one, including, for example, methoxycarbonylmethyl, ethoxycarbonylmethyl, n-propoxycarbonylmethyl, i-propoxycarbonylmethyl, n-butoxycarbonylmethyl, i-butoxycarbonylmethyl, t-butoxycarbonylmethyl, n-hexyloxycarbonylmethyl, n-heptyloxycarbonylmethyl, 1-methoxycarbonylethyl, 1-ethoxycarbonylethyl, 1-n-butoxyethyl, 2-methoxycarbonylethyl, 2-ethoxycarbonylethyl, 1-methoxycarbonylpropyl, 3-ethoxycarbonylpropyl, 4-methoxycarbonylbutyl, 6-ethoxycarbonylhexyl, 1-methoxycarbonyl-1-methylethyl, 1-iso-propoxycarbonyl-1-methylethyl and 1-ethoxycarbonyl-2-methylpropyl groups.

The alkali metal for B includes, for example, lithium sodium and potassium.

The alkaline earth metal for B includes, for example, magnesium, calcium, strontium and barium. Preferred are magnesium, calcium and barium.

The ammonium group of NHT⁴T⁵T⁶ for B includes, for example, ammonium, monomethylammonium, dimethylammonium, trimethylammonium, diethylammonium, triethylammonium, di-isopropylammonium, di-isopropylethylammonium, hexylmethylammonium, cyclopropylmethylammonium, cyclohexylmethylammonium, allylmethylammonium, benzylmethylammonium and 4-methylcyclohexylethylammonium groups. Any two of T⁴, T⁵ and T⁶ may form, along with the nitrogen atom to which they are bonded, a heterocyclic, 5-, 6-, 7- or 8-membered ammonium group optionally having oxygen, nitrogen and/or sulfur atoms.

The methoxy group substituted by a phenyl group optionally substituted by a halogen atom or a C₁-C₄ alkyl group for G includes, for example, benzyloxy, 2-chlorobenzyloxy, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 3-methylbenzyloxy, 4-t-butylbenzyloxy, 2,6-difluorobenzyloxy and 2-fluoro-4-chlorobenzyloxy groups.

The heterocyclic, 5-, 6-, 7- or 8-membered ammonium group optionally having oxygen, nitrogen and/or sulfur atoms, which is formed by two of T⁴, T⁵ and T⁶ along with the nitrogen atom to which they are bonded, includes, for example, pyrrolidine, pyrazolidine, imidazolidine, oxazolidine, isoxazolidine, thiazolidine, piperidine, piperazine, morpholine, thiamorpholine, hexamethylenimine and heptamethylenimine groups. The haloalkylsulfenyl group for G, R, W, X, Y and Z may be a straight chain or branched C₁-C₄ haloalkylthio group, including, for example, fluoromethylthio, chlorodifluoromethylthio, bromodifluoromethylthio, trifluoromethylthio, trichloromethylthio, 2,2,2-trifluoroethylthio, 1,1,2,2-tetrafluoroethylthio, fluoroethylthio, pentafluoroethylthio and fluoro-iso-propylthio groups.

The haloalkylsulfinyl group for G, R, W, X, Y and Z may be a straight chain or branched, C₁-C₄ haloalkylsulfinyl group, including, for example, fluoromethylsulfinyl, chlorodifluoromethylsulfinyl, bromodifluoromethylsulfinyl, trifluoromethylsulfinyl, trichloromethylsulfinyl, 2,2,2-trifluoroethylsulfinyl, 1,1,2,2-tetrafluoroethylsulfinyl, fluoroethylsulfinyl, pentafluoroethylsulfinyl and fluoro-iso-propylsulfinyl groups.

The haloalkylsulfonyl group for G, R, W, X, Y and Z may be a straight chain or branched, C₁-C₄ haloalkylsulfonyl group, including, for example, fluoromethylsulfonyl, chlorodifluoromethylsulfonyl, bromodifluoromethylsulfonyl, trifluoromethylsulfonyl, trichloromethylsulfonyl, 2,2,2-trifluoroethylsulfopyl, 1,1,2,2-tetrafluoroethylsulfonyl, fluoroethylsulfonyl, pentafluoroethylsulfonyl and fluoro-isopropylsulfonyl groups.

The haloalkenyl group for G, R, T¹ and W may be a straight chain or branched C₂-C₄ haloalkenyl group, including, for example, 2-chloroethenyl, 2-bromoethenyl and 2,2-dichloroethenyl groups.

The alkenyloxy group for G, R, R¹, T¹, W, Y and Y¹ may be a straight chain or branched C₂-C₄ alkenyloxy group, including, for example, allyloxy, 2-propenyloxy, 2-butenyloxy and 2-methyl-2-propenyloxy groups.

The haloalkenyloxy group for G, R, W and Y may be a straight chain or branched C₂-C₄ haloalkenyloxy group, including, for example, 3-chloro-2-propenyloxy, 3,3-dichloro-2-propenyloxy, 4-chloro-2-butenyloxy, 4,4-dichloro-3-butenyloxy and 4,4-difluoro-3-butenyloxy groups.

The alkenylsulfenyl group for G, R, W, X, Y and Z may be a straight chain or branched C₂-C₄ alkenylsulfenyl group, including, for example, allylsulfenyl, 2-propenylsulfenyl, 2-butenylsulfenyl and 2-methyl-2-propenylsulfenyl groups.

The alkenylsulfinyl group for G, R, W, X, Y and Z may be a straight chain or branched C₂-C₄ alkenylsulfinyl group, including, for example, allylsulfinyl, 2-propenylsulfinyl, 2-butenylsulfinyl and 2-methyl-2-propenylsulfinyl groups.

The alkenylsulfonyl group for G, R, W, X, Y and Z may be a straight chain or branched C₂-C₄ alkenylsulfonyl group, including, for example, allylsulfonyl, 2-propenylsulfonyl, 2-butenylsulfonyl and 2-methyl-2-propenylsulfonyl groups.

The haloalkenylsulfenyl group for G, R, W and Y may be a straight chain or branched C₂-C₄ haloalkenylsulfenyl group, including, for example, 3-chloro-2-propenylsulfenyl, 4-chloro-2-butenylsulfenyl, 3,3-dichloro-2-propenylsulfenyl, 4,4-dichloro-3-butenylsulfenyl and 4,4-difluoro-3-butenylsulfenyl groups.

The haloalkenylsulfinyl group for G, R, W and Y may be a straight chain or branched C₂-C₄ haloalkenylsulfinyl group, including, for example, 3-chloro-2-propenylsulfinyl, 3,3-dichloro-2-propenylsulfinyl, 4-chloro-2-butenylsulfinyl, 4,4-dichloro-3-butenylsulfinyl and 4,4-difluoro-3-butenylsulfinyl groups.

The haloalkenylsulfonyl group for G, R, W and Y may be a straight chain or branched C₂-C₄ haloalkenylsulfonyl group, including, for example, 3-chloro-2-propenylsulfonyl, 3,3-dichloro-2-propenylsulfonyl, 4-chloro-2-butenylsulfonyl, 4,4-dichloro-3-butenylsulfonyl and 4,4-difluoro-3-butenylsulfonyl groups.

The C₂-C₄ haloalkynyl group for G, R and W includes, for example, chloroethynyl, bromoethynyl, iodoethynyl, 3-chloro-1-propynyl and 3-bromo-1-butynyl groups.

The C₂-C₄ alkynyloxy group for G, R, W and Y includes, for example, 2-propynyloxy, 2-butynyloxy and 1-methyl-2-propynyloxy groups.

The C₂-C₄ haloalkynyloxy group for G, R, W and Y includes, for example, 3-chloro-2-propynyloxy, 3-bromo-2-propynyloxy and 3-iodo-2-propynyloxy groups.

The C₂-C₆ alkynylsulfenyl group for G, R, W and Y includes, for example, 2-propynylsulfenyl, 2-butynylsulfenyl and 1-methyl-2-propynylsulfenyl groups.

The C₂-C₆ alkynylsulfinyl group for G, R, W and Y includes, for example, 2-propynylsulfinyl, 2-butynylsulfinyl and 1-methyl-2-propynylsulfinyl groups.

The C₂-C₆ alkynylsulfonyl group for G, R, W and Y includes, for example, 2-propynylsulfonyl, 2-butynylsulfonyl and 1-methyl-2-propynylsulfonyl groups.

The C₂-C₆ haloalkynylsulfenyl group for G, R, W and Y includes, for example, 3-chloro-2-propynylsulfenyl, 3-bromo-2-propynylsulfenyl and 3-iodo-2-propynylsulfenyl groups.

The C₂-C₆ haloalkynylsulfinyl group for G, R, W and Y includes, for example, 3-chloro-2-propynylsulfinyl, 3-bromo-2-propynylsulfinyl and 3-iodo-2-propynylsulfinyl groups.

The C₂-C₆ haloalkynylsulfonyl group for G, R, W and Y includes, for example, 3-chloro-2-propynylsulfonyl, 3-bromo-2-propynylsulfonyl and 3-iodo-2-propynylsulfonyl groups.

The C₂-C₄ alkylcarbonyloxy group for G, R, W and Y includes, for example, acetoxy, propanoyloxy, butanoyloxy and isopropylcarbonyloxy groups.

The benzoyl group optionally substituted by X for E and G includes, for example, benzoyl, 2-chlorobenzoyl, 3-chlorobenzoyl, 4-chlorobenzoyl, 4-bromobenzoyl, 4-fluorobenzoyl, 3-methylbenzoyl, 4-methylbenzoyl, 4-tert-butylbenzoyl and 3,4-dichlorobenzoyl groups.

Even at low concentration, the compounds of the present invention effectively prevent various pests, which include, for example, so-called agricultural insect pests that injure agricultural and horticultural crops and trees, so-called livestock insect pests that live on livestock and poultry, so-called sanitary insect pests that have various negative influences on the human living environment including houses, so-called stored products insect pests that injure grains stored in storehouses, and also acarids, nematodes, molluscs and crustaceans that live in the same sites as above and injure those mentioned above.

Examples of insect pests, acarids, nematodes, molluscs and crustaceans capable of being exterminated by the compounds of the present invention are mentioned below, which, however, are not limitative.

Insect pests of Lepidoptera, such as rice stem borer (Chilo suppressalis Walker), rice leafroller (Cnaphalocrocis medinalis Guenée), green rice caterpillar (Naranga aenescens Moore), rice skipper (Parnara guttata Bremer et Gvey), diamond back moths (Plutella xylostella Linné), cabbage armyworms (Mamestra brassicae Linné), common white (Pieris rapae crucivora Boisduval), turnip moth (Agrotis segetum Denis et Schiffermüller), common cutworm (Spodptera litura Fabricius), beet armyworm (Spodoptera exigua Hübner), smaller tea tortrix (Adoxophyes sp.), oriental tea tortrix (Homona magnanima Diakonoff), peach fruit moth (Carposina niponensis Walsingham), oriental fruit moth (Grapholita molesta Busck), summer fruit tortrix (Adoxophyes orana fasciata Walsingham), apple leafminers (Phyllonorycter ringoniella Matsumura), corn earworm (Helicoverpa zea Boddie), tobacco bad worms (Heliothis virescens Fabricius), European corn borer (Ostrinia nubilalis Hübner), fall armyworm (Spodoptera frugiperda J. E. Smith), Codling moth moth (Cydia pomonella Linné), fall webworms (Hyphantria cunea Drury), etc.;

Insect pests of Hemiptera, such as green rice leafhopper (Nephotettix cincticeps Uhler), brown rice planthoppers (Nilaparvata lugens Stal), green peach aphid (Myzus persicae Sulzer), cotton aphid (Aphis gossypii Glover), greenhouse whitefly (Trialeurodes vaporariorum Westwood), sweetpotato white fly (Bemisia tabaci Gennadius), pear psylla (Psylla pyricola Forster), azalea lace bug (Stephanitis pyrioides Scott), arrowhead scale (Unaspis yanonensis Kuwana), comstock mealybug (Pseudococcus comstocki Kuwana), red wax scale (Ceroplastes rubens Maskell), brown-marmorated stinkbug (Halyomorpha mista Uhler), cabbage bug (Eurydema rugosam Motschulsky), bed bug (Cimex lectularius Linné), etc.;

Insect pests of Coleoptera, such as twenty-eight-spotted ladybird (Henosepilachna vigintioctopunctata Fabricius), cupreous chafers (Anomala cuprea Hope), ricewater weevil (Lissorhoptrus oryzophilus Kuschel), sweetpotato weevil (Cylas formicarius Fabricius), cucurbit leaf beetle (Aulacophora femoralis Motschulsky), striped flea beetle (Phyllotreta striolata Fablicius), white-spotted longicorn beetle (Anoplophora malasiaca Thomson), pine sawyers (Monochamus alternatus Hope), corn rootworms (Diabrotica spp.), rice weevil (Sitophilus zeamais Motschulsky), lesser rice weevil (Sitophilus oryzae Linné), granary weevils (Sitophilus granarius Linné), red four beetle (Tribolium castaneum Herbst), etc.;

Insect pests of Diptera, such as legume leafminer (Liriomyza trifolii Burgess), seedcorn maggot (Delia platura Meigen), Hessia fly (Mayetiola destructor Say), melon fly (Dacus (Zengodacus) cucurbitae Coquillett), Mediterranear fruit fly (Ceratitis capitata Wiedemann), house flies (Musca domestica Linné), stable fly (Stomoxys calcitrans Linné), Sheep ked (Melophagus orinus), common cattle grub (Hypoderm lineatum devillers), nothern cattle grub (Hypoderma boris Linné), sheep botfly (Oestrus ovis Linné), tsetse fly (Golossina palpalis Robineau-Desvoidy), common gnat (Culex pipiens pallens Coquillett), yellow-fever mosquitoes (Aedes negypti Linné), Anopheles culicifacies), etc.

Insect pests of Hymenoptera, such as cabbage sawfly (Athalis rosae ruficornis Jakovlev), pine sawfly (Neodiprion sertifer Geoffroy), chestnut sawfly (Apethymus kuri Takeuchi), etc.;

Insect pests of Thysanoptera, such as melon thrips (Thrips palmi Karny), onion thrips (Thrips tabaci Lindeman), western flower thrips (Frankliniella occidentalis Pergande), flower thrip (Frankliniella intonsa Trybom), yellow tea thrip (Scirtothrips dorsalis Hood), etc.;

Insect pests of Dictyoptera, such as smokybrown cockroache (Periplaneta fuliginosa Serville), Japanese cockroach (Periplaneta japonica Karny), German cockroaches (Blattella germanica Linné), etc.;

Insect pests of Orthoptera, such as oriental migratory locust (Locusta migratoria Linné), rice grasshopper (Oxya yezoensis Shiraki), desert locust (Schistocerca gregaria Forskal), etc.;

Insect pests of Isoptera, such as Formosan subterranean termit (Coptotermes formosanus Shiraki), (Reticulitermes (Leucotermes) speratus Kolbe), (Odontotermes formosanus Shirakif), etc.;

Insect pests of Siphonaptera, such as cat fleas (Ctenocephalides felis Bouché), human fleas (Pulex irritans Linné), oriental rat flea (Xenopsylla cheopis Rothschild), etc.;

Insect pests of Mallophaga, such as Chicken bodylouse (Menacanthus stramineus Nitsch), cattle biting louse (Bovicola bovis Linné), etc.;

Insect pests of Anoplura, such as short-nosed cattle louse (Haematopinus eurysternus Nitzsh), hog louse (Haematopinus suis Linné), longnosed cattle louse (Linognathus vituli Linné), little cattle louse (Solenopotes capillatus Enderlein), etc.

Pests of TETRANYCHIDAE, such as citrus red mite (Panonychus citri McGregor), European red mite (Panonychus ulmi Kock), two-spotted spider mite (Tetranychus urticae Koch), Kanzawa spinder mite (Tetranychus kanzawai Kishida), etc.;

Pests of ERIOPHYDAE, such as pink citrus rust mite (Aculops pelekassi Keifor), pear rust mite (Epitrimerus pyri Nalepa), dry bulb mite (Aceria tulipae Keiter), pink tea mite (Acaphylla theae watt), etc.;

Pests of TARSONEMIDAE, such as broad mites (Polyphagotarsonemus latus Banks), cyclamen mite, strawberry mite (Steneotarsonemus pallidus Banks), etc.;

Pests of ACARIDAE, such as mold mite, copra mite, forage mite (Tyrophagus putrescetiae Schrank), bulb mite (Rhizoglyphus robini Claparede), etc.;

Pests of VARROIDAE, such as bee brood mite (Varroa jacobsoni Oudemans), etc.;

Pests of Ixodidae, such as bull ticks (Boophilus microplus Canestrini), (Haemaphysalis longicornis Neumann), etc.;

Pests of Sarcoptidae, such as sarcoptes mange mite (Sarcaptes scabiei Linné), etc.;

Nematodes, such as southern root-knot nematode (Meloidogyne incognita Kofoid et White), northern root-knot nematode (Meloidogyne hapla Chitwood), Cobb root-lesion nematode (Pratylenchus penetraus Cobb), walnut root-lesion nematode (Pratylenchus vulnus Allen et Jensen), potato cyst nematode (Globodera rostochiensis Wollenweber), pine wood nematode (Bursaphelenchus xylophilus Steiner et Buhrer), etc.;

Mollusca, such as apple snail (Pomacea canaliculata Lamarck), (Incilaria pilineata Benson), (Acusta despecta sieboldiana Pfeiffer), (Euhadra peliomphala Pfeiffer), pillbug (Armadillidium vulgare Latreille), etc.;

Crustaceans, such as pillbug (Armadillidium vulgare Latreille), etc.

The plant diseases to be controlled by the compounds of the present invention are as follows:

Blast (Pyricularia oryzae), Helminthosporium leaf spot (Cochliobolus miyabeanus) and Sheath blight (Rhizoctonia solani) of rice, Powdery mildew (Erysiphe graminis f. sp. hordei, f. sp. tritici), Leaf stripe (Pyrenophora graminea), Net blotch (Pyrenophora teres), Fusarium blight (Gibberella zeae), yellow rust, black stem rust and brown rust (Puccinia striiformis, P. graminis, P. recondita and P. hordei), Snow blight and snow mold (Typhula sp., Micronectriella nivais), Loose smut (Ustilago tritici, U. nuda), Eyespot (Pseudocercorsporella herpotrichoides), Scald and leaft blotch (Rhynchosporium secalis), Speckled blotch (Septoria tritici), and Glume blotch (Leptosphaeria nodorum) of barley and wheat,

Melanose (Diaporthe citri), Scab (Elsinoe fawcetti), and Common green mold and blue mold (Penicillium digitatum, P. italicum) of citrus fruit,

Blossom blight (Sclerotinia mali), Canker (Valsa mali), Powder mildew (Podosphaera leucotricha), Alternaria leaft spot (Alternaria mali) and Scab (Venturia inaequalis) of apple,

Scab (Venturia nashicola), Black spot (Alternaria Kikuchiana) and Rust (Gymnosporangium haraeanum) of pear,

Brown rot (Sclerotinia cinerea), Scab (Cladosporium carpophilum), and Phomopsis rot (Phomopsis sp.) of peach,

Downy mildew (Plasmopara viticola), Anthracnose (Elsinoe ampelina), Ripe rot (Glomerella cingulata), Powdery mildew (Uncinula necator) and Rust (Phakopsora ampelopsidis) of grape,

Anthracnose (Gloesporium kaki), Powdery mildew (Phyllactinia kakicola), Angular leaf spot (Cercospora kaki), and Circular leaf spot (Mycosphaerella nawae) of persimmon,

Downy mildew (Pseudoperenospora cubensis), Anthracnose (Colletotrichum lagenarium), Powdery mildew (Sphaerotheca fuliginea), and Gummy stem blight (Mycosphaerella melonis) of cucurbit,

Late blight (Phytophthora infestans), Early blight (Alternaria solani) and Leaf mold (Cladosporium fulvam) of tomato.

Brown spot (Phomopsis vexans) and Powdery mildew (Erysiphe cichoracoarum) of egg plant,

Alternaria leaft spot (Alternaria japonica) and white spot (Cerocosporella brassicae) of vegetable of the family crucifers.

Rust (Puccinia allii) of welsh onion.

Purple seed stain (Cercospora kikuchii), Sphaceloma scab (Elsinoe glycines) and Pot and stem blight (Diaporthe phaseololum) of soybean,

Anthracnose (Collectorichum lindemuthianum) of kidney bean.

Leaf spot (Mycosphaerella personatum) and Brown leaf spot (Cercospora arachidicola) of peanut,

Powdery mildew (Erysiphe pisi) of garden pea,

Early blight (Alternaria solani) of potato,

Powdery mildew (Sphaerotheca humuli) of strawberry,

Net blister blight (Exobasidium reticulatum) and White scab (Elsinoe leucospila) of tea,

Brown spot (Alternaria longipes), Powdery mildew (Erysiphe cichoracearum) and Anthracnose (Colletotrichum tabacum) of tobacco,

Cercospora leaft spot (Cercospora beticola) of sugar beat,

Black spot (Diplocarpon rosae) and Powdery mildew (Sphaerotheca pannosa) of rose,

Leaf spot (Septoria chrysanthemiindici) and Rust (Puccinia horiana) of chrysanthemum,

Gray mold (Botrytis cinerea) of various kinds of crops, and,

Sclerotinia rot (Sclerotinia sclerotiorum) of various kinds of crops.

In addition, the compounds of the present invention are effective in presenting the attachment of aquatic organisms, even at extremely low concentrations. Aquatic organisms to which the invention is directed are, for example, shellfishes and algae, such as mussel, barnacle, oyster, hydrozoan, hydra, Serpula, ascidian, seamoss, Bagula, mud pond snail, sea lettuce, green layer, Ectocarpus, etc.

Specifically, the compounds of the present invention can effectively exterminate various pests and phytopathogenic microbes of, for example, Orthoptera, Hemiptera, Lepidoptera, Coleoptera, Hymenoptera, Diptera, Temitidae, and also mites and louses, even when used at low concentrations. In addition, the compounds of the invention are effective in preventing the attachment of various aquatic organisms living in sea water and fresh water to aquatic constructions, etc. On the other hand, the compounds of the present invention contains useful compounds that have few negative influences on mammals, fishes, shellfishes and useful insects.

Of the compounds of the invention, those having CN as E can be produced according to the following methods (Scheme 1).

In (Scheme 1), Q, A and B have the same meanings as defined above; L represents a suitable leaving group, such as a chlorine atom, a bromine atom, an iodine atom, an alkoxy group having from 1 to 4 carbon atoms, a phenoxy group, an alkylsulfonyloxy group having from 1 to 4 carbon atoms, a benzenesulfonyloxy group, a toluenesulfonyloxy group, a phenoxy group, a 1-pyrazolyl group or a 1-imidazolyl group; L′ represents a halogen atom; and alkyl represents an alkyl group preferably having from 1 to 4 carbon atoms.

Method A in (Scheme 1) is to react an acetonitrile derivative of formula (3) with an acid chloride, ester or amide of formula (4) or with an acid anhydride of formula (5) to give compounds (1′) of the present invention. The compound (1′) of the invention is optionally reacted with an alkyl halide, an alkyl sulfonate, a trimethylsilyl halide, a sulfonyl chloride, a sulfamoyl chloride, a thiocarbamoyl chloride, an acid chloride or an ester of formula (8) to be converted into compounds (1) of the invention. Depending on the type of B in the compounds (1) of the invention, the compound (1′) is reacted with a dihydropyran, an isocyanate or a thioisocyanate to give the compounds (1). In Method A, if the compound of formula (4) or (5) is used in an excessive amount, the compounds (1) can be directly obtained without isolating the compounds (1′).

Where Q is bonded to the acrylonitrile moiety via a nitrogen atom, compounds (1′) may be produced according to Method B. Method B is to react a heterocyclic compound of formula (6) with a halogenocyanoketone derivative of formula (7) to give compounds (1′) of the invention.

Where A is bonded to the acrylonitrile moiety via a nitrogen atom, compounds (1′) may be produced according to Method C. Method C is to react a cyanoacetic acid derivative of formula (9) with a heterocyclic compound of formula (10) to give compounds (1′) of the invention. As the case may be, the compound of formula (9) will be prepared by reacting an acetonitrile derivative of formula (3), such as that used in Method A, with a carbonic acid ester in the presence of a base.

Of the compounds of the invention, those where E is

In (Scheme 2), Q, A, E, B, L, L′ and alkyl have the same meanings as above.

Method D in (Scheme 2) is to react a compound of formula (11) with an acid chloride, ester or amide of formula (4) or with an acid anhydride of formula (5) to give the compounds (1′) of the present invention. The compound (1′) of the invention is optionally reacted with an alkyl halide, an alkyl sulfonate, a trimethylsilyl halide, a sulfonyl chloride, a sulfamoyl chloride, a thiocarbamoyl chloride, an acid chloride or an ester of formula (8) to be converted into the compounds (1) of the invention. Depending on the type of B in the compounds (1) of the invention, the compound (1′) is reacted with a dihydropyran, an isocyanate or a thioisocyanate to give the compounds (1). In Method A, if the compound of formula (4) or (5) is used in an excessive amount, the compounds (1) can be directly obtained without isolating the compounds (1′).

Where Q is bonded to the ethylene moiety via a nitrogen atom, the compounds (1′) may be produced according to Method E. Method E is to react a heterocyclic compound of formula (6) with a compound of formula (12) in the presence of a base to give compounds (1′) of the invention.

Where A is bonded to the ethylene moiety via a nitrogen atom, the compounds (1′) may be produced according to Method F. Method F is to react a compound of formula (13) with a heterocyclic compound of formula (10) through dealcoholation to give the compounds (1′) of the invention. As the case may be, the compound of formula (13) will be prepared by reacting a compound of formula (11), such as that used in Method D, with a carbonic acid ester in the presence of a base.

If desired, the compounds (1′) where E is an alkoxycarbonyl group may be hydrolyzed, decarboxylated and halogenated to give the compounds of the invention where E is a halogen atom. As the case may be, the compounds of the invention where E is a halogen atom may be reacted with a nucleophilic reagent corresponding to E (e.g., triester phosphites, alkyl mercaptans, thiophenols, metal acetylides, metal cyanides, metal azides, nitrites) to give different compounds of the invention. Also as the case may be, the compounds to be obtained through decarboxylation of the compounds (1′) where E is an alkoxycarbonyl group may be reacted with an electrophilic reagent under basic conditions to give the compounds of the invention.

As the case may be, the processes of (Scheme 1) and (Scheme 2) are preferably effected in the presence of a base. The base to be used includes, for example, alkali metal alkoxides such as sodium ethoxide, sodium methoxide and t-butoxy potassium; alkali metal hydroxides such as sodium hydroxide and potassium hydroxide; alkali metal carbonates such as sodium carbonate and potassium carbonate; organic bases such as triethylamine, pyridine and DBU; organic lithium compounds such as butyl lithium; lithium amides such as lithium diisopropylamide and lithium bistrimethylsilylamide; and sodium hydride.

The reactions of (Scheme 1) and (Scheme 2) may be effected in a solvent that is inert to the reaction. The solvent includes, for example, lower alcohols such as methanol and ethanol; aromatic hydrocarbons such as benzene and toluene; etherd such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane and 1,2-diethoxyethane; halogenated hydrocarbons such as methylene chloride, chloroform and 1,2-dichloroethane; amides such as dimethylformamide and dimethylacetamide; acetonitrile; dimethylsulfoxide; and mixed solvents of these. As the case may be, also employable are mixed solvent comprising said solvents and water. Also as the case may be, a quaternary ammonium salt such as tetra-n-butylammonium bromide may be added to the reaction system as a catalyst to obtain good results. The reaction temperature may be freely settled within a range between −30° C. and 200° C. Preferably, the reaction temperature falls between 0° C. and 15° C., or between 0° C. and the boiling point of the solvent if used. The base may be used in an amount of from 0.05 to 10 equivalents, preferably from 0.05 to 3 equivalents, of the reaction substrate.

The compounds of the present invention may be separated from reaction mixtures according to any ordinary methods. If the purification of the compounds of the invention is needed, they can be separated and purified by any ordinary methods of, for example, recrystallization or column chromatography.

Of the compounds of the invention, those having an asymmetric carbon atom include optically-active compounds of (+) form and (−) form.

Methods of producing the compounds (3) to be used in (Scheme 1) are referred to hereinunder. The compounds (3) can be produced according to the following (Scheme 3).

1) A benzyl halide, a benzyl alkylsulfonate, a benzyl arylsulfonate, a halomethyl-heterocyclic compound, an alkylsulfonyloxymethyl-heterocyclic compound or an arylsulfonyloxymethyl-heterocyclic compound of formula (14) is reacted with a suitable cyanating reagent to give compounds (3). Alternatively, a phenylacetic acid derivative or a heterocyclic acetic acid derivative is converted into the corresponding amide derivative, which is then dehydrated to give compounds (3).

2) A heterocyclic halide (15) is condensed with a cyanoacetate (16) in the presence of a base to give a compound (17), which is then hydrolyzed and decarboxylated to give compounds (3).

3) To obtain compounds (3) where Q is bonded to the ethylene moiety via a nitrogen atom, a heterocyclic derivative (6) where the nitrogen atom of Q is unsubstituted is reacted with a haloacetonitrile derivative in the presence of a base. Alternatively, the compound (6) is reacted with a compound (18) in the presence of a base to give a compound (17), said compound (18) being obtained through halogenation of a cyanoacetate, and thereafter the compound (17) is hydrolyzed and decarboxylated to obtain the compounds (3).

The compounds (11) to be used in (Scheme 2) can be produced in the same manner as in the production of the compounds (3) mentioned above.

The compounds (7) to be used in (Scheme 1) can be produced by condensing a benzoic acid halide or heterocyclic carboxylic acid halide with a cyanoacetate in the presence of a base followed by halogenating the resulting condensate.

The above-mentioned halomethyl-heterocyclic compounds, alkylsulfonyloxymethyl-heterocyclic compounds and arylsulfonyloxymethyl-heterocyclic compounds can be derived from heterocyclic methane derivatives or heterocyclic carboxylate derivatives that are produced according to ordinary methods (see Alan R. Katritzky, and Charles W. Rees; Comprehensive Heterocyclic Chemistry, Vol. 2, Vol. 3, Vol. 4, Vol. 5 or Vol. 6). To produce the compounds (14) where Q is an oxazol-4-yl or thiazol-4-yl group, a carboxylic acid amide or thioamide can be reacted with 1,3-dichloro-2-propanone.

Examples of the compounds of the present invention are shown in Table 1 to Table 14 below. The abbreviations in these Tables are for the meanings mentioned below:

Me: methyl group, Et: ethyl group, Pr: propyl group, Bu: butyl group, Pen: pentyl group, Hex: hexyl group, Hep: heptyl group, Oct: octyl group, Non: nonyl group, Dec: decyl group, Ph: phenyl group, n: normal, i: iso, sec: secondary, t: tertiary, c: cyclo.

TABLE 1
or
R1	R2	R3	B	Y1	Y2	Y3
2,6-F2—Ph	H	H	H	H	H	H
2,6-F2—Ph	H	H	H	H	Cl	H
2,6-F2—Ph	H	H	H	H	Me	H
2,6-F2—Ph	H	H	H	H	OMe	H
2,6-F2—Ph	H	H	H	H	SMe	H
2,6-F2—Ph	H	H	H	H	OCF3	H
2,6-F2—Ph	H	H	H	H	CF3	H
2,6-F2—Ph	H	H	H	H	CO2Me	H
2,6-F2—Ph	H	H	H	H	H	Me
2,6-F2—Ph	H	H	H	Me	H	Me
2,6-F2—Ph	H	H	H	Me	H	CF3
2,6-F2—Ph	H	H	H	Me	H	H
2,6-F2—Ph	H	H	H	Me	Me	Me
2,6-F2—Ph	H	H	H	Me	Me	H
2,6-F2—Ph	H	H	H	Me	Cl	Me
2,6-F2—Ph	H	H	H	Me	Cl	H
2,6-F2—Ph	Cl	H	H	Me	Cl	Me
2,6-F2—Ph	H	H	H	Et	Me	Me
2,6-F2—Ph	H	H	H	Et	H	H
2,6-F2—Ph	H	H	H	nPr	Me	Me
2,6-F2—Ph	H	H	H	iPr	Me	Me
2,6-F2—Ph	H	H	H	iPr	Cl	Me
2,6-F2—Ph	H	H	H	nBu	Me	Me
2,6-F2—Ph	H	H	H	tBu	Me	Me
2,6-F2—Ph	H	H	H	Cl	Me	Me
2,6-F2—Ph	H	H	H	Cl	Me	H
2,6-F2—Ph	H	H	H	Cl	H	Me
2,6-F2—Ph	H	H	H	Cl	H	CF3
2,6-F2—Ph	H	H	H	Cl	H	H
2,6-F2—Ph	Me	H	H	Cl	H	H
2,6-F2—Ph	Cl	H	H	Cl	H	H
2,6-F2—Ph	NO2	H	H	Cl	H	H
2,6-F2—Ph	CO2Me	H	H	Cl	H	H
2,6-F2—Ph	CO2Et	H	H	Cl	H	H
2,6-F2—Ph	H	H	H	Cl	Cl	Me
2,6-F2—Ph	Me	H	H	Cl	Cl	Me
2,6-F2—Ph	H	Me	H	Cl	Cl	Me
2,6-F2—Ph	H	Cl	H	Cl	CI	Me
2,6-F2—Ph	Cl	H	H	Cl	Cl	Me
2,6-F2—Ph	Cl	Cl	H	Cl	Cl	Me
2,6-F2—Ph	Cl	Cl	B1	Cl	Cl	Me
2,6-F2—Ph	Ph	H	H	Cl	Cl	Me
2,6-F2—Ph	H	Ph	H	Cl	Cl	Me
2,6-F2—Ph	CF3	H	H	Cl	Cl	Me
2,6-F2—Ph	H	CF3	H	Cl	Cl	Me
2,6-F2—Ph	cPr	H	H	Cl	Cl	Me
2,6-F2—Ph	H	cPr	H	Cl	Cl	Me
2,6-F2—Ph	OMe	H	H	Cl	Cl	Me
2,6-F2—Ph	H	OMe	H	Cl	Cl	Me
2,6-F2—Ph	NH2	H	H	Cl	Cl	Me
2,6-F2—Ph	H	NH2	H	Cl	Cl	Me
2,6-F2—Ph	NHMe	H	H	Cl	Cl	Me
2,6-F2—Ph	H	NHMe	H	Cl	Cl	Me
2,6-F2—Ph	NMe2	H	H	Cl	Cl	Me
2,6-F2—Ph	H	NMe2	H	Cl	Cl	Me
2,6-F2—Ph	NO2	H	H	Cl	Cl	Me
2,6-F2—Ph	H	NO2	H	Cl	Cl	Me
2,6-F2—Ph	CN	H	H	Cl	Cl	Me
2,6-F2—Ph	H	CN	H	Cl	Cl	Me
2,6-F2—Ph	OH	H	H	Cl	Cl	Me
2,6-F2—Ph	H	OH	H	Cl	Cl	Me
2,6-F2—Ph	CO2Me	H	H	Cl	Cl	Me
2,6-F2—Ph	H	CO2Me	H	Cl	Cl	Me
2,6-F2—Ph	CO2Et	H	H	Cl	Cl	Me
2,6-F2—Ph	H	H	H	Cl	Cl	H
2,6-F2—Ph	H	H	H	Cl	Cl	CF3
2,6-F2—Ph	H	H	H	Cl	Cl	CF2H
2,6-F2—Ph	H	H	H	Cl	Cl	CH2OMe
2,6-F2—Ph	H	H	H	Cl	Cl	COMe
2,6-F2—Ph	H	H	H	Cl	Cl	Ph
2,6-F2—Ph	H	H	H	Cl	Cl	CH2Ph
2,6-F2—Ph	H	H	H	Cl	CF3	Me
2,6-F2—Ph	H	H	H	Br	Me	Me
2,6-F2—Ph	H	H	H	Me	Br	Me
2,6-F2—Ph	H	H	H	Me	Br	H
2,6-F2—Ph	H	H	H	Br	H	H
2,6-F2—Ph	H	H	H	OMe	Me	Me
2,6-F2—Ph	H	H	H	Me	OMe	Me
2,6-F2—Ph	H	H	H	OMe	H	H
2,6-F2—Ph	H	H	H	H	OMe	H
2,6-F2—Ph	H	H	H	Cl	OMe	Me
2,6-F2—Ph	H	H	H	OCF3	Me	Me
2,6-F2—Ph	H	H	H	OCF3	Cl	Me
2,6-F2—Ph	H	H	H	OCF3	H	H
2,6-F2—Ph	H	H	H	Me	OCF3	Me
2,6-F2—Ph	H	H	H	Cl	OCF3	Me
2,6-F2—Ph	H	H	H	SMe	Cl	Me
2,6-F2—Ph	H	H	H	Me	SMe	Me
2,6-F2—Ph	H	H	H	Cl	SMe	Me
2,6-F2—Ph	H	H	H	SMe	H	H
2,6-F2—Ph	H	H	H	SOMe	Cl	Me
2,6-F2—Ph	H	H	H	Cl	SOMe	Me
2,6-F2—Ph	H	H	H	SOMe	H	H
2,6-F2—Ph	H	H	H	SO2Me	Cl	Me
2,6-F2—Ph	H	H	H	Cl	SO2Me	Me
2,6-F2—Ph	H	H	H	SO2Me	H	H
2,6-F2—Ph	H	H	H	CF3	Me	Me
2,6-F2—Ph	H	H	H	CF3	Cl	H
2,6-F2—Ph	H	H	H	CF3	Cl	Me
2,6-F2—Ph	Me	H	H	CF3	Cl	Me
2,6-F2—Ph	Cl	H	H	CF3	Cl	Me
2,6-F2—Ph	Br	H	H	CF3	Cl	Me
2,6-F2—Ph	CF3	H	H	CF3	Cl	Me
2,6-F2—Ph	NO2	H	H	CF3	Cl	Me
2,6-F2—Ph	CN	H	H	CF3	Cl	Me
2,6-F2—Ph	CO2Me	H	H	CF3	Cl	Me
2,6-F2—Ph	CO2Et	H	H	CF3	Cl	Me
2,6-F2—Ph	H	H	H	CF3	Cl	CF3
2,6-F2—Ph	H	H	H	CF3	Cl	CF2H
2,6-F2—Ph	H	H	H	CF3	Cl	CH2OMe
2,6-F2—Ph	H	H	H	CF3	Cl	COCH3
2,6-F2—Ph	H	H	H	CF3	H	Me
2,6-F2—Ph	H	H	H	CF3	H	H
2,6-F2—Ph	H	H	H	CF3	Br	Me
2,6-F2—Ph	H	H	H	CF3	SMe	Me
2,6-F2—Ph	H	H	H	CF3	SOMe	Me
2,6-F2—Ph	H	H	H	CF3	SO2Me	Me
2,6-F2—Ph	H	H	H	CF3	CF3	Me
2,6-F2—Ph	H	H	H	CF3	NO2	Me
2,6-F2—Ph	H	H	H	CF3	CN	Me
2,6-F2—Ph	H	H	H	CF3	NHMe	Me
2,6-F2—Ph	H	H	H	CF3	NMe2	Me
2,6-F2—Ph	H	H	H	CF3	Ph	Me
2,6-F2—Ph	H	H	H	CF3	CH2Ph	Me
2,6-F2—Ph	H	H	H	CF3	OPh	Me
2,6-F2—Ph	H	H	H	CF3	OH	Me
2,6-F2—Ph	H	H	H	CF3	CO2Me	Me
2,6-F2—Ph	H	H	H	CF3	OMe	Me
2,6-F2—Ph	H	H	H	CF3	OCF3	Me
2,6-F2—Ph	H	H	H	CF3	OCF2H	Me
2,6-F2—Ph	H	H	H	CF3	OCF2H	CF2H
2,6-F2—Ph	H	H	H	NO2	CF3	Me
2,6-F2—Ph	H	H	H	NO2	Cl	Me
2,6-F2—Ph	H	H	H	NO2	Me	Me
2,6-F2—Ph	H	H	H	NO2	H	H
2,6-F2—Ph	H	H	H	Cl	NO2	Me
2,6-F2—Ph	H	H	H	CN	CF3	Me
2,6-F2—Ph	H	H	H	CN	Cl	Me
2,6-F2—Ph	H	H	H	CN	Me	Me
2,6-F2—Ph	H	H	H	CN	H	H
2,6-F2—Ph	H	H	H	Cl	CN	Me
2,6-F2—Ph	H	H	H	Br	CN	Me
2,6-F2—Ph	H	H	H	NHMe	Me	Me
2,6-F2—Ph	H	H	H	NHMe	Cl	Me
2,6-F2—Ph	H	H	H	NHMe	H	H
2,6-F2—Ph	H	H	H	Cl	NHMe	Me
2,6-F2—Ph	H	H	H	NMe2	Me	Me
2,6-F2—Ph	H	H	H	NMe2	Cl	Me
2,6-F2—Ph	H	H	H	NMe2	H	H
2,6-F2—Ph	H	H	H	Cl	NMe2	Me
2,6-F2—Ph	H	H	H	Ph	Cl	Me
2,6-F2—Ph	H	H	H	Ph	H	H
2,6-F2—Ph	H	H	H	Cl	Ph	Me
2,6-F2—Ph	H	H	H	CH2Ph	Me	Me
2,6-F2—Ph	H	H	H	CH2Ph	H	H
2,6-F2—Ph	H	H	H	Cl	CH2Ph	Me
2,6-F2—Ph	H	H	H	OPh	Cl	Me
2,6-F2—Ph	H	H	H	OPh	H	H
2,6-F2—Ph	H	H	H	Cl	OPh	Me
2,6-F2—Ph	H	H	H	OH	Me	Me
2,6-F2—Ph	H	H	H	OH	H	H
2,6-F2—Ph	H	H	H	Cl	OH	Me
2,6-F2—Ph	H	H	H	CO2Me	Me	Me
2,6-F2—Ph	H	H	H	CO2Me	Cl	Me
2,6-F2—Ph	H	H	H	CO2Me	H	H
2,6-F2—Ph	H	H	H	cPr	Me	Me
2,6-F2—Ph	H	H	H	cPr	Cl	Me
2,6-F2—Ph	H	H	B1	Cl	Cl	Me
2,6-F2—Ph	Cl	H	B1	Cl	Cl	Me
2,6-F2—Ph	H	H	B2	Cl	Cl	Me
2,6-F2—Ph	H	H	B3	Cl	Cl	Me
2,6-F2—Ph	H	H	B4	Cl	Cl	Me
2,6-F2—Ph	Cl	H	B4	Cl	Cl	Me
2,6-F2—Ph	Cl	Me	B4	Cl	Cl	Me
2,6-F2—Ph	NO2	H	B4	Cl	Cl	Me
2,6-F2—Ph	CO2Me	H	B4	Cl	Cl	Me
2,6-F2—Ph	CO2Et	H	B4	Cl	Cl	Me
2,6-F2—Ph	H	H	B5	Cl	Cl	Me
2,6-F2—Ph	Cl	H	B5	Cl	Cl	Me
2,6-F2—Ph	H	H	B6	Cl	Cl	Me
2,6-F2—Ph	Cl	H	B6	Cl	Cl	Me
2,6-F2—Ph	NO2	H	B6	Cl	Cl	Me
2,6-F2—Ph	CO2Me	H	B6	Cl	Cl	Me
2,6-F2—Ph	CO2Et	H	B6	Cl	Cl	Me
2,6-F2—Ph	H	H	B7	Cl	Cl	Me
2,6-F2—Ph	Cl	H	B7	Cl	Cl	Me
2,6-F2—Ph	NO2	H	B7	Cl	Cl	Me
2 6-F2—Ph	CO2Me	H	B7	Cl	Cl	Me
2,6-F2—Ph	CO2Et	H	B7	Cl	Cl	Me
2,6-F2—Ph	H	H	B8	Cl	Cl	Me
2,6-F2—Ph	H	H	B9	Cl	Cl	Me
2,6-F2—Ph	H	H	B10	Cl	Cl	Me
2,6-F2—Ph	H	H	B11	Cl	Cl	Me
2,6-F2—Ph	H	H	B12	Cl	Cl	Me
2,6-F2—Ph	H	H	B13	Cl	Cl	Me
2,6-F2—Ph	H	H	B14	Cl	Cl	Me
2,6-F2—Ph	H	H	B15	Cl	Cl	Me
2,6-F2—Ph	H	H	B16	Cl	Cl	Me
2,6-F2—Ph	H	H	B17	Cl	Cl	Me
2,6-F2—Ph	H	H	B18	Cl	Cl	Me
2,6-F2—Ph	H	H	B19	Cl	Cl	Me
2,6-F2—Ph	H	H	B20	CI	Cl	Me
2,6-F2—Ph	H	H	B21	Cl	Cl	Me
2,6-F2—Ph	H	H	B22	Cl	Cl	Me
2,6-F2—Ph	H	H	B23	Cl	Cl	Me
2,6-F2—Ph	H	H	B24	Cl	Cl	Me
2,6-F2—Ph	H	H	B25	Cl	Cl	Me
2,6-F2—Ph	H	H	B26	Cl	Cl	Me
2,6-F2—Ph	H	H	B27	Cl	Cl	Me
2,6-F2—Ph	H	H	B28	Cl	Cl	Me
2,6-F2—Ph	H	H	B29	Cl	Cl	Me
2,6-F2—Ph	H	H	B30	Cl	Cl	Me
2,6-F2—Ph	H	H	B31	Cl	Cl	Me
2,6-F2—Ph	H	H	B32	Cl	Cl	Me
2,6-F2—Ph	H	H	B33	Cl	Cl	Me
2,6-F2—Ph	H	H	B34	Cl	Cl	Me
2,6-F2—Ph	H	H	Na	Cl	Cl	Me
2,6-F2—Ph	H	H	K	Cl	Cl	Me
2,6-F2—Ph	H	H	B1	CF3	Cl	Me
2,6-F2—Ph	H	H	B2	CF3	Cl	Me
2,6-F2—Ph	H	H	B3	CF3	Cl	Me
2,6-F2—Ph	H	H	B4	CF3	Cl	Me
2,6-F2—Ph	Me	H	B4	CF3	Cl	Me
2,6-F2—Ph	Cl	H	B4	CF3	Cl	Me
2,6-F2—Ph	NO2	H	B4	CF3	Cl	Me
2,6-F2—Ph	CO2Me	H	B4	CF3	Cl	Me
2,6-F2—Ph	CO2Et	H	B4	CF3	Cl	Me
2,6-F2—Ph	H	H	B5	CF3	Cl	Me
2,6-F2—Ph	Cl	H	B5	CF3	Cl	Me
2,6-F2—Ph	H	H	B6	CF3	Cl	Me
2,6-F2—Ph	Me	H	B6	CF3	Cl	Me
2,6-F2—Ph	Cl	H	B6	CF3	Cl	Me
2,6-F2—Ph	NO2	H	B6	CF3	Cl	Me
2,6-F2—Ph	CO2Me	H	B6	CF3	Cl	Me
2,6-F2—Ph	CO2Et	H	B6	CF3	Cl	Me
2,6-F2—Ph	H	H	B7	CF3	Cl	Me
2,6-F2—Ph	Me	H	B7	CF3	Cl	Me
2,6-F2—Ph	Cl	H	B7	CF3	Cl	Me
2,6-F2—Ph	NO2	H	B7	CF3	Cl	Me
2,6-F2—Ph	CO2Me	H	B7	CF3	Cl	Me
2,6-F2—Ph	CO2Et	H	B7	CF3	Cl	Me
2,6-F2—Ph	H	H	B8	CF3	Cl	Me
2,6-F2—Ph	H	H	B9	CF3	Cl	Me
2,6-F2—Ph	H	H	B10	CF3	Cl	Me
2,6-F2—Ph	H	H	B11	CF3	Cl	Me
2,6-F2—Ph	H	H	B12	CF3	Cl	Me
2,6-F2—Ph	H	H	B13	CF3	Cl	Me
2,6-F2—Ph	H	H	B14	CF3	Cl	Me
2,6-F2—Ph	H	H	B15	CF3	Cl	Me
2,6-F2—Ph	H	H	B16	CF3	Cl	Me
2,6-F2—Ph	H	H	B17	CF3	Cl	Me
2,6-F2—Ph	H	H	B18	CF3	Cl	Me
2,6-F2—Ph	H	H	B19	CF3	Cl	Me
2,6-F2—Ph	H	H	B20	CF3	Cl	Me
2,6-F2—Ph	H	H	B21	CF3	Cl	Me
2,6-F2—Ph	H	H	B22	CF3	Cl	Me
2,6-F2—Ph	H	H	B23	CF3	Cl	Me
2,6-F2—Ph	H	H	B24	CF3	Cl	Me
2,6-F2—Ph	H	H	B25	CF3	Cl	Me
2,6-F2—Ph	H	H	B26	CF3	Cl	Me
2,6-F2—Ph	H	H	B27	CF3	Cl	Me
2,6-F2—Ph	H	H	B28	CF3	Cl	Me
2,6-F2—Ph	H	H	B29	CF3	Cl	Me
2,6-F2—Ph	H	H	B30	CF3	Cl	Me
2,6-F2—Ph	H	H	B31	CF3	Cl	Me
2,6-F2—Ph	H	H	B32	CF3	Cl	Me
2,6-F2—Ph	H	H	B33	CF3	Cl	Me
2,6-F2—Ph	H	H	B34	CF3	Cl	Me
2,6-F2—Ph	H	H	Na	CF3	Cl	Me
2,6-F2—Ph	H	H	K	CF3	Cl	Me
2,6-F2—Ph	H	H	B1	Cl	H	H
2,6-F2—Ph	H	H	B2	Cl	H	H
2,6-F2—Ph	H	H	B3	Cl	H	H
2,6-F2—Ph	H	H	B4	Cl	H	H
2,6-F2—Ph	Me	H	B4	Cl	H	H
2,6-F2—Ph	Cl	H	B4	Cl	H	H
2,6-F2—Ph	NO2	H	B4	Cl	H	H
2,6-F2—Ph	CO2Me	H	B4	Cl	H	H
2,6-F2—Ph	CO2Et	H	B4	Cl	H	H
2,6-F2—Ph	H	H	B5	Cl	H	H
2,6-F2—Ph	H	H	B6	Cl	H	H
2,6-F2—Ph	NO2	H	B6	Cl	H	H
2,6-F2—Ph	H	H	B7	Cl	H	H
2,6-F2—Ph	Me	H	B7	Cl	H	H
2,6-F2—Ph	Cl	H	B7	Cl	H	H
2,6-F2—Ph	NO2	H	B7	Cl	H	H
2,6-F2—Ph	CO2Me	H	B7	Cl	H	H
2,6-F2—Ph	CO2Et	H	B7	Cl	H	H
2,6-F2—Ph	H	H	B8	Cl	H	H
2,6-F2—Ph	H	H	B9	Cl	H	H
2,6-F2—Ph	H	H	B10	Cl	H	H
2,6-F2—Ph	H	H	B11	Cl	H	H
2,6-F2—Ph	H	H	B12	Cl	H	H
2,6-F2—Ph	H	H	B13	Cl	H	H
2,6-F2—Ph	H	H	B14	Cl	H	H
2,6-F2—Ph	H	H	B15	Cl	H	H
2,6-F2—Ph	H	H	B16	Cl	H	H
2,6-F2—Ph	H	H	B17	Cl	H	H
2,6-F2—Ph	H	H	B18	Cl	H	H
2,6-F2—Ph	H	H	B19	Cl	H	H
2,6-F2—Ph	H	H	B20	Cl	H	H
2,6-F2—Ph	H	H	B21	Cl	H	H
2,6-F2—Ph	H	H	B22	Cl	H	H
2,6-F2—Ph	H	H	B23	Cl	H	H
2,6-F2—Ph	H	H	B24	Cl	H	H
2,6-F2—Ph	H	H	B25	Cl	H	H
2,6-F2—Ph	H	H	B26	Cl	H	H
2,6-F2—Ph	H	H	B27	Cl	H	H
2,6-F2—Ph	H	H	B28	Cl	H	H
2,6-F2—Ph	H	H	B29	Cl	H	H
2,6-F2—Ph	H	H	B30	Cl	H	H
2,6-F2—Ph	H	H	B31	Cl	H	H
2,6-F2—Ph	H	H	B32	Cl	H	H
2,6-F2—Ph	H	H	B33	Cl	H	H
2,6-F2—Ph	H	H	B34	Cl	H	H
2,6-F2—Ph	H	H	Na	Cl	H	H
2,6-F2—Ph	H	H	K	Cl	H	H
tBu	H	H	H	H	H	Me
tBu	H	H	H	Me	H	Me
tBu	H	H	H	Me	H	CF3
tBu	H	H	B7	Me	H	H
tBu	H	H	H	Me	Me	Me
tBu	H	H	H	Me	Cl	Me
tBu	Cl	H	H	Me	Cl	Me
tBu	H	H	H	Et	Me	Me
tBu	H	H	B8	Et	H	H
tBu	H	H	H	Cl	Me	Me
tBu	H	H	H	Cl	Me	H
tBu	H	H	H	Cl	H	Me
tBu	H	H	H	Cl	H	CF3
tBu	H	H	H	Cl	H	H
tBu	Me	H	B7	Cl	H	H
tBu	Cl	H	B7	Cl	H	H
tBu	NO2	H	B7	Cl	H	H
tBu	CO2Me	H	B7	Cl	H	H
tBu	CO2Et	H	B7	Cl	H	H
tBu	H	H	H	Cl	Cl	Me
tBu	Me	H	H	Cl	Cl	Me
tBu	Cl	H	H	Cl	Cl	Me
tBu	CF3	H	H	Cl	Cl	Me
tBu	cPr	H	H	Cl	Cl	Me
tBu	OMe	H	H	Cl	Cl	Me
tBu	NO2	H	H	Cl	Cl	Me
tBu	CN	H	H	Cl	Cl	Me
tBu	CO2Me	H	H	Cl	Cl	Me
tBu	CO2Et	H	H	Cl	Cl	Me
tBu	H	H	H	Cl	Cl	H
tBu	H	H	H	Cl	Cl	CF3
tBu	H	H	H	Cl	Cl	CF2H
tBu	H	H	H	Cl	Cl	CH2OMe
tBu	H	H	H	Cl	Cl	COMe
tBu	H	H	H	Cl	CF3	Me
tBu	H	H	H	Br	Me	Me
tBu	H	H	H	Me	Br	Me
tBu	H	H	H	Me	Br	H
tBu	H	H	B34	Br	H	H
tBu	H	H	H	OMe	Me	Me
tBu	H	H	H	Me	OMe	Me
tBu	H	H	H	OMe	H	H
tBu	H	H	H	Cl	OMe	Me
tBu	H	H	H	OCF3	Me	Me
tBu	H	H	H	OCF3	Cl	Me
tBu	H	H	H	OCF3	H	H
tBu	H	H	H	Me	OCF3	Me
tBu	H	H	H	Cl	OCF3	Me
tBu	H	H	H	SMe	Cl	Me
tBu	H	H	H	Me	SMe	Me
tBu	H	H	H	Cl	SMe	Me
tBu	H	H	B7	SMe	H	H
tBu	H	H	H	CF3	Me	Me
tBu	H	H	H	CF3	Cl	H
tBu	H	H	H	CF3	Cl	Me
tBu	Me	H	H	CF3	Cl	Me
tBu	Cl	H	H	CF3	Cl	Me
tBu	Br	H	H	CF3	Cl	Me
tBu	CF3	H	H	CF3	Cl	Me
tBu	NO2	H	H	CF3	Cl	Me
tBu	CN	H	H	CF3	Cl	Me
tBu	CO2Me	H	H	CF3	Cl	Me
tBu	CO2Et	H	H	CF3	Cl	Me
tBu	H	H	H	CF3	Cl	CF3
tBu	H	H	H	CF3	Cl	CF2H
tBu	H	H	H	CF3	Cl	CH2OMe
tBu	H	H	H	CF3	Cl	COCH3
tBu	H	H	H	CF3	H	Me
tBu	H	H	H	CF3	H	H
tBu	H	H	H	CF3	Br	Me
tBu	H	H	H	CF3	SMe	Me
tBu	H	H	H	CF3	SOMe	Me
tBu	H	H	H	CF3	SO2Me	Me
tBu	H	H	H	CF3	CF3	Me
tBu	H	H	H	CF3	NO2	Me
tBu	H	H	H	CF3	CN	Me
tBu	H	H	H	CF3	NHMe	Me
tBu	H	H	H	CF3	NMe2	Me
tBu	H	H	H	CF3	OH	Me
tBu	H	H	H	CF3	CO2Me	Me
tBu	H	H	H	CF3	OMe	Me
tBu	H	H	H	CF3	OCF3	Me
tBu	H	H	H	CF3	OCF2H	Me
tBu	H	H	H	CF3	OCF2H	CF2H
tBu	H	H	H	NO2	Cl	Me
tBu	H	H	H	NO2	Me	Me
tBu	H	H	H	NO2	H	H
tBu	H	H	H	Cl	NO2	Me
tBu	H	H	H	CN	Cl	Me
tBu	H	H	H	CN	Me	Me
tBu	H	H	H	CN	H	H
tBu	H	H	H	Cl	CN	Me
tBu	H	H	H	NMe2	H	H
tBu	H	H	H	Cl	NMe2	Me
tBu	H	H	H	OH	Me	Me
tBu	H	H	H	OH	H	H
tBu	H	H	H	Cl	OH	Me
tBu	H	H	H	CO2Me	Me	Me
tBu	H	H	H	CO2Me	Cl	Me
tBu	H	H	H	CO2Me	H	H
tBu	H	H	B1	Cl	Cl	Me
tBu	Cl	H	B1	Cl	Cl	Me
tBu	H	H	B2	Cl	Cl	Me
tBu	H	H	B3	Cl	Cl	Me
tBu	H	H	B4	Cl	Cl	Me
tBu	Me	H	B4	Cl	Cl	Me
tBu	Cl	H	B4	Cl	Cl	Me
tBu	NO2	H	B4	Cl	Cl	Me
tBu	CO2Me	H	B4	Cl	Cl	Me
tBu	CO2Et	H	B4	Cl	Cl	Me
tBu	H	H	B5	Cl	Cl	Me
tBu	H	H	B6	Cl	Cl	Me
tBu	Cl	H	B6	Cl	Cl	Me
tBu	H	H	B7	Cl	Cl	Me
tBu	Me	H	B7	Cl	Cl	Me
tBu	Cl	H	B7	Cl	Cl	Me
tBu	NO2	H	B7	Cl	Cl	Me
tBu	CO2Me	H	B7	Cl	Cl	Me
tBu	CO2Et	H	B7	Cl	Cl	Me
tBu	H	H	B8	Cl	Cl	Me
tBu	H	H	B9	Cl	Cl	Me
tBu	H	H	B10	Cl	Cl	Me
tBu	H	H	B11	Cl	Cl	Me
tBu	H	H	B12	Cl	Cl	Me
tBu	H	H	B13	Cl	Cl	Me
tBu	H	H	B14	Cl	Cl	Me
tBu	H	H	B15	Cl	Cl	Me
tBu	H	H	B16	Cl	Cl	Me
tBu	H	H	B17	Cl	Cl	Me
tBu	H	H	B18	Cl	Cl	Me
tBu	H	H	B19	Cl	Cl	Me
tBu	H	H	B20	Cl	Cl	Me
tBu	H	H	B21	Cl	Cl	Me
tBu	H	H	B22	Cl	Cl	Me
tBu	H	H	B23	Cl	Cl	Me
tBu	H	H	B24	Cl	Cl	Me
tBu	H	H	B25	Cl	Cl	Me
tBu	H	H	B26	Cl	Cl	Me
tBu	H	H	B27	Cl	Cl	Me
tBu	H	H	B28	Cl	Cl	Me
tBu	H	H	B29	Cl	Cl	Me
tBu	H	H	B30	Cl	Cl	Me
tBu	H	H	B31	Cl	Cl	Me
tBu	H	H	B32	Cl	Cl	Me
tBu	H	H	B33	Cl	Cl	Me
tBu	H	H	B34	Cl	Cl	Me
tBu	H	H	Na	Cl	Cl	Me
tBu	H	H	K	Cl	Cl	Me
tBu	H	H	B1	CF3	Cl	Me
tBu	H	H	B2	CF3	Cl	Me
tBu	H	H	B3	CF3	Cl	Me
tBu	H	H	B4	CF3	Cl	Me
tBu	Me	H	B4	CF3	Cl	Me
tBu	Cl	H	B4	CF3	Cl	Me
tBu	NO2	H	B4	CF3	Cl	Me
tBu	CO2Me	H	B4	CF3	Cl	Me
tBu	CO2Et	H	B4	CF3	Cl	Me
tBu	H	H	B5	CF3	Cl	Me
tBu	H	H	B6	CF3	Cl	Me
tBu	Cl	H	B6	CF3	Cl	Me
tBu	H	H	B7	CF3	Cl	Me
tBu	Me	H	B7	CF3	Cl	Me
tBu	Cl	H	B7	CF3	Cl	Me
tBu	NO2	H	B7	CF3	Cl	Me
tBu	CO2Me	H	B7	CF3	Cl	Me
tBu	CO2Et	H	B7	CF3	Cl	Me
tBu	H	H	B8	CF3	Cl	Me
tBu	H	H	B9	CF3	Cl	Me
tBu	H	H	B10	CF3	Cl	Me
tBu	H	H	B11	CF3	Cl	Me
tBu	H	H	B12	CF3	Cl	Me
tBu	H	H	B13	CF3	Cl	Me
tBu	H	H	B14	CF3	Cl	Me
tBu	H	H	B15	CF3	Cl	Me
tBu	H	H	B16	CF3	Cl	Me
tBu	H	H	B17	CF3	Cl	Me
tBu	H	H	B18	CF3	Cl	Me
tBu	H	H	B19	CF3	Cl	Me
tBu	H	H	B20	CF3	Cl	Me
tBu	H	H	B21	CF3	Cl	Me
tBu	H	H	B22	CF3	Cl	Me
tBu	H	H	B23	CF3	Cl	Me
tBu	H	H	B24	CF3	Cl	Me
tBu	H	H	B25	CF3	Cl	Me
tBu	H	H	B26	CF3	Cl	Me
tBu	H	H	B27	CF3	Cl	Me
tBu	H	H	B28	CF3	Cl	Me
tBu	H	H	B29	CF3	Cl	Me
tBu	H	H	B30	CF3	Cl	Me
tBu	H	H	B31	CF3	Cl	Me
tBu	H	H	B32	CF3	Cl	Me
tBu	H	H	B33	CF3	Cl	Me
tBu	H	H	B34	CF3	Cl	Me
tBu	H	H	Na	CF3	Cl	Me
tBu	H	H	K	CF3	Cl	Me
tBu	H	H	B1	Cl	H	H
tBu	H	H	B2	Cl	H	H
tBu	H	H	B3	Cl	H	H
tBu	H	H	B4	Cl	H	H
tBu	H	H	B5	Cl	H	H
tBu	H	H	B6	Cl	H	H
tBu	H	H	B7	Cl	H	H
tBu	H	H	B8	Cl	H	H
tBu	H	H	B9	Cl	H	H
tBu	H	H	B10	Cl	H	H
tBu	H	H	B11	Cl	H	H
tBu	H	H	B12	Cl	H	H
tBu	H	H	B13	Cl	H	H
tBu	H	H	B14	Cl	H	H
tBu	H	H	B15	Cl	H	H
tBu	H	H	B16	Cl	H	H
tBu	H	H	B17	Cl	H	H
tBu	H	H	B18	Cl	H	H
tBu	H	H	B19	Cl	H	H
tBu	H	H	B20	Cl	H	H
tBu	H	H	B21	Cl	H	H
tBu	H	H	B22	Cl	H	H
tBu	H	H	B23	Cl	H	H
tBu	H	H	B24	Cl	H	H
tBu	H	H	B25	Cl	H	H
tBu	H	H	B26	Cl	H	H
tBu	H	H	B27	Cl	H	H
tBu	H	H	B28	Cl	H	H
tBu	H	H	B29	Cl	H	H
tBu	H	H	B30	Cl	H	H
tBu	H	H	B31	Cl	H	H
tBu	H	H	B32	Cl	H	H
tBu	H	H	B33	Cl	H	H
tBu	H	H	B34	Cl	H	H
tBu	H	H	Na	Cl	H	H
tBu	H	H	K	Cl	H	H
2-pyridyl	H	H	H	H	H	Me
2-pyridyl	H	H	H	Me	H	Me
2-pyridyl	H	H	H	Me	H	CF3
2-pyridyl	H	H	B7	Me	H	H
2-pyridyl	H	H	H	Me	Me	Me
2-pyridyl	H	H	H	Me	Cl	Me
2-pyridyl	Cl	H	H	Me	Cl	Me
2-pyridyl	H	H	H	Et	Me	Me
2-pyridyl	H	H	H	Et	H	H
2-pyridyl	H	H	H	Cl	Me	Me
2-pyridyl	H	H	H	Cl	Me	H
2-pyridyl	H	H	H	Cl	H	Me
2-pyridyl	H	H	H	Cl	H	CF3
2-pyridyl	H	H	B7	Cl	H	H
2-pyridyl	Me	H	B7	Cl	H	H
2-pyridyl	Cl	H	B7	CI	H	H
2-pyridyl	CF3	H	B7	CI	H	H
2-pyridyl	cPr	H	B7	Cl	H	H
2-pyridyl	OMe	H	B7	Cl	H	H
2-pyridyl	NO2	H	B7	Cl	H	H
2-pyridyl	CN	H	B7	Cl	H	H
2-pyridyl	CO2Me	H	B7	Cl	H	H
2-pyridyl	CO2Et	H	B7	Cl	H	H
2-pyridyl	H	H	H	Cl	Cl	Me
2-pyridyl	Me	H	H	Cl	Cl	Me
2-pyridyl	Cl	H	H	Cl	Cl	Me
2-pyridyl	CF3	H	H	Cl	Cl	Me
2-pyridyl	cPr	H	H	Cl	Cl	Me
2-pyridyl	OMe	H	H	Cl	Cl	Me
2-pyridyl	NO2	H	H	Cl	Cl	Me
2-pyridyl	CN	H	H	Cl	Cl	Me
2-pyridyl	CO2Me	H	H	Cl	Cl	Me
2-pyridyl	CO2Et	H	H	Cl	Cl	Me
2-pyridyl	H	H	H	Cl	Cl	H
2-pyridyl	H	H	H	Cl	Cl	CF3
2-pyridyl	H	H	H	Cl	Cl	CF2H
2-pyridyl	H	H	H	Cl	Cl	CH2OMe
2-pyridyl	H	H	H	Cl	Cl	COMe
2-pyridyl	H	H	H	Cl	CF3	Me
2-pyridyl	H	H	H	Br	Me	Me
2-pyridyl	H	H	H	Me	Br	Me
2-pyridyl	H	H	H	Me	Br	H
2-pyridyl	H	H	H	Br	H	H
2-pyridyl	H	H	H	OMe	Me	Me
2-pyridyl	H	H	H	Me	OMe	Me
2-pyridyl	H	H	B7	OMe	H	H
2-pyridyl	H	H	H	Cl	OMe	Me
2-pyridyl	H	H	H	OCF3	Me	Me
2-pyridyl	H	H	H	OCF3	Cl	Me
2-pyridyl	H	H	B7	OCF3	H	H
2-pyridyl	H	H	H	Me	OCF3	Me
2-pyridyl	H	H	H	Cl	OCF3	Me
2-pyridyl	H	H	H	SMe	Cl	Me
2-pyridyl	H	H	H	Me	SMe	Me
2-pyridyl	H	H	H	Cl	SMe	Me
2-pyridyl	H	H	B7	SMe	H	H
2-pyridyl	H	H	H	CF3	Me	Me
2-pyridyl	H	H	H	CF3	Cl	H
2-pyridyl	H	H	H	CF3	Cl	Me
2-pyridyl	Me	H	H	CF3	Cl	Me
2-pyridyl	Cl	H	H	CF3	Cl	Me
2-pyridyl	Br	H	H	CF3	Cl	Me
2-pyridyl	CF3	H	H	CF3	Cl	Me
2-pyridyl	NO2	H	H	CF3	Cl	Me
2-pyridyl	CN	H	H	CF3	Cl	Me
2-pyridyl	CO2Me	H	H	CF3	Cl	Me
2-pyridyl	CO2Et	H	H	CF3	Cl	Me
2-pyridyl	H	H	H	CF3	Cl	CF3
2-pyridyl	H	H	H	CF3	Cl	CF2H
2-pyridyl	H	H	H	CF3	Cl	CH2OMe
2-pyridyl	H	H	H	CF3	Cl	COCH3
2-pyridyl	H	H	H	CF3	H	Me
2-pyridyl	H	H	H	CF3	H	H
2-pyridyl	H	H	H	CF3	Br	Me
2-pyridyl	H	H	H	CF3	SMe	Me
2-pyridyl	H	H	H	CF3	SOMe	Me
2-pyridyl	H	H	H	CF3	SO2Me	Me
2-pyridyl	H	H	H	CF3	CF3	Me
2-pyridyl	H	H	H	CF3	NO2	Me
2-pyridyl	H	H	H	CF3	CN	Me
2-pyridyl	H	H	H	CF3	NHMe	Me
2-pyridyl	H	H	H	CF3	NMe2	Me
2-pyridyl	H	H	H	CF3	OH	Me
2-pyridyl	H	H	H	CF3	CO2Me	Me
2-pyridyl	H	H	H	CF3	OMe	Me
2-pyridyl	H	H	H	CF3	OCF3	Me
2-pyridyl	H	H	H	CF3	OCF2H	Me
2-pyridyl	H	H	H	CF3	OCF2H	CF2H
2-pyridyl	H	H	H	NO2	Cl	Me
2-pyridyl	H	H	H	NO2	Me	Me
2-pyridyl	H	H	B7	NO2	H	H
2-pyridyl	H	H	H	Cl	NO2	Me
2-pyridyl	H	H	H	CN	Cl	Me
2-pyridyl	H	H	H	CN	Me	Me
2-pyridyl	H	H	H	CN	H	H
2-pyridyl	H	H	H	Cl	CN	Me
2-pyridyl	H	H	H	NMe2	H	H
2-pyridyl	H	H	H	Cl	NMe2	Me
2-pyridyl	H	H	H	OH	Me	Me
2-pyridyl	H	H	H	OH	H	H
2-pyridyl	H	H	H	Cl	OH	Me
2-pyridyl	H	H	H	CO2Me	Me	Me
2-pyridyl	H	H	H	CO2Me	Cl	Me
2-pyridyl	H	H	H	CO2Me	H	H
2-pyridyl	H	H	B1	Cl	Cl	Me
2-pyridyl	H	H	B2	Cl	Cl	Me
2-pyridyl	H	H	B3	Cl	Cl	Me
2-pyridyl	H	H	B4	Cl	Cl	Me
2-pyridyl	H	H	B5	Cl	Cl	Me
2-pyridyl	H	H	B6	Cl	Cl	Me
2-pyridyl	H	H	B7	Cl	Cl	Me
2-pyridyl	Cl	H	B7	Cl	Cl	Me
2-pyridyl	H	H	B8	Cl	Cl	Me
2-pyridyl	H	H	B9	Cl	Cl	Me
2-pyridyl	H	H	B10	Cl	Cl	Me
2-pyridyl	H	H	B11	Cl	Cl	Me
2-pyridyl	H	H	B12	Cl	Cl	Me
2-pyridyl	H	H	B13	Cl	Cl	Me
2-pyridyl	H	H	B14	Cl	Cl	Me
2-pyridyl	H	H	B15	Cl	Cl	Me
2-pyridyl	H	H	B16	Cl	Cl	Me
2-pyridyl	H	H	B17	Cl	Cl	Me
2-pyridyl	H	H	B18	Cl	Cl	Me
2-pyridyl	H	H	B19	Cl	Cl	Me
2-pyridyl	H	H	B20	Cl	Cl	Me
2-pyridyl	H	H	B21	Cl	Cl	Me
2-pyridyl	H	H	B22	Cl	Cl	Me
2-pyridyl	H	H	B23	Cl	Cl	Me
2-pyridyl	H	H	B24	Cl	Cl	Me
2-pyridyl	H	H	B25	Cl	Cl	Me
2-pyridyl	H	H	B26	Cl	Cl	Me
2-pyridyl	H	H	B27	Cl	Cl	Me
2-pyridyl	H	H	B28	Cl	Cl	Me
2-pyridyl	H	H	B29	Cl	Cl	Me
2-pyridyl	H	H	B30	Cl	Cl	Me
2-pyridyl	H	H	B31	Cl	Cl	Me
2-pyridyl	H	H	B32	Cl	Cl	Me
2-pyridyl	H	H	B33	Cl	Cl	Me
2-pyridyl	H	H	B34	Cl	Cl	Me
2-pyridyl	H	H	Na	Cl	Cl	Me
2-pyridyl	H	H	K	Cl	Cl	Me
2-pyridyl	H	H	B1	CF3	Cl	Me
2-pyridyl	H	H	B2	CF3	Cl	Me
2-pyridyl	H	H	B3	CF3	Cl	Me
2-pyridyl	H	H	B4	CF3	Cl	Me
2-pyridyl	Cl	H	B4	CF3	Cl	Me
2-pyridyl	CO2Me	H	B4	CF3	Cl	Me
2-pyridyl	H	H	B5	CF3	Cl	Me
2-pyridyl	H	H	B6	CF3	Cl	Me
2-pyridyl	H	H	B7	CF3	Cl	Me
2-pyridyl	Cl	H	B7	CF3	Cl	Me
2-pyridyl	NO2	H	B7	CF3	Cl	Me
2-pyridyl	CO2Me	H	B7	CF3	Cl	Me
2-pyridyl	H	H	B8	CF3	Cl	Me
2-pyridyl	H	H	B9	CF3	Cl	Me
2-pyridyl	H	H	B10	CF3	Cl	Me
2-pyridyl	H	H	B11	CF3	Cl	Me
2-pyridyl	H	H	B12	CF3	Cl	Me
2-pyridyl	H	H	B13	CF3	Cl	Me
2-pyridyl	H	H	B14	CF3	Cl	Me
2-pyridyl	H	H	B15	CF3	Cl	Me
2-pyridyl	H	H	B16	CF3	Cl	Me
2-pyridyl	H	H	B17	CF3	Cl	Me
2-pyridyl	H	H	B18	CF3	Cl	Me
2-pyridyl	H	H	B19	CF3	Cl	Me
2-pyridyl	H	H	B20	CF3	Cl	Me
2-pyridyl	H	H	B21	CF3	Cl	Me
2-pyridyl	H	H	B22	CF3	Cl	Me
2-pyridyl	H	H	B23	CF3	Cl	Me
2-pyridyl	H	H	B24	CF3	Cl	Me
2-pyridyl	H	H	B25	CF3	Cl	Me
2-pyridyl	H	H	B26	CF3	Cl	Me
2-pyridyl	H	H	B27	CF3	Cl	Me
2-pyridyl	H	H	B28	CF3	Cl	Me
2-pyridyl	H	H	B29	CF3	Cl	Me
2-pyridyl	H	H	B30	CF3	Cl	Me
2-pyridyl	H	H	B31	CF3	Cl	Me
2-pyridyl	H	H	B32	CF3	Cl	Me
2-pyridyl	H	H	B33	CF3	Cl	Me
2-pyridyl	H	H	B34	CF3	Cl	Me
2-pyridyl	H	H	Na	CF3	Cl	Me
2-pyridyl	H	H	K	CF3	Cl	Me
2-pyridyl	H	H	B1	Cl	H	H
2-pyridyl	H	H	B2	Cl	H	H
2-pyridyl	H	H	B3	Cl	H	H
2-pyridyl	H	H	B4	Cl	H	H
2-pyridyl	Me	H	B4	Cl	H	H
2-pyridyl	Cl	H	B4	Cl	H	H
2-pyridyl	NO2	H	B4	Cl	H	H
2-pyridyl	CO2Me	H	B4	Cl	H	H
2-pyridyl	CO2Et	H	B4	Cl	H	H
2-pyridyl	H	H	B5	Cl	H	H
2-pyridyl	H	H	B6	Cl	H	H
2-pyridyl	NO2	H	B6	Cl	H	H
2-pyridyl	H	H	B7	Cl	H	H
2-pyridyl	Me	H	B7	Cl	H	H
2-pyridyl	Cl	H	B7	Cl	H	H
2-pyridyl	NO2	H	B7	Cl	H	H
2-pyridyl	CO2Me	H	B7	Cl	H	H
2-pyridyl	CO2Et	H	B7	Cl	H	H
2-pyridyl	H	H	B8	Cl	H	H
2-pyridyl	H	H	B9	Cl	H	H
2-pyridyl	H	H	B10	Cl	H	H
2-pyridyl	H	H	B11	Cl	H	H
2-pyridyl	H	H	B12	Cl	H	H
2-pyridyl	H	H	B13	Cl	H	H
2-pyridyl	H	H	B14	Cl	H	H
2-pyridyl	H	H	B15	Cl	H	H
2-pyridyl	H	H	B16	Cl	H	H
2-pyridyl	H	H	B17	Cl	H	H
2-pyridyl	H	H	B18	Cl	H	H
2-pyridyl	H	H	B19	Cl	H	H
2-pyridyl	H	H	B20	Cl	H	H
2-pyridyl	H	H	B21	Cl	H	H
2-pyridyl	H	H	B22	Cl	H	H
2-pyridyl	H	H	B23	Cl	H	H
2-pyridyl	H	H	B24	Cl	H	H
2-pyridyl	H	H	B25	Cl	H	H
2-pyridyl	H	H	B26	Cl	H	H
2-pyridyl	H	H	B27	Cl	H	H
2-pyridyl	H	H	B28	Cl	H	H
2-pyridyl	H	H	B29	Cl	H	H
2-pyridyl	H	H	B30	Cl	H	H
2-pyridyl	H	H	B31	Cl	H	H
2-pyridyl	H	H	B32	Cl	H	H
2-pyridyl	H	H	B33	Cl	H	H
2-pyridyl	H	H	B34	Cl	H	H
2-pyridyl	H	H	Na	Cl	H	H
2-pyridyl	H	H	K	Cl	H	H
3-pyridyl	H	H	H	Cl	Cl	Me
3-pyridyl	H	H	H	CF3	Cl	Me
3-pyridyl	H	H	H	Cl	H	H
3-pyridyl	H	H	B4	Cl	H	H
3-pyridyl	H	H	B7	Cl	H	H
4-pyridyl	H	H	H	Cl	Cl	Me
4-pyridyl	H	H	H	CF3	Cl	Me
4-pyridyl	H	H	H	Cl	H	H
4-pyridyl	H	H	B4	Cl	H	H
4-pyridyl	H	H	B7	Cl	H	H
3-Me-pyridin-	H	H	H	Cl	Cl	Me
2-yl
2-F—Ph	H	H	H	Me	H	Me
2-F—Ph	H	H	H	Me	Me	Me
2-F—Ph	H	H	H	Me	Cl	Me
2-F—Ph	H	H	H	Cl	H	H
2-F—Ph	H	H	H	Cl	H	Me
2-F—Ph	H	H	H	Cl	H	CF3
2-F—Ph	H	H	H	Cl	Cl	Me
2-F—Ph	Cl	H	H	Cl	Cl	Me
2-F—Ph	H	H	B7	OMe	H	H
2-F—Ph	H	H	B7	SMe	H	H
2-F—Ph	H	H	H	CF3	Me	Me
2-F—Ph	H	H	H	CF3	Cl	Me
2-F—Ph	Cl	H	H	CF3	Cl	Me
2-F—Ph	H	H	H	CF3	H	Me
2-F—Ph	H	H	B1	Cl	Cl	Me
2-F—Ph	Cl	H	B1	Cl	Cl	Me
2-F—Ph	H	H	B3	Cl	Cl	Me
2-F—Ph	Cl	H	B4	Cl	Cl	Me
2-F—Ph	H	H	B6	Cl	Cl	Me
2-F—Ph	H	H	B7	Cl	Cl	Me
2-F—Ph	Cl	H	B7	Cl	Cl	Me
2-F—Ph	H	H	B9	Cl	Cl	Me
2-F—Ph	H	H	B20	Cl	Cl	Me
2-F—Ph	H	H	B24	Cl	Cl	Me
2-F—Ph	H	H	B2	CF3	Cl	Me
2-F—Ph	H	H	B3	CF3	Cl	Me
2-F—Ph	H	H	B4	CF3	Cl	Me
2-F—Ph	Cl	H	B4	CF3	Cl	Me
2-F—Ph	H	H	B6	CF3	Cl	Me
2-F—Ph	H	H	B7	CF3	Cl	Me
2-F—Ph	Cl	H	B7	CF3	Cl	Me
2-F—Ph	H	H	B9	CF3	Cl	Me
2-F—Ph	H	H	B20	CF3	Cl	Me
2-F—Ph	H	H	B24	CF3	Cl	Me
2-F—Ph	H	H	B6	Cl	H	H
2-F—Ph	H	H	B7	Cl	H	H
3-F—Ph	H	H	H	Cl	Cl	Me
3-F—Ph	Cl	H	H	Cl	Cl	Me
3-F—Ph	H	H	H	CF3	Cl	Me
3-F—Ph	Cl	H	H	CF3	Cl	Me
4-F—Ph	H	H	H	CI	Cl	Me
4-F—Ph	CI	H	H	CI	Cl	Me
4-F—Ph	H	H	H	CF3	CI	Me
4-F—Ph	CI	H	H	CF3	Cl	Me
2,3-F2—Ph	H	H	H	Cl	Cl	Me
2,3-F2—Ph	H	H	H	CF3	Cl	Me
2,4-F2—Ph	H	H	H	Cl	Cl	Me
2,4-F2—Ph	H	H	H	CF3	Cl	Me
2,5-F2—Ph	H	H	H	Cl	Cl	Me
2,5-F2—Ph	H	H	H	CF3	Cl	Me
Ph	H	H	H	Me	H	Me
Ph	H	H	H	Me	Me	Me
Ph	H	H	H	Me	Cl	Me
Ph	H	H	B7	Cl	H	H
Ph	H	H	H	Cl	H	Me
Ph	H	H	H	Cl	H	CF3
Ph	H	H	H	Cl	Cl	Me
Ph	Cl	H	H	Cl	Cl	Me
Ph	H	H	B7	OMe	H	H
Ph	H	H	B7	SMe	H	H
Ph	H	H	H	CF3	Me	Me
Ph	H	H	H	CF3	Cl	Me
Ph	Cl	H	H	CF3	Cl	Me
Ph	H	H	B7	CF3	H	Me
Ph	H	H	B1	Cl	Cl	Me
Ph	Cl	H	B1	CI	Cl	Me
Ph	H	H	B3	Cl	Cl	Me
Ph	Cl	H	B4	Cl	Cl	Me
Ph	H	H	B6	Cl	Cl	Me
Ph	H	H	B7	Cl	Cl	Me
Ph	Cl	H	B7	Cl	Cl	Me
Ph	H	H	B9	Cl	Cl	Me
Ph	H	H	B20	Cl	Cl	Me
Ph	H	H	B24	Cl	Cl	Me
Ph	H	H	B2	CF3	Cl	Me
Ph	H	H	B3	CF3	Cl	Me
Ph	H	H	B4	CF3	Cl	Me
Ph	Cl	H	B4	CF3	Cl	Me
Ph	H	H	B6	CF3	Cl	Me
Ph	H	H	B7	CF3	Cl	Me
Ph	Cl	H	B7	CF3	Cl	Me
Ph	H	H	B9	CF3	Cl	Me
Ph	H	H	B20	CF3	Cl	Me
Ph	H	H	B24	CF3	Cl	Me
Ph	H	H	B6	Cl	H	H
Ph	H	H	B7	Cl	H	H
3,4-F2—Ph	H	H	H	Cl	Cl	Me
3,4-F2—Ph	H	H	H	CF3	Cl	Me
3,5-F2—Ph	H	H	H	Cl	Cl	Me
3,5-F2—Ph	H	H	H	CF3	Cl	Me
2-Cl—Ph	H	H	H	Me	H	Me
2-Cl—Ph	H	H	H	Me	Me	Me
2-Cl—Ph	H	H	H	Me	Cl	Me
2-Cl—Ph	H	H	H	Cl	H	H
2-Cl—Ph	H	H	H	Cl	H	Me
2-Cl—Ph	H	H	H	Cl	H	CF3
2-Cl—Ph	H	H	H	Cl	Cl	Me
2-Cl—Ph	Cl	H	H	Cl	Cl	Me
2-Cl—Ph	H	H	H	OMe	H	H
2-Cl—Ph	H	H	H	SMe	H	H
2-Cl—Ph	H	H	H	CF3	Me	Me
2-Cl—Ph	H	H	H	CF3	Cl	Me
2-Cl—Ph	Cl	H	H	CF3	Cl	Me
2-Cl—Ph	H	H	H	CF3	H	Me
2-Cl—Ph	H	H	B1	Cl	Cl	Me
2-Cl—Ph	Cl	H	B1	Cl	Cl	Me
2-Cl—Ph	H	H	B3	Cl	Cl	Me
2-Cl—Ph	Cl	H	B4	Cl	Cl	Me
2-Cl—Ph	H	H	B6	Cl	Cl	Me
2-Cl—Ph	H	H	B7	Cl	Cl	Me
2-Cl—Ph	Cl	H	B7	Cl	Cl	Me
2-Cl—Ph	H	H	B9	Cl	Cl	Me
2-Cl—Ph	H	H	B20	Cl	Cl	Me
2-Cl—Ph	H	H	B24	Cl	Cl	Me
2-Cl—Ph	H	H	B2	CF3	Cl	Me
2-Cl—Ph	H	H	B3	CF3	Cl	Me
2-Cl—Ph	H	H	B4	CF3	Cl	Me
2-Cl—Ph	Cl	H	B4	CF3	Cl	Me
2-Cl—Ph	H	H	B6	CF3	Cl	Me
2-Cl—Ph	H	H	B7	CF3	Cl	Me
2-Cl—Ph	Cl	H	B7	CF3	Cl	Me
2-Cl—Ph	H	H	B9	CF3	Cl	Me
2-Cl—Ph	H	H	B20	CF3	Cl	Me
2-Cl—Ph	H	H	B24	CF3	Cl	Me
2-Cl—Ph	H	H	B6	Cl	H	H
2-Cl—Ph	H	H	B7	Cl	H	H
3-Cl—Ph	H	H	H	Cl	Cl	Me
3-Cl—Ph	Cl	H	H	Cl	Cl	Me
3-Cl—Ph	H	H	H	CF3	Cl	Me
3-Cl—Ph	Cl	H	H	CF3	Cl	Me
4-Cl—Ph	H	H	H	Cl	Cl	Me
4-Cl—Ph	Cl	H	H	Cl	Cl	Me
4-Cl—Ph	H	H	H	CF3	Cl	Me
4-Cl—Ph	Cl	H	H	CF3	Cl	Me
2,3-Cl2—Ph	H	H	H	Cl	Cl	Me
2,3-Cl2—Ph	H	H	H	CF3	Cl	Me
2,4-Cl2—Ph	H	H	H	Cl	Cl	Me
2,4-Cl2—Ph	H	H	H	CF3	Cl	Me
2,5-Cl2—Ph	H	H	H	Cl	Cl	Me
2,5-Cl2—Ph	H	H	H	CF3	Cl	Me
2,6-C12—Ph	H	H	H	Me	H	Me
2,6-C12—Ph	H	H	H	Me	Me	Me
2,6-Cl2—Ph	H	H	H	Me	Cl	Me
2,6-Cl2—Ph	H	H	B7	Cl	H	H
2,6-Cl2—Ph	H	H	H	Cl	H	Me
2,6-Cl2—Ph	H	H	H	Cl	H	CF3
2,6-Cl2—Ph	H	H	H	Cl	Cl	Me
2,6-Cl2—Ph	Cl	H	H	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B7	OMe	H	H
2,6-Cl2—Ph	H	H	B7	SMe	H	H
2,6-Cl2—Ph	H	H	H	CF3	Me	Me
2,6-Cl2—Ph	H	H	H	CF3	Cl	Me
2,6-Cl2—Ph	Cl	H	H	CF3	Cl	Me
2,6-Cl2—Ph	H	H	H	CF3	H	Me
2,6-Cl2—Ph	H	H	B1	Cl	Cl	Me
2,6-Cl2—Ph	Cl	H	B1	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B3	Cl	Cl	Me
2,6-Cl2—Ph	Cl	H	B4	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B6	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B7	Cl	Cl	Me
2,6-Cl2—Ph	Cl	H	B7	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B9	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B20	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B24	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B2	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B3	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B4	CF3	Cl	Me
2,6-Cl2—Ph	Cl	H	B4	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B6	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B7	CF3	Cl	Me
2,6-Cl2—Ph	Cl	H	B7	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B9	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B20	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B24	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B8	Cl	H	H
2,6-Cl2—Ph	H	H	B15	Cl	H	H
3,4-Cl2—Ph	H	H	H	Cl	Cl	Me
3,4-Cl2—Ph	H	H	H	CF3	Cl	Me
3,5-Cl2—Ph	H	H	H	Cl	Cl	Me
3,5-Cl2—Ph	H	H	H	CF3	Cl	Me
2-Me—Ph	H	H	H	Cl	Cl	Me
2-Me—Ph	H	H	H	CF3	Cl	Me
2,6-Me2—Ph	H	H	H	Cl	Cl	Me
2,6-Me2—Ph	H	H	H	CF3	Cl	Me
2-MeO—Ph	H	H	H	Cl	Cl	Me
2-MeO—Ph	H	H	H	CF3	Cl	Me
2-MeO—Ph	Cl	H	H	CF3	Cl	Me
2-CF3O—Ph	H	H	H	Cl	Cl	Me
2-CF3O—Ph	H	H	H	CF3	Cl	Me
2-SMe—Ph	H	H	H	Cl	Cl	Me
2-SMe—Ph	H	H	H	CF3	Cl	Me
2-SOMe—Ph	H	H	H	Cl	Cl	Me
2-SOMe—Ph	H	H	H	CF3	Cl	Me
2-SO2Me—Ph	H	H	H	Cl	Cl	Me
2-SO2Me—Ph	H	H	H	CF3	Cl	Me
2-CF3—Ph	H	H	H	Cl	Cl	Me
2-CF3—Ph	H	H	H	CF3	Cl	Me
2-NO2—Ph	H	H	H	Cl	Cl	Me
2-NO2—Ph	H	H	H	CF3	Cl	Me
2-CN—Ph	H	H	H	Cl	Cl	Me
2-CN—Ph	H	H	H	CF3	Cl	Me
2-NHMe—Ph	H	H	H	Cl	Cl	Me
2-NHMe—Ph	H	H	H	CF3	Cl	Me
2-NMe2—Ph	H	H	H	Cl	Cl	Me
2-NMe2—Ph	H	H	H	CF3	Cl	Me
4-CH2Ph—Ph	H	H	H	Cl	Cl	Me
4-OPh—Ph	H	H	H	Cl	Cl	Me
2-OH—Ph	H	H	H	Cl	Cl	Me
2-OH—Ph	H	H	H	CF3	Cl	Me
2-CO2Me—Ph	H	H	H	Cl	Cl	Me
2-CO2Me—Ph	H	H	H	CF3	Cl	Me
2-CO2Et—Ph	H	H	H	Cl	Cl	Me
2-CO2Et—Ph	H	H	H	CF3	Cl	Me
H	CO2Et	Ph	H	Cl	Cl	Me
Cl	CO2Et	H	H	Cl	Cl	Me
Me	Ph	H	H	Cl	Cl	Me
Et	Me	H	H	Cl	Cl	Me
nPr	H	H	H	Cl	Cl	Me
iPr	H	H	H	Cl	Cl	Me
iPr	H	H	H	CF3	Cl	Me
nBu	H	H	H	Cl	Cl	Me
nBu	H	H	H	CF3	Cl	Me
iBu	H	H	H	Cl	Cl	Me
iBu	H	H	H	CF3	Cl	Me
iBu	H	H	B7	Cl	Cl	Me
iBu	H	H	B7	CF3	Cl	Me
secBu	H	H	H	Cl	Cl	Me
secBu	H	H	H	CF3	Cl	Me
2,2-Me2-propyl	H	H	H	Cl	Cl	Me
nHex	H	H	H	Cl	Cl	Me
ethenyl	H	H	H	Cl	Cl	Me
1-propenyl	H	H	H	Cl	Cl	Me
1-propenyl	H	H	H	CF3	Cl	Me
ethynyl	H	H	H	Cl	Cl	Me
1-propynyl	H	H	H	Cl	Cl	Me
1-propynyl	H	H	H	CF3	Cl	Me
CF3	H	H	H	Cl	Cl	Me
CF3	H	H	H	CF3	Cl	Me
C2F5	H	H	H	Cl	Cl	Me
C2F5	H	H	H	CF3	Cl	Me
2,2-Cl2-cPr	H	H	H	Cl	Cl	Me
2,2-Cl2-cPr	H	H	H	CF3	Cl	Me
cPr	H	H	H	Cl	Cl	Me
cPr	H	H	H	CF3	Cl	Me
1-Me-cPr	H	H	H	Cl	Cl	Me
1-Me-cPr	H	H	H	CF3	Cl	Me
cHex	H	H	H	Cl	Cl	Me
cHex	H	H	H	CF3	Cl	Me
OMe	H	H	H	Cl	Cl	Me
OtBu	H	H	H	Cl	Cl	Me
OtBu	H	H	H	CF3	Cl	Me
OCF3	H	H	H	Cl	Cl	Me
OCF3	H	H	H	CF3	Cl	Me
StBu	H	H	H	Cl	Cl	Me
StBu	H	H	H	CF3	Cl	Me
SOtBu	H	H	H	Cl	Cl	Me
SOtBu	H	H	H	CF3	Cl	Me
SO2tBu	H	H	H	Cl	Cl	Me
SO2tBu	H	H	H	CF3	CI	Me
NO2	H	H	H	Cl	Cl	Me
NO2	H	H	H	CF3	Cl	Me
CN	H	H	H	Cl	Cl	Me
CN	H	H	H	CF3	Cl	Me
NH2	H	H	H	Cl	Cl	Me
NH2	H	H	H	CF3	Cl	Me
NHMe	H	H	H	Cl	Cl	Me
NHMe	H	H	H	CF3	Cl	Me
NMe2	H	H	H	Cl	Cl	Me
NMe2	H	H	H	CF3	Cl	Me
CH2Ph	H	H	H	Cl	Cl	Me
CH2Ph	H	H	H	CF3	Cl	Me
OPh	H	H	H	Cl	Cl	Me
OPh	H	H	H	CF3	Cl	Me
OH	H	H	H	Cl	Cl	Me
OH	H	H	H	CF3	Cl	Me
naphthyl-1	H	H	H	Cl	Cl	Me
naphthyl-1	H	H	H	CF3	Cl	Me
naphthyl-2	H	H	H	Cl	Cl	Me
naphthyl-2	H	H	H	CF3	Cl	Me
CO2Me	H	H	H	Cl	Cl	Me
CO2Me	H	H	H	CF3	Cl	Me
CO2Et	H	H	H	Cl	Cl	Me
CO2Et	H	H	H	CF3	Cl	Me
2-thienyl	H	H	H	Cl	Cl	Me
2-thienyl	H	H	H	CF3	Cl	Me
CH2OMe	H	H	H	Cl	Cl	Me
COCH3	H	H	H	Cl	Cl	Me
—N═CMe2	H	H	H	Cl	Cl	Me
—N═CMe2	H	H	H	CF3	Cl	Me
—(CH2)3—	H	H	Cl	Cl	Me
—(CH2)3—	H	H	CF3	Cl	Me
—(CH2)4—	H	H	Cl	Cl	Me
—(CH2)4—	H	H	CF3	Cl	Me

TABLE 2
R1	R2	R3	B	Y1	Y2	Y3
2,6-F2—Ph	H	H	H	Me	H	Me
2,6-F2—Ph	H	H	H	Me	H	CF3
2,6-F2—Ph	H	H	H	Me	H	H
2,6-F2—Ph	H	H	H	Me	Me	Me
2,6-F2—Ph	H	H	H	Me	Cl	Me
2,6-F2—Ph	Cl	H	H	Me	Cl	Me
2,6-F2—Ph	H	H	H	Et	Me	Me
2,6-F2—Ph	H	H	H	Cl	Me	Me
2,6-F2—Ph	H	H	H	Cl	H	Me
2,6-F2—Ph	H	H	H	Cl	H	CF3
2,6-F2—Ph	H	H	H	Cl	H	H
2,6-F2—Ph	Me	H	H	Cl	H	H
2,6-F2—Ph	Cl	H	H	Cl	H	H
2,6-F2—Ph	H	H	H	Cl	Cl	Me
2,6-F2—Ph	Me	H	H	Cl	Cl	Me
2,6-F2—Ph	H	Cl	H	Cl	Cl	Me
2,6-F2—Ph	Cl	H	H	Cl	Cl	Me
2,6-F2—Ph	CF3	H	H	Cl	Cl	Me
2,6-F2—Ph	OMe	H	H	Cl	Cl	Me
2,6-F2—Ph	NH2	H	H	Cl	Cl	Me
2,6-F2—Ph	NHMe	H	H	Cl	Cl	Me
2,6-F2—Ph	NMe2	H	H	Cl	Cl	Me
2,6-F2—Ph	NO2	H	H	Cl	Cl	Me
2,6-F2—Ph	CN	H	H	Cl	Cl	Me
2,6-F2—Ph	OH	H	H	Cl	Cl	Me
2,6-F2—Ph	CO2Me	H	H	Cl	Cl	Me
2,6-F2—Ph	CO2Et	H	H	Cl	Cl	Me
2,6-F2—Ph	H	H	H	Cl	Cl	CF3
2,6-F2—Ph	H	H	H	Cl	Cl	CF2H
2,6-F2—Ph	H	H	H	Cl	Cl	CH2OMe
2,6-F2—Ph	H	H	H	Cl	Cl	COMe
2,6-F2—Ph	H	H	H	Cl	CF3	Me
2,6-F2—Ph	H	H	H	Br	Me	Me
2,6-F2—Ph	H	H	H	Me	Br	Me
2,6-F2—Ph	H	H	H	Me	OMe	Me
2,6-F2—Ph	H	H	H	OMe	H	H
2,6-F2—Ph	H	H	H	OCF3	H	H
2,6-F2—Ph	H	H	H	SMe	H	H
2,6-F2—Ph	H	H	H	CF3	Me	Me
2,6-F2—Ph	H	H	H	CF3	Cl	Me
2,6-F2—Ph	Me	H	H	CF3	Cl	Me
2,6-F2—Ph	Cl	H	H	CF3	Cl	Me
2,6-F2—Ph	Br	H	H	CF3	Cl	Me
2,6-F2—Ph	CF3	H	H	CF3	Cl	Me
2,6-F2—Ph	NO2	H	H	CF3	Cl	Me
2,6-F2—Ph	CN	H	H	CF3	Cl	Me
2,6-F2—Ph	CO2Me	H	H	CF3	Cl	Me
2,6-F2—Ph	CO2Et	H	H	CF3	Cl	Me
2,6-F2—Ph	H	H	H	CF3	Cl	CF3
2,6-F2—Ph	H	H	H	CF3	Cl	CF2H
2,6-F2—Ph	H	H	H	CF3	Cl	CH2OMe
2,6-F2—Ph	H	H	H	CF3	Cl	COCH3
2,6-F2—Ph	H	H	H	CF3	H	Me
2,6-F2—Ph	H	H	H	CF3	Br	Me
2,6-F2—Ph	H	H	H	CF3	NO2	Me
2,6-F2—Ph	H	H	H	CF3	CN	Me
2,6-F2—Ph	H	H	H	CF3	NHMe	Me
2,6-F2—Ph	H	H	H	CF3	NMe2	Me
2,6-F2—Ph	H	H	H	CF3	CO2Me	Me
2,6-F2—Ph	H	H	H	CF3	OMe	Me
2,6-F2—Ph	H	H	H	CF3	OCF2H	CF2H
2,6-F2—Ph	H	H	H	Cl	NO2	Me
2,6-F2—Ph	H	H	H	Cl	CN	Me
2,6-F2—Ph	H	H	H	CO2Me	Me	Me
2,6-F2—Ph	H	H	B1	Cl	Cl	Me
2,6-F2—Ph	H	H	B2	Cl	Cl	Me
2,6-F2—Ph	H	H	B3	Cl	Cl	Me
2,6-F2—Ph	H	H	B4	Cl	Cl	Me
2,6-F2—Ph	H	H	B5	Cl	Cl	Me
2,6-F2—Ph	H	H	B6	Cl	Cl	Me
2,6-F2—Ph	H	H	B7	Cl	Cl	Me
2,6-F2—Ph	H	H	B8	Cl	Cl	Me
2,6-F2—Ph	H	H	B9	Cl	Cl	Me
2,6-F2—Ph	H	H	B10	Cl	Cl	Me
2,6-F2—Ph	H	H	B11	Cl	Cl	Me
2,6-F2—Ph	H	H	B12	Cl	Cl	Me
2,6-F2—Ph	H	H	B13	Cl	Cl	Me
2,6-F2—Ph	H	H	B14	Cl	Cl	Me
2,6-F2—Ph	H	H	B15	Cl	Cl	Me
2,6-F2—Ph	H	H	B16	Cl	Cl	Me
2,6-F2—Ph	H	H	B17	Cl	Cl	Me
2,6-F2—Ph	H	H	B18	Cl	Cl	Me
2,6-F2—Ph	H	H	B19	Cl	Cl	Me
2,6-F2—Ph	H	H	B20	Cl	Cl	Me
2,6-F2—Ph	H	H	B21	Cl	Cl	Me
2,6-F2—Ph	H	H	B22	Cl	Cl	Me
2,6-F2—Ph	H	H	B23	Cl	Cl	Me
2,6-F2—Ph	H	H	B24	Cl	Cl	Me
2,6-F2—Ph	H	H	B25	Cl	Cl	Me
2,6-F2—Ph	H	H	B26	Cl	Cl	Me
2,6-F2—Ph	H	H	B27	Cl	Cl	Me
2,6-F2—Ph	H	H	B28	Cl	Cl	Me
2,6-F2—Ph	H	H	B29	Cl	Cl	Me
2,6-F2—Ph	H	H	B30	Cl	Cl	Me
2,6-F2—Ph	H	H	B31	Cl	Cl	Me
2,6-F2—Ph	H	H	B32	Cl	Cl	Me
2,6-F2—Ph	H	H	B33	Cl	Cl	Me
2,6-F2—Ph	H	H	B34	Cl	Cl	Me
2,6-F2—Ph	H	H	Na	Cl	Cl	Me
2,6-F2—Ph	H	H	K	Cl	Cl	Me
2,6-F2—Ph	H	H	B2	CF3	Cl	Me
2,6-F2—Ph	H	H	B3	CF3	Cl	Me
2,6-F2—Ph	H	H	B4	CF3	Cl	Me
2,6-F2—Ph	H	H	B5	CF3	Cl	Me
2,6-F2—Ph	H	H	B6	CF3	Cl	Me
2,6-F2—Ph	H	H	B7	CF3	Cl	Me
2,6-F2—Ph	H	H	B8	CF3	Cl	Me
2,6-F2—Ph	H	H	B9	CF3	Cl	Me
2,6-F2—Ph	H	H	B10	CF3	Cl	Me
2,6-F2—Ph	H	H	B11	CF3	Cl	Me
2,6-F2—Ph	H	H	B12	CF3	Cl	Me
2,6-F2—Ph	H	H	B13	CF3	Cl	Me
2,6-F2—Ph	H	H	B14	CF3	Cl	Me
2,6-F2—Ph	H	H	B15	CF3	Cl	Me
2,6-F2—Ph	H	H	B16	CF3	Cl	Me
2,6-F2—Ph	H	H	B17	CF3	Cl	Me
2,6-F2—Ph	H	H	B18	CF3	Cl	Me
2,6-F2—Ph	H	H	B19	CF3	Cl	Me
2,6-F2—Ph	H	H	B20	CF3	Cl	Me
2,6-F2—Ph	H	H	B21	CF3	Cl	Me
2,6-F2—Ph	H	H	B22	CF3	Cl	Me
2,6-F2—Ph	H	H	B23	CF3	Cl	Me
2,6-F2—Ph	H	H	B24	CF3	Cl	Me
2,6-F2—Ph	H	H	B25	CF3	Cl	Me
2,6-F2—Ph	H	H	B26	CF3	Cl	Me
2,6-F2—Ph	H	H	B27	CF3	Cl	Me
2,6-F2—Ph	H	H	B28	CF3	Cl	Me
2,6-F2—Ph	H	H	B29	CF3	Cl	Me
2,6-F2—Ph	H	H	B30	CF3	Cl	Me
2,6-F2—Ph	H	H	B31	CF3	Cl	Me
2,6-F2—Ph	H	H	B32	CF3	Cl	Me
2,6-F2—Ph	H	H	B33	CF3	Cl	Me
2,6-F2—Ph	H	H	B34	CF3	Cl	Me
2,6-F2—Ph	H	H	Na	CF3	Cl	Me
2,6-F2—Ph	H	H	K	CF3	Cl	Me
2,6-F2—Ph	H	H	B7	Cl	H	H
2,6-F2—Ph	H	H	B9	Cl	H	H
2,6-F2—Ph	H	H	B10	Cl	H	H
2,6-F2—PhPh	H	H	B11	Cl	H	H
tBu	H	H	H	Me	H	Me
tBu	H	H	H	Me	H	CF3
tBu	H	H	H	Me	H	H
tBu	H	H	H	Me	Me	Me
tBu	H	H	H	Me	Cl	Me
tBu	Cl	H	H	Me	Cl	Me
tBu	H	H	H	Cl	Me	Me
tBu	H	H	H	Cl	H	Me
tBu	H	H	H	Cl	H	CF3
tBu	H	H	H	Cl	H	H
tBu	H	H	H	Cl	Cl	Me
tBu	Me	H	H	Cl	Cl	Me
tBu	Cl	H	H	Cl	Cl	Me
tBu	NO2	H	H	Cl	Cl	Me
tBu	CO2Me	H	H	Cl	Cl	Me
tBu	CO2Et	H	H	Cl	Cl	Me
tBu	H	H	H	Cl	Cl	CF3
tBu	H	H	H	Cl	Cl	CF2H
tBu	H	H	H	Cl	Cl	CH2OMe
tBu	H	H	H	Cl	Cl	COMe
tBu	H	H	H	Cl	CF3	Me
tBu	H	H	H	Br	Me	Me
tBu	H	H	H	Me	Br	Me
tBu	H	H	H	OMe	H	H
tBu	H	H	H	CF3	Me	Me
tBu	H	H	H	CF3	Cl	Me
tBu	Me	H	H	CF3	Cl	Me
tBu	Cl	H	H	CF3	Cl	Me
tBu	NO2	H	H	CF3	Cl	Me
tBu	CO2Me	H	H	CF3	Cl	Me
tBu	CO2Et	H	H	CF3	Cl	Me
tBu	H	H	H	CF3	Cl	CF3
tBu	H	H	H	CF3	Cl	CF2H
tBu	H	H	H	CF3	Cl	CH2OMe
tBu	H	H	H	CF3	Cl	COCH3
tBu	H	H	H	CF3	H	Me
tBu	H	H	H	CF3	NO2	Me
tBu	H	H	H	CF3	NHMe	Me
tBu	H	H	H	CF3	NMe2	Me
tBu	H	H	H	NO2	Me	Me
tBu	H	H	H	CN	Cl	Me
tBu	H	H	H	CN	Me	Me
tBu	H	H	H	Cl	CN	Me
tBu	H	H	H	CO2Me	Me	Me
tBu	H	H	H	CO2Me	Cl	Me
tBu	H	H	B1	Cl	Cl	Me
tBu	Cl	H	B1	Cl	Cl	Me
tBu	H	H	B2	Cl	Cl	Me
tBu	H	H	B3	Cl	Cl	Me
tBu	H	H	B4	Cl	Cl	Me
tBu	H	H	B5	Cl	Cl	Me
tBu	H	H	B6	Cl	Cl	Me
tBu	H	H	B7	Cl	Cl	Me
tBu	H	H	B8	Cl	Cl	Me
tBu	H	H	B9	Cl	Cl	Me
tBu	H	H	B10	Cl	Cl	Me
tBu	H	H	B11	Cl	Cl	Me
tBu	H	H	B12	Cl	Cl	Me
tBu	H	H	B13	Cl	Cl	Me
tBu	H	H	B14	Cl	Cl	Me
tBu	H	H	B15	Cl	Cl	Me
tBu	H	H	B16	Cl	Cl	Me
tBu	H	H	B17	Cl	Cl	Me
tBu	H	H	B18	Cl	Cl	Me
tBu	H	H	B19	Cl	Cl	Me
tBu	H	H	B20	Cl	Cl	Me
tBu	H	H	B21	Cl	Cl	Me
tBu	H	H	B22	Cl	Cl	Me
tBu	H	H	B23	Cl	Cl	Me
tBu	H	H	B24	Cl	Cl	Me
tBu	H	H	B25	Cl	Cl	Me
tBu	H	H	B26	Cl	Cl	Me
tBu	H	H	B27	Cl	Cl	Me
tBu	H	H	B28	Cl	Cl	Me
tBu	H	H	B29	Cl	Cl	Me
tBu	H	H	B30	Cl	Cl	Me
tBu	H	H	B31	Cl	Cl	Me
tBu	H	H	B32	Cl	Cl	Me
tBu	H	H	B33	Cl	Cl	Me
tBu	H	H	B34	Cl	Cl	Me
tBu	H	H	Na	Cl	Cl	Me
tBu	H	H	K	Cl	Cl	Me
tBu	H	H	B2	CF3	Cl	Me
tBu	H	H	B3	CF3	Cl	Me
tBu	H	H	B4	CF3	Cl	Me
tBu	H	H	B5	CF3	Cl	Me
tBu	H	H	B6	CF3	Cl	Me
tBu	H	H	B7	CF3	Cl	Me
tBu	H	H	B8	CF3	Cl	Me
tBu	H	H	B9	CF3	Cl	Me
tBu	H	H	B10	CF3	Cl	Me
tBu	H	H	B11	CF3	Cl	Me
tBu	H	H	B12	CF3	Cl	Me
tBu	H	H	B13	CF3	Cl	Me
tBu	H	H	B14	CF3	Cl	Me
tBu	H	H	B15	CF3	Cl	Me
tBu	H	H	B16	CF3	Cl	Me
tBu	H	H	B17	CF3	Cl	Me
tBu	H	H	B18	CF3	Cl	Me
tBu	H	H	B19	CF3	Cl	Me
tBu	H	H	B20	CF3	Cl	Me
tBu	H	H	B21	CF3	Cl	Me
tBu	H	H	B22	CF3	Cl	Me
tBu	H	H	B23	CF3	Cl	Me
tBu	H	H	B24	CF3	Cl	Me
tBu	H	H	B25	CF3	Cl	Me
tBu	H	H	B26	CF3	Cl	Me
tBu	H	H	B27	CF3	Cl	Me
tBu	H	H	B28	CF3	Cl	Me
tBu	H	H	B29	CF3	Cl	Me
tBu	H	H	B30	CF3	Cl	Me
tBu	H	H	B31	CF3	Cl	Me
tBu	H	H	B32	CF3	Cl	Me
tBu	H	H	B33	CF3	Cl	Me
tBu	H	H	B34	CF3	Cl	Me
tBu	H	H	Na	CF3	Cl	Me
tBu	H	H	K	CF3	Cl	Me
tBu	H	H	B7	Cl	H	H
tBu	H	H	B8	Cl	H	H
tBu	H	H	B15	Cl	H	H
tBu	H	H	B17	Cl	H	H
tBu	H	H	B18	Cl	H	H
tBu	H	H	B34	Cl	H	H
2-pyridyl	H	H	H	Me	H	Me
2-pyridyl	H	H	H	Me	H	CF3
2-pyridyl	H	H	B7	Me	H	H
2-pyridyl	H	H	H	Me	Me	Me
2-pyridyl	H	H	H	Me	Cl	Me
2-pyridyl	H	H	H	Cl	Me	Me
2-pyridyl	H	H	H	Cl	H	Me
2-pyridyl	H	H	H	Cl	H	CF3
2-pyridyl	H	H	H	Cl	H	H
2-pyridyl	Cl	H	H	Cl	H	H
2-pyridyl	CO2Me	H	H	Cl	H	H
2-pyridyl	CO2Et	H	H	Cl	H	H
2-pyridyl	H	H	H	Cl	Cl	Me
2-pyridyl	H	H	H	Cl	CF3	Me
2-pyridyl	H	H	H	Br	Me	Me
2-pyridyl	H	H	H	Me	Br	Me
2-pyridyl	H	H	B7	OMe	H	H
2-pyridyl	H	H	H	CF3	Me	Me
2-pyridyl	H	H	H	CF3	Cl	Me
2-pyridyl	H	H	H	CF3	H	Me
2-pyridyl	H	H	B7	CF3	H	H
2-pyridyl	H	H	B1	Cl	Cl	Me
2-pyridyl	H	H	B3	Cl	Cl	Me
2-pyridyl	H	H	B7	Cl	Cl	Me
2-pyridyl	H	H	B3	CF3	Cl	Me
2-pyridyl	H	H	B7	CF3	Cl	Me
2-pyridyl	H	H	B3	Cl	H	H
2-pyridyl	H	H	B4	Cl	H	H
2-pyridyl	H	H	B5	Cl	H	H
2-pyridyl	H	H	B6	Cl	H	H
2-pyridyl	H	H	B7	Cl	H	H
2-pyridyl	H	H	B8	Cl	H	H
2-pyridyl	H	H	B9	Cl	H	H
2-pyridyl	H	H	B10	Cl	H	H
2-pyridyl	H	H	B11	Cl	H	H
2-pyridyl	H	H	B15	Cl	H	H
2-pyridyl	H	H	B16	Cl	H	H
2-pyridyl	H	H	B17	Cl	H	H
2-pyridyl	H	H	B28	Cl	H	H
2-pyridyl	H	H	B30	Cl	H	H
2-pyridyl	H	H	B31	Cl	H	H
2-pyridyl	H	H	B32	Cl	H	H
2-pyridyl	H	H	B34	Cl	H	H
3-pyridyl	H	H	H	Cl	Cl	Me
3-pyridyl	H	H	H	Cl	H	H
4-pyridyl	H	H	H	Cl	Cl	Me
4-pyridyl	H	H	H	Cl	H	H
2-F—Ph	H	H	H	Cl	H	H
2-F—Ph	H	H	H	Cl	Cl	Me
2-F—Ph	H	H	B7	OMe	H	H
2-F—Ph	H	H	B7	SMe	H	H
2-F—Ph	H	H	H	CF3	Cl	Me
2-F—Ph	H	H	H	CF3	H	Me
2-F—Ph	H	H	B1	Cl	Cl	Me
2-F—Ph	H	H	B3	Cl	Cl	Me
2-F—Ph	H	H	B6	Cl	Cl	Me
2-F—Ph	H	H	B7	Cl	Cl	Me
2-F—Ph	Cl	H	B7	Cl	Cl	Me
2-F—Ph	H	H	B3	CF3	Cl	Me
2-F—Ph	H	H	B6	CF3	Cl	Me
2-F—Ph	H	H	B7	CF3	Cl	Me
2-F—Ph	Cl	H	B7	CF3	Cl	Me
2-F—Ph	H	H	B7	Cl	H	H
3-F—Ph	H	H	H	Cl	Cl	Me
3-F—Ph	H	H	H	CF3	Cl	Me
4-F—Ph	H	H	H	Cl	Cl	Me
4-F—Ph	H	H	H	CF3	Cl	Me
2,3-F2—Ph	H	H	H	Cl	Cl	Me
2,4-F2—Ph	H	H	H	Cl	Cl	Me
2,5-F2—Ph	H	H	H	Cl	Cl	Me
Ph	H	H	H	Cl	H	H
Ph	H	H	H	Cl	Cl	Me
Ph	H	H	H	OMe	H	H
Ph	H	H	H	SMe	H	H
Ph	H	H	H	CF3	Cl	Me
Ph	H	H	H	CF3	H	Me
Ph	H	H	B1	Cl	Cl	Me
Ph	H	H	B3	Cl	Cl	Me
Ph	H	H	B6	Cl	Cl	Me
Ph	H	H	B7	Cl	Cl	Me
Ph	Cl	H	B7	Cl	Cl	Me
Ph	H	H	B3	CF3	Cl	Me
Ph	H	H	B6	CF3	Cl	Me
Ph	H	H	B7	CF3	Cl	Me
Ph	Cl	H	B7	CF3	Cl	Me
Ph	H	H	B7	Cl	H	H
Ph	H	H	H	Cl	Cl	Me
Ph	H	H	H	Cl	Cl	Me
2-Cl—Ph	H	H	H	Cl	H	H
2-Cl—Ph	H	H	H	Cl	Cl	Me
2-Cl—Ph	H	H	H	OMe	H	H
2-Cl—Ph	H	H	H	SMe	H	H
2-Cl—Ph	H	H	H	CF3	Cl	Me
2-Cl—Ph	H	H	H	CF3	H	Me
2-Cl—Ph	H	H	B1	Cl	Cl	Me
2-Cl—Ph	H	H	B3	Cl	Cl	Me
2-Cl—Ph	H	H	B6	Cl	Cl	Me
2-Cl—Ph	H	H	B7	Cl	Cl	Me
2-Cl—Ph	Cl	H	B7	Cl	Cl	Me
2-Cl—Ph	H	H	B3	CF3	Cl	Me
2-Cl—Ph	H	H	B6	CF3	Cl	Me
2-Cl—Ph	H	H	B7	CF3	Cl	Me
2-Cl—Ph	Cl	H	B7	CF3	Cl	Me
2-Cl—Ph	H	H	B7	Cl	H	H
3-Cl—Ph	H	H	H	Cl	Cl	Me
4-Cl—Ph	H	H	H	Cl	Cl	Me
2,3-Cl2—Ph	H	H	H	Cl	Cl	Me
2,4-Cl2—Ph	H	H	H	Cl	Cl	Me
2,5-Cl2—Ph	H	H	H	Cl	Cl	Me
2,6-Cl2—Ph	H	H	H	Cl	H	H
2,6-Cl2—Ph	H	H	H	Cl	Cl	Me
2,6-Cl2—Ph	H	H	H	OMe	H	H
2,6-Cl2—Ph	H	H	H	SMe	H	H
2,6-Cl2—Ph	H	H	H	CF3	Cl	Me
2,6-Cl2—Ph	H	H	H	CF3	H	Me
2,6-Cl2—Ph	H	H	B1	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B3	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B6	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B7	Cl	Cl	Me
2,6-Cl2—Ph	Cl	H	B7	Cl	Cl	Me
2,6-Cl2—Ph	H	H	B3	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B6	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B7	CF3	Cl	Me
2,6-Cl2—Ph	Cl	H	B7	CF3	Cl	Me
2,6-Cl2—Ph	H	H	B7	Cl	H	H
3,4-Cl2—Ph	H	H	H	Cl	Cl	Me
3,5-Cl2—Ph	H	H	H	Cl	Cl	Me
2-Me—Ph	H	H	H	Cl	Cl	Me
2-Me—Ph	H	H	H	CF3	Cl	Me
2,6-Me2—Ph	H	H	H	Cl	Cl	Me
2,6-Me2—Ph	H	H	H	CF3	Cl	Me
2-MeO—Ph	H	H	H	Cl	Cl	Me
2-MeO—Ph	H	H	H	CF3	Cl	Me
2-CF3O—Ph	H	H	H	Cl	Cl	Me
2-SMe—Ph	H	H	H	Cl	Cl	Me
2-SOMe—Ph	H	H	H	Cl	Cl	Me
2-SO2Me—Ph	H	H	H	Cl	Cl	Me
2-CF3—Ph	H	H	H	Cl	Cl	Me
2-NO2—Ph	H	H	H	Cl	Cl	Me
2-CN—Ph	H	H	H	Cl	Cl	Me
2-NHMe—Ph	H	H	H	Cl	Cl	Me
2-NMe2—Ph	H	H	H	Cl	Cl	Me
4-benzyl-Ph	H	H	H	Cl	Cl	Me
4-phenoxy-Ph	H	H	H	Cl	Cl	Me
2-OH—Ph	H	H	H	Cl	Cl	Me
2-CO2Me—Ph	H	H	H	Cl	Cl	Me
2-CO2Et—Ph	H	H	H	Cl	Cl	Me
H	CO2Et	Ph	H	Cl	Cl	Me
Me	Ph	H	H	Cl	Cl	Me
Et	Me	H	H	Cl	Cl	Me
nPr	H	H	H	Cl	Cl	Me
iPr	H	H	H	Cl	Cl	Me
iPr	H	H	H	CF3	Cl	Me
nBu	H	H	H	Cl	Cl	Me
nBu	H	H	H	CF3	Cl	Me
iBu	H	H	H	Cl	Cl	Me
iBu	H	H	H	CF3	Cl	Me
iBu	H	H	B7	Cl	Cl	Me
iBu	H	H	B7	CF3	Cl	Me
iBu	H	H	H	Cl	H	H
secBu	H	H	H	Cl	Cl	Me
secBu	H	H	H	CF3	Cl	Me
2,2-Me2-propyl	H	H	H	Cl	Cl	Me
nHex	H	H	H	Cl	Cl	Me
ethenyl	H	H	H	Cl	Cl	Me
1-propenyl	H	H	H	Cl	Cl	Me
1-propenyl	H	H	H	CF3	Cl	Me
ethynyl	H	H	H	Cl	Cl	Me
1-propynyl	H	H	H	Cl	Cl	Me
CF3	H	H	H	Cl	Cl	Me
CHF2	H	H	H	Cl	Cl	Me
C2F5	H	H	H	Cl	Cl	Me
2,2-Cl2—cPr	H	H	H	Cl	Cl	Me
2,2-Cl2—cPr	H	H	H	CF3	Cl	Me
cPr	H	H	H	Cl	Cl	Me
cPr	H	H	H	CF3	Cl	Me
1-Me—cPr	H	H	H	Cl	Cl	Me
1-Me—cPr	H	H	H	CF3	Cl	Me
cHex	H	H	H	Cl	Cl	Me
cHex	H	H	H	CF3	Cl	Me
CH2Ph	H	H	H	Cl	Cl	Me
naphthyl-1	H	H	H	Cl	Cl	Me
naphthyl-1	H	H	H	CF3	Cl	Me
naphthyl-2	H	H	H	Cl	Cl	Me
CO2Me	H	H	H	Cl	Cl	Me
CO2Et	H	H	H	Cl	Cl	Me
2-thienyl	H	H	H	Cl	Cl	Me
CH2OMe	H	H	H	Cl	Cl	Me
CH2OEt	H	H	H	Cl	Cl	Me
COCH3	H	H	H	Cl	Cl	Me
COtBu	H	H	H	Cl	Cl	Me

TABLE 3
	R1	R2	R3	B	Y1	Y2
	2,6-F2—Ph	H	H	H	Me	Me
	2,6-F2—Ph	H	H	H	Et	Me
	2,6-F2—Ph	Me	H	H	Et	Me
	2,6-F2—Ph	Cl	H	H	Et	Me
	2,6-F2—Ph	H	Cl	H	Et	Me
	2,6-F2—Ph	H	H	H	Cl	Cl
	2,6-F2—Ph	H	H	H	Cl	Me
	2,6-F2—Ph	H	H	H	Cl	CF3
	2,6-F2—Ph	H	H	H	Me	Cl
	2,6-F2—Ph	H	H	H	Br	Me
	2,6-F2—Ph	H	H	H	Me	Br
	2,6-F2—Ph	H	H	H	Me	CF3
	2,6-F2—Ph	H	H	H	OMe	Me
	2,6-F2—Ph	H	H	H	OCF3	Me
	2,6-F2—Ph	H	H	H	SMe	Me
	2,6-F2—Ph	H	H	H	CO2Me	Me
	2,6-F2—Ph	H	H	H	CO2Et	Me
	2,6-F2—Ph	H	H	H	CF3	Me
	2,6-F2—Ph	H	H	H	CF3	H
	2,6-F2—Ph	H	H	B3	CF3	Me
	2,6-F2—Ph	H	H	B6	CF3	Me
	2,6-F2—Ph	H	H	B7	CF3	Me
	2,6-F2—Ph	Cl	H	B7	CF3	Me
	tBu	H	H	H	Me	Me
	tBu	H	H	H	Et	Me
	tBu	H	H	H	Cl	Cl
	tBu	H	H	H	Cl	Me
	tBu	H	H	H	Me	Cl
	tBu	H	H	H	Cl	CF3
	tBu	H	H	H	Br	Me
	tBu	H	H	H	Me	Br
	tBu	H	H	H	Me	CF3
	tBu	H	H	H	OMe	Me
	tBu	H	H	H	OCF3	Me
	tBu	H	H	H	SMe	Me
	tBu	H	H	H	CO2Me	Me
	tBu	H	H	H	CO2Et	Me
	tBu	H	H	H	CF3	Me
	tBu	Me	H	H	CF3	Me
	tBu	Cl	H	H	CF3	Me
	tBu	Br	H	H	CF3	Me
	tBu	CF3	H	H	CF3	Me
	tBu	NO2	H	H	CF3	Me
	tBu	CN	H	H	CF3	Me
	tBu	CO2Me	H	H	CF3	Me
	tBu	CO2Et	H	H	CF3	Me
	tBu	H	H	H	CF3	H
	tBu	H	H	H	CF3	Br
	tBu	H	H	H	CF3	NO2
	tBu	H	H	H	CF3	CN
	tBu	H	H	H	CF3	NHMe
	tBu	H	H	H	CF3	NMe2
	tBu	H	H	H	CF3	CO2Me
	tBu	H	H	B2	CF3	Me
	tBu	H	H	B3	CF3	Me
	tBu	H	H	B4	CF3	Me
	tBu	H	H	B5	CF3	Me
	tBu	H	H	B6	CF3	Me
	tBu	H	H	B7	CF3	Me
	tBu	Cl	H	B7	CF3	Me
	tBu	H	H	B8	CF3	Me
	tBu	H	H	B9	CF3	Me
	tBu	H	H	B10	CF3	Me
	tBu	H	H	B11	CF3	Me
	tBu	H	H	B12	CF3	Me
	tBu	H	H	B13	CF3	Me
	tBu	H	H	B14	CF3	Me
	tBu	H	H	B15	CF3	Me
	tBu	H	H	B16	CF3	Me
	tBu	H	H	B17	CF3	Me
	tBu	H	H	B18	CF3	Me
	tBu	H	H	B19	CF3	Me
	tBu	H	H	B20	CF3	Me
	tBu	H	H	B21	CF3	Me
	tBu	H	H	B22	CF3	Me
	tBu	H	H	B23	CF3	Me
	tBu	H	H	B24	CF3	Me
	tBu	H	H	B25	CF3	Me
	tBu	H	H	B26	CF3	Me
	tBu	H	H	B27	CF3	Me
	tBu	H	H	B28	CF3	Me
	tBu	H	H	B29	CF3	Me
	tBu	H	H	B30	CF3	Me
	tBu	H	H	B31	CF3	Me
	tBu	H	H	B32	CF3	Me
	tBu	H	H	B33	CF3	Me
	tBu	H	H	B34	CF3	Me
	tBu	H	H	Na	CF3	Me
	tBu	H	H	K	CF3	Me
	2-pyridyl	H	H	H	Me	Me
	2-pyridyl	H	H	H	Et	Me
	2-pyridyl	H	H	H	Cl	Cl
	2-pyridyl	H	H	H	Cl	Me
	2-pyridyl	H	H	H	Cl	CF3
	2-pyridyl	H	H	H	Me	Cl
	2-pyridyl	H	H	H	Br	Me
	2-pyridyl	H	H	H	Me	Br
	2-pyridyl	H	H	H	Me	CF3
	2-pyridyl	H	H	H	OMe	Me
	2-pyridyl	H	H	H	OCF3	Me
	2-pyridyl	H	H	H	SMe	Me
	2-pyridyl	H	H	H	CO2Me	Me
	2-pyridyl	H	H	H	CO2Et	Me
	2-pyridyl	H	H	H	CF3	Me
	2-pyridyl	H	H	H	CF3	H
	2-pyridyl	H	H	B3	CF3	Me
	2-pyridyl	H	H	B6	CF3	Me
	2-pyridyl	H	H	B7	CF3	Me
	3-pyridyl	H	H	H	CF3	Me
	4-pyridyl	H	H	H	CF3	Me
	2-F—Ph	H	H	H	Me	Me
	2-F—Ph	H	H	H	Et	Me
	2-F—Ph	H	H	H	CF3	Me
	2-F—Ph	H	H	H	CF3	Cl
	2-F—Ph	H	H	H	CF3	H
	2-F—Ph	H	H	B3	CF3	Me
	2-F—Ph	H	H	B6	CF3	Me
	2-F—Ph	H	H	B7	CF3	Me
	3-F—Ph	H	H	H	CF3	Me
	4-F—Ph	H	H	H	CF3	Me
	2,3-F2—Ph	H	H	H	CF3	Me
	2,4-F2—Ph	H	H	H	CF3	Me
	2,5-F2—Ph	H	H	H	CF3	Me
	Ph	H	H	H	Me	Me
	Ph	H	H	H	Et	Me
	Ph	H	H	H	CF3	Me
	Ph	H	H	H	CF3	Cl
	Ph	H	H	H	CF3	H
	Ph	H	H	B3	CF3	Me
	Ph	H	H	B6	CF3	Me
	Ph	H	H	B7	CF3	Me
	3,4-F2—Ph	H	H	H	CF3	Me
	3,5-F2—Ph	H	H	H	CF3	Me
	2-Cl—Ph	H	H	H	Me	Me
	2-Cl—Ph	H	H	H	Et	Me
	2-Cl—Ph	H	H	H	CF3	Me
	2-Cl—Ph	H	H	H	CF3	Cl
	2-Cl—Ph	H	H	H	CF3	H
	2-Cl—Ph	H	H	B3	CF3	Me
	2-Cl—Ph	H	H	B6	CF3	Me
	2-Cl—Ph	H	H	B7	CF3	Me
	3-Cl—Ph	H	H	H	CF3	Me
	4-Cl—Ph	H	H	H	CF3	Me
	2,3-Cl2—Ph	H	H	H	CF3	Me
	2,4-Cl2—Ph	H	H	H	CF3	Me
	2,5-Cl2—Ph	H	H	H	CF3	Me
	2,6-Cl2—Ph	H	H	H	Me	Me
	2,6-Cl2—Ph	H	H	H	Et	Me
	2,6-Cl2—Ph	H	H	H	CF3	Me
	2,6-Cl2—Ph	H	H	H	CF3	Cl
	2,6-Cl2—Ph	H	H	H	CF3	H
	2,6-Cl2—Ph	H	H	B3	CF3	Me
	2,6-Cl2—Ph	H	H	B6	CF3	Me
	2,6-Cl2—Ph	H	H	B7	CF3	Me
	3,4-Cl2—Ph	H	H	H	CF3	Me
	3,5-Cl2—Ph	H	H	H	CF3	Me
	2-Me—Ph	H	H	H	CF3	Me
	2,6-Me2—Ph	H	H	H	CF3	Me
	2-MeO—Ph	H	H	H	CF3	Me
	2-CF3O—Ph	H	H	H	CF3	Me
	2-SMe—Ph	H	H	H	CF3	Me
	2-SOMe—Ph	H	H	H	CF3	Me
	2-SO2Me—Ph	H	H	H	CF3	Me
	2-CF3—Ph	H	H	H	CF3	Me
	2-NO2—Ph	H	H	H	CF3	Me
	2-CN—Ph	H	H	H	CF3	Me
	2-NHMe—Ph	H	H	H	CF3	Me
	2-NMe2—Ph	H	H	H	CF3	Me
	4-benzyl-Ph	H	H	H	Et	Me
	4-phenoxy-Ph	H	H	H	CF3	Me
	2-OH—Ph	H	H	H	CF3	Me
	2-CO2Me—Ph	H	H	H	CF3	Me
	2-CO2Et—Ph	H	H	H	CF3	Me
	H	CO2Et	Ph	H	CF3	Me
	Me	Ph	H	H	CF3	Me
	Et	Me	H	H	CF3	Me
	nPr	H	H	H	CF3	Me
	iPr	H	H	H	Et	Me
	iPr	H	H	H	CF3	Me
	nBu	H	H	H	Et	Me
	nBu	H	H	H	CF3	Me
	iBu	H	H	H	Et	Me
	iBu	H	H	H	CF3	Me
	iBu	H	H	B7	Et	Me
	iBu	H	H	B7	CF3	Me
	secBu	H	H	H	Et	Me
	secBu	H	H	H	CF3	Me
	2,2-Me2-propyl	H	H	H	CF3	Me
	nHex	H	H	H	CF3	Me
	ethenyl	H	H	H	CF3	Me
	1-propenyl	H	H	H	CF3	Me
	ethynyl	H	H	H	CF3	Me
	1-propynyl	H	H	H	CF3	Me
	CF3	H	H	H	CF3	Me
	CHF2	H	H	H	CF3	Me
	C2F5	H	H	H	CF3	Me
	2,2-Cl2—cPr	H	H	H	Et	Me
	2,2-Cl2—cPr	H	H	H	CF3	Me
	cPr	H	H	H	Et	Me
	cPr	H	H	H	CF3	Me
	1-Me—cPr	H	H	H	Et	Me
	1-Me—cPr	H	H	H	CF3	Me
	cHex	H	H	H	Et	Me
	cHex	H	H	H	CF3	Me
	CH2Ph	H	H	H	CF3	Me
	naphthyl-1	H	H	H	Et	Me
	naphthyl-1	H	H	H	CF3	Me
	naphthyl-2	H	H	H	CF3	Me
	CO2Me	H	H	H	CF3	Me
	CO2Et	H	H	H	CF3	Me
	2-thienyl	H	H	H	CF3	Me
	CH2OMe	H	H	H	CF3	Me
	CH2OEt	H	H	H	CF3	Me
	COCH3	H	H	H	CF3	Me
	COtBu	H	H	H	CF3	Me
	COPh	H	H	H	CF3	Me

TABLE 4
R1	R2	B	Y1	Y2	Y3
2,6-F2—Ph	H	H	H	CF3	Me
2,6-F2—Ph	H	H	Me	H	Me
2,6-F2—Ph	H	H	Me	H	CF3
2,6-F2—Ph	H	B7	Me	H	H
2,6-F2—Ph	H	H	Me	Me	Me
2,6-F2—Ph	H	H	Me	Cl	Me
2,6-F2—Ph	H	H	Me	Br	Me
2,6-F2—Ph	H	H	Et	Me	Me
2,6-F2—Ph	H	H	Cl	Me	Me
2,6-F2—Ph	H	H	Cl	H	Me
2,6-F2—Ph	H	H	Cl	H	CF3
2,6-F2—Ph	H	H	Cl	H	H
2,6-F2—Ph	H	H	Cl	Cl	Me
2,6-F2—Ph	H	H	Cl	Cl	CF3
2,6-F2—Ph	H	H	Cl	Cl	CF2H
2,6-F2—Ph	H	H	Cl	Cl	CH2OMe
2,6-F2—Ph	H	H	Cl	Cl	COMe
2,6-F2—Ph	H	H	Cl	CF3	Me
2,6-F2—Ph	H	H	Br	Me	Me
2,6-F2—Ph	H	H	Me	OMe	Me
2,6-F2—Ph	H	B7	OMe	H	H
2,6-F2—Ph	H	B7	OCF3	H	H
2,6-F2—Ph	H	B7	SMe	H	H
2,6-F2—Ph	H	H	CF3	Me	Me
2,6-F2—Ph	H	H	CF3	Cl	Me
2,6-F2—Ph	H	H	CF3	Cl	CF3
2,6-F2—Ph	H	H	CF3	Cl	CF2H
2,6-F2—Ph	H	H	CF3	Cl	CH2OMe
2,6-F2—Ph	H	H	CF3	H	Me
2,6-F2—Ph	H	H	CF3	Br	Me
2,6-F2—Ph	H	H	CF3	NO2	Me
2,6-F2—Ph	H	H	CF3	CN	Me
2,6-F2—Ph	H	H	CF3	NHMe	Me
2,6-F2—Ph	H	H	CF3	NMe2	Me
2,6-F2—Ph	H	H	CF3	CO2Me	Me
2,6-F2—Ph	H	H	CF3	OMe	Me
2,6-F2—Ph	H	H	CF3	OCF2H	CF2H
2,6-F2—Ph	H	H	Cl	NO2	Me
2,6-F2—Ph	H	H	Cl	CN	Me
2,6-F2—Ph	H	H	CO2Me	Me	Me
2,6-F2—Ph	H	B1	Cl	Cl	Me
2,6-F2—Ph	H	B3	Cl	Cl	Me
2,6-F2—Ph	H	B6	Cl	Cl	Me
2,6-F2—Ph	H	B7	Cl	Cl	Me
2,6-F2—Ph	H	B2	CF3	Cl	Me
2,6-F2—Ph	H	B3	CF3	Cl	Me
2,6-F2—Ph	H	B4	CF3	Cl	Me
2,6-F2—Ph	H	B5	CF3	Cl	Me
2,6-F2—Ph	H	B6	CF3	Cl	Me
2,6-F2—Ph	H	B7	CF3	Cl	Me
2,6-F2—Ph	H	B8	CF3	Cl	Me
2,6-F2—Ph	H	B9	CF3	Cl	Me
2,6-F2—Ph	H	B10	CF3	Cl	Me
2,6-F2—Ph	H	B11	CF3	Cl	Me
2,6-F2—Ph	H	B12	CF3	Cl	Me
2,6-F2—Ph	H	B13	CF3	Cl	Me
2,6-F2—Ph	H	B14	CF3	Cl	Me
2,6-F2—Ph	H	B15	CF3	Cl	Me
2,6-F2—Ph	H	B16	CF3	Cl	Me
2,6-F2—Ph	H	B17	CF3	Cl	Me
2,6-F2—Ph	H	B18	CF3	Cl	Me
2,6-F2—Ph	H	B19	CF3	Cl	Me
2,6-F2—Ph	H	B20	CF3	Cl	Me
2,6-F2—Ph	H	B21	CF3	Cl	Me
2,6-F2—Ph	H	B22	CF3	Cl	Me
2,6-F2—Ph	H	B23	CF3	Cl	Me
2,6-F2—Ph	H	B24	CF3	Cl	Me
2,6-F2—Ph	H	B25	CF3	Cl	Me
2,6-F2—Ph	H	B26	CF3	Cl	Me
2,6-F2—Ph	H	B27	CF3	Cl	Me
2,6-F2—Ph	H	B28	CF3	Cl	Me
2,6-F2—Ph	H	B29	CF3	Cl	Me
2,6-F2—Ph	H	B30	CF3	Cl	Me
2,6-F2—Ph	H	B31	CF3	Cl	Me
2,6-F2—Ph	H	B32	CF3	Cl	Me
2,6-F2—Ph	H	B33	CF3	Cl	Me
2,6-F2—Ph	H	B34	CF3	Cl	Me
2,6-F2—Ph	H	Na	CF3	Cl	Me
2,6-F2—Ph	H	K	CF3	Cl	Me
2,6-F2—Ph	H	B7	Cl	H	H
2,6-F2—Ph	H	B9	Cl	H	H
2,6-F2—Ph	H	B10	Cl	H	H
2,6-F2—Ph	H	B11	Cl	H	H
tBu	H	H	H	CF3	Me
tBu	H	H	Me	H	Me
tBu	H	H	Me	H	CF3
tBu	H	B7	Me	H	H
tBu	H	H	Me	Me	Me
tBu	H	H	Me	Cl	Me
tBu	H	H	Me	Br	Me
tBu	H	H	Et	Me	Me
tBu	H	H	Cl	Me	Me
tBu	H	H	Cl	H	Me
tBu	H	H	Cl	H	CF3
tBu	H	H	Cl	H	H
tBu	Me	H	Cl	H	H
tBu	Cl	H	Cl	H	H
tBu	H	H	Cl	Cl	Me
tBu	H	H	Cl	Cl	CF3
tBu	H	H	Cl	Cl	CF2H
tBu	H	H	Cl	Cl	CH2OMe
tBu	H	H	Cl	Cl	COMe
tBu	H	H	Cl	CF3	Me
tBu	H	H	Br	Me	Me
tBu	H	H	Me	OMe	Me
tBu	H	B7	OMe	H	H
tBu	H	B7	OCF3	H	H
tBu	H	B7	SMe	H	H
tBu	H	H	CF3	Me	Me
tBu	H	H	CF3	Cl	Me
tBu	Br	H	CF3	Cl	Me
tBu	CF3	H	CF3	Cl	Me
tBu	NO2	H	CF3	Cl	Me
tBu	CN	H	CF3	Cl	Me
tBu	CO2Me	H	CF3	Cl	Me
tBu	CO2Et	H	CF3	Cl	Me
tBu	H	H	CF3	Cl	CF3
tBu	H	H	CF3	Cl	CF2H
tBu	H	H	CF3	Cl	CH2OMe
tBu	H	H	CF3	H	Me
tBu	H	H	CF3	Br	Me
tBu	H	H	CF3	NO2	Me
tBu	H	H	CF3	CN	Me
tBu	H	H	CF3	NHMe	Me
tBu	H	H	CF3	NMe2	Me
tBu	H	H	CF3	CO2Me	Me
tBu	H	H	CF3	OMe	Me
tBu	H	H	CF3	OCF2H	CF2H
tBu	H	H	Cl	NO2	Me
tBu	H	H	Cl	CN	Me
tBu	H	H	CO2Me	Me	Me
tBu	H	B1	Cl	Cl	Me
tBu	H	B2	Cl	Cl	Me
tBu	H	B3	Cl	Cl	Me
tBu	H	B4	Cl	Cl	Me
tBu	H	B5	Cl	Cl	Me
tBu	H	B6	Cl	Cl	Me
tBu	H	B7	Cl	Cl	Me
tBu	H	B8	Cl	Cl	Me
tBu	H	B9	Cl	Cl	Me
tBu	H	B10	Cl	Cl	Me
tBu	H	B11	Cl	Cl	Me
tBu	H	B12	Cl	Cl	Me
tBu	H	B13	Cl	Cl	Me
tBu	H	B14	Cl	Cl	Me
tBu	H	B15	Cl	Cl	Me
tBu	H	B16	Cl	Cl	Me
tBu	H	B17	Cl	Cl	Me
tBu	H	B18	Cl	Cl	Me
tBu	H	B19	Cl	Cl	Me
tBu	H	B20	Cl	Cl	Me
tBu	H	B21	Cl	Cl	Me
tBu	H	B22	Cl	Cl	Me
tBu	H	B23	Cl	Cl	Me
tBu	H	B24	Cl	Cl	Me
tBu	H	B25	Cl	Cl	Me
tBu	H	B26	Cl	Cl	Me
tBu	H	B27	Cl	Cl	Me
tBu	H	B28	Cl	Cl	Me
tBu	H	B29	Cl	Cl	Me
tBu	H	B30	Cl	Cl	Me
tBu	H	B31	Cl	Cl	Me
tBu	H	B32	Cl	Cl	Me
tBu	H	B33	Cl	Cl	Me
tBu	H	B34	Cl	Cl	Me
tBu	H	Na	Cl	Cl	Me
tBu	H	K	Cl	Cl	Me
tBu	H	B2	CF3	Cl	Me
tBu	H	B3	CF3	Cl	Me
tBu	H	B4	CF3	Cl	Me
tBu	H	B5	CF3	Cl	Me
tBu	H	B6	CF3	Cl	Me
tBu	H	B7	CF3	Cl	Me
tBu	H	B8	CF3	Cl	Me
tBu	H	B9	CF3	Cl	Me
tBu	H	B10	CF3	Cl	Me
tBu	H	B11	CF3	Cl	Me
tBu	H	B12	CF3	Cl	Me
tBu	H	B13	CF3	Cl	Me
tBu	H	B14	CF3	Cl	Me
tBu	H	B15	CF3	Cl	Me
tBu	H	B16	CF3	Cl	Me
tBu	H	B17	CF3	Cl	Me
tBu	H	B18	CF3	Cl	Me
tBu	H	B19	CF3	Cl	Me
tBu	H	B20	CF3	Cl	Me
tBu	H	B21	CF3	Cl	Me
tBu	H	B22	CF3	Cl	Me
tBu	H	B23	CF3	Cl	Me
tBu	H	B24	CF3	Cl	Me
tBu	H	B25	CF3	Cl	Me
tBu	H	B26	CF3	Cl	Me
tBu	H	B27	CF3	Cl	Me
tBu	H	B28	CF3	Cl	Me
tBu	H	B29	CF3	Cl	Me
tBu	H	B30	CF3	Cl	Me
tBu	H	B31	CF3	Cl	Me
tBu	H	B32	CF3	Cl	Me
tBu	H	B33	CF3	Cl	Me
tBu	H	B34	CF3	Cl	Me
tBu	H	Na	CF3	Cl	Me
tBu	H	K	CF3	Cl	Me
tBu	H	B7	Cl	H	H
tBu	H	B8	Cl	H	H
tBu	H	B15	Cl	H	H
tBu	H	B34	Cl	H	H
2-pyridyl	H	H	H	CF3	Me
2-pyridyl	H	H	Me	H	Me
2-pyridyl	H	H	Me	H	CF3
2-pyridyl	H	B7	Me	H	H
2-pyridyl	H	H	Me	Me	Me
2-pyridyl	H	H	Me	Cl	Me
2-pyridyl	H	H	Me	Br	Me
2-pyridyl	H	H	Et	Me	Me
2-pyridyl	H	H	Cl	Me	Me
2-pyridyl	H	H	Cl	H	Me
2-pyridyl	H	H	Cl	H	CF3
2-pyridyl	H	H	Cl	H	H
2-pyridyl	Me	H	Cl	H	H
2-pyridyl	Cl	H	Cl	H	H
2-pyridyl	H	H	Cl	Cl	Me
2-pyridyl	H	H	Cl	Cl	CF3
2-pyridyl	H	H	Cl	Cl	CF2H
2-pyridyl	H	H	Cl	Cl	CH2OMe
2-pyridyl	H	H	Cl	Cl	COMe
2-pyridyl	H	H	Cl	CF3	Me
2-pyridyl	H	H	Br	Me	Me
2-pyridyl	H	H	Me	OMe	Me
2-pyridyl	H	H	Br	H	H
2-pyridyl	H	H	OMe	H	H
2-pyridyl	H	B7	OCF3	H	H
2-pyridyl	H	B7	SMe	H	H
2-pyridyl	H	B7	NH2	H	H
2-pyridyl	H	B7	NHMe	H	H
2-pyridyl	H	B7	NMe2	H	H
2-pyridyl	H	B7	NO2	H	H
2-pyridyl	H	B7	CN	H	H
2-pyridyl	H	B7	CO2Me	H	H
2-pyridyl	H	B7	CO2Et	H	H
2-pyridyl	H	H	CF3	Me	Me
2-pyridyl	H	H	CF3	Cl	Me
2-pyridyl	H	H	CF3	H	Me
2-pyridyl	H	H	CF3	Br	Me
2-pyridyl	H	H	CF3	CO2Me	Me
2-pyridyl	H	H	Cl	NO2	Me
2-pyridyl	H	H	Cl	CN	Me
2-pyridyl	H	H	CO2Me	Me	Me
2-pyridyl	H	B3	Cl	Cl	Me
2-pyridyl	H	B6	Cl	Cl	Me
2-pyridyl	H	B7	Cl	Cl	Me
2-pyridyl	H	B3	CF3	Cl	Me
2-pyridyl	H	B6	CF3	Cl	Me
2-pyridyl	H	B7	CF3	Cl	Me
2-pyridyl	H	B2	Cl	H	H
2-pyridyl	H	B3	Cl	H	H
2-pyridyl	H	B4	Cl	H	H
2-pyridyl	H	B5	Cl	H	H
2-pyridyl	H	B6	Cl	H	H
2-pyridyl	H	B7	Cl	H	H
2-pyridyl	H	B8	Cl	H	H
2-pyridyl	H	B9	Cl	H	H
2-pyridyl	H	B10	Cl	H	H
2-pyridyl	H	B11	Cl	H	H
2-pyridyl	H	B12	Cl	H	H
2-pyridyl	H	B13	Cl	H	H
2-pyridyl	H	B14	Cl	H	H
2-pyridyl	H	B15	Cl	H	H
2-pyridyl	H	B16	Cl	H	H
2-pyridyl	H	B17	Cl	H	H
2-pyridyl	H	B18	Cl	H	H
2-pyridyl	H	B19	Cl	H	H
2-pyridyl	H	B20	Cl	H	H
2-pyridyl	H	B21	Cl	H	H
2-pyridyl	H	B22	Cl	H	H
2-pyridyl	H	B23	Cl	H	H
2-pyridyl	H	B24	Cl	H	H
2-pyridyl	H	B25	Cl	H	H
2-pyridyl	H	B26	Cl	H	H
2-pyridyl	H	B27	Cl	H	H
2-pyridyl	H	B28	Cl	H	H
2-pyridyl	H	B29	Cl	H	H
2-pyridyl	H	B30	Cl	H	H
2-pyridyl	H	B31	Cl	H	H
2-pyridyl	H	B32	Cl	H	H
2-pyridyl	H	B33	Cl	H	H
2-pyridyl	H	B34	Cl	H	H
2-pyridyl	H	Na	Cl	H	H
2-pyridyl	H	K	Cl	H	H
3-pyridyl	H	H	Cl	Cl	Me
3-pyridyl	H	H	CF3	Cl	Me
3-pyridyl	H	H	Cl	H	H
4-pyridyl	H	H	Cl	Cl	Me
4-pyridyl	H	H	CF3	Cl	Me
4-pyridyl	H	H	Cl	H	H
2-F—Ph	H	H	Me	Me	Me
2-F—Ph	H	H	Me	Cl	Me
2-F—Ph	H	H	Cl	Me	Me
2-F—Ph	H	H	Cl	H	H
2-F—Ph	H	H	Cl	Cl	Me
2-F—Ph	H	B7	OMe	H	H
2-F—Ph	H	B7	SMe	H	H
2-F—Ph	H	B7	CF3	Cl	Me
2-F—Ph	H	B7	CF3	H	Me
2-F—Ph	H	Bi	Cl	Cl	Me
2-F—Ph	H	B3	Cl	Cl	Me
2-F—Ph	H	B6	Cl	Cl	Me
2-F—Ph	H	B7	Cl	Cl	Me
2-F—Ph	H	B3	CF3	Cl	Me
2-F—Ph	H	B6	CF3	Cl	Me
2-F—Ph	H	B7	CF3	Cl	Me
2-F—Ph	H	B7	Cl	H	H
3-F-Ph	H	H	Cl	Cl	Me
4-F-Ph	H	H	Cl	Cl	Me
2,3-F2—Ph	H	H	Cl	Cl	Me
2,4-F2—Ph	H	H	Cl	Cl	Me
2,5-F2—Ph	H	H	Cl	Cl	Me
Ph	H	H	Me	Me	Me
Ph	H	H	Me	Cl	Me
Ph	H	H	Cl	Me	Me
Ph	H	H	Cl	H	H
Ph	H	H	Cl	Cl	Me
Ph	H	B7	OMe	H	H
Ph	H	B7	SMe	H	H
Ph	H	H	CF3	Cl	Me
Ph	H	H	CF3	H	Me
Ph	H	B1	Cl	Cl	Me
Ph	H	B3	Cl	Cl	Me
Ph	H	B6	Cl	Cl	Me
Ph	H	B7	Cl	Cl	Me
Ph	H	B3	CF3	Cl	Me
Ph	H	B6	CF3	Cl	Me
Ph	H	B7	CF3	Cl	Me
Ph	Me	B7	CF3	Cl	Me
Ph	H	B7	Cl	H	H
3,4-F2—Ph	H	H	Cl	Cl	Me
3,5-F2—Ph	H	H	Cl	Cl	Me
2-Cl-Ph	H	H	Me	Me	Me
2-Cl-Ph	H	H	Me	Cl	Me
2-Cl-Ph	H	H	Cl	Me	Me
2-Cl-Ph	H	H	Cl	H	H
2-Cl-Ph	H	H	Cl	Cl	Me
2-Cl-Ph	H	H	OMe	H	H
2-Cl-Ph	H	H	SMe	H	H
2-Cl-Ph	H	H	CF3	Cl	Me
2-Cl-Ph	H	H	CF3	H	Me
2-Cl-Ph	H	B1	Cl	Cl	Me
2-Cl-Ph	H	B3	Cl	Cl	Me
2-Cl-Ph	H	B6	Cl	Cl	Me
2-Cl-Ph	H	B7	Cl	Cl	Me
2-Cl-Ph	H	B3	CF3	Cl	Me
2-Cl-Ph	H	B6	CF3	Cl	Me
2-Cl-Ph	H	B7	CF3	Cl	Me
2-Cl-Ph	H	B7	Cl	H	H
3-Cl-Ph	H	H	Cl	Cl	Me
4-Cl-Ph	H	H	Cl	Cl	Me
2,3-Cl2—Ph	H	H	Cl	Cl	Me
2,4-Cl2—Ph	H	H	Cl	Cl	Me
2,5-Cl2—Ph	H	H	Cl	Cl	Me
2,6-Cl2—Ph	H	H	Me	Me	Me
2,6-Cl2—Ph	H	H	Me	Cl	Me
2,6-Cl2—Ph	H	H	Cl	Me	Me
2,6-Cl2—Ph	H	H	Cl	H	H
2,6-Cl2—Ph	H	H	Cl	Cl	Me
2,6-Cl2—Ph	H	B7	OMe	H	H
2,6-Cl2—Ph	H	B7	SMe	H	H
2,6-Cl2—Ph	H	H	CF3	Cl	Me
2,6-Cl2—Ph	H	H	CF3	H	Me
2,6-Cl2—Ph	H	B1	Cl	Cl	Me
2,6-Cl2—Ph	H	B3	Cl	Cl	Me
2,6-Cl2—Ph	H	B6	Cl	Cl	Me
2,6-Cl2—Ph	H	B7	Cl	Cl	Me
2,6-C12—Ph	Cl	B7	Cl	Cl	Me
2,6-Cl2—Ph	H	B3	CF3	Cl	Me
2,6-Cl2—Ph	H	B6	CF3	Cl	Me
2,6-Cl2—Ph	H	B7	CF3	Cl	Me
2,6-Cl2—Ph	Cl	B7	CF3	Cl	Me
2,6-Cl2—Ph	H	B7	Cl	H	H
3,4-Cl2—Ph	H	H	Cl	Cl	Me
3,5-Cl2—Ph	H	H	Cl	Cl	Me
2-Me—Ph	H	H	Cl	Cl	Me
2-Me—Ph	H	H	CF3	Cl	Me
2,6-Me2—Ph	H	H	Cl	Cl	Me
2,6-Me2—Ph	H	H	CF3	Cl	Me
2-MeO-Ph	H	H	Ci	Cl	Me
2-MeO-Ph	H	H	CF3	Cl	Me
2-CF3O—Ph	H	H	Cl	Cl	Me
2-CF3O—Ph	H	H	CF3	Cl	Me
2-SMe—Ph	H	H	Cl	Cl	Me
2-SMe—Ph	H	H	CF3	Cl	Me
2-SOMe—Ph	H	H	Cl	Cl	Me
2-SOMe—Ph	H	H	CF3	Cl	Me
2-SO2Me—Ph	H	H	Cl	Cl	Me
2-SO2Me-Ph	H	H	CF3	Cl	Me
2-CF3—Ph	H	H	Cl	Cl	Me
2-CF3—Ph	H	H	CF3	Cl	Me
2-NO2—Ph	H	H	Cl	Cl	Me
2-NO2—Ph	H	H	CF3	Cl	Me
2-CN-Ph	H	H	Cl	Cl	Me
2-CN-Ph	H	H	CF3	Cl	Me
2-NHMe-Ph	H	H	Cl	Cl	Me
2-NMe2—Ph	H	H	Cl	Cl	Me
4-benzyl-Ph	H	H	Cl	Cl	Me
4-phenoxy-Ph	H	H	Cl	Cl	Me
2-OH-Ph	H	H	Cl	Cl	Me
2-CO2Me—Ph	H	H	Cl	Cl	Me
2-CO2Me—Ph	H	H	CF3	Cl	Me
2-CO2Et—Ph	H	H	Cl	Cl	Me
2-CO2Et—Ph	H	H	CF3	Cl	Me
H	H	H	Cl	Cl	Me
Me	H	H	Cl	Cl	Me
Et	H	H	Cl	Cl	Me
nPr	H	H	Cl	Cl	Me
iPr	H	H	Cl	Cl	Me
iPr	H	H	CF3	Cl	Me
nBu	H	H	Cl	Cl	Me
nBu	H	H	CF3	Cl	Me
iBu	H	H	Cl	Cl	Me
iBu	H	H	CF3	Cl	Me
iBu	H	B7	Cl	Cl	Me
iBu	H	B7	CF3	Cl	Me
iBu	H	H	Cl	H	H
secBu	H	H	Cl	Cl	Me
secBu	H	H	CF3	Cl	Me
2,2-Me2-propyl	H	H	Cl	Cl	Me
nHex	H	H	Cl	Cl	Me
ethenyl	H	H	Cl	Cl	Me
1-propenyl	H	H	Cl	Cl	Me
1-propenyl	H	H	CF3	Cl	Me
ethynyl	H	H	Cl	Cl	Me
1-propynyl	H	H	Cl	Cl	Me
CF3	H	H	Cl	Cl	Me
CF3	H	H	CF3	Cl	Me
CHF2	H	H	Cl	Cl	Me
C2F5	H	H	Cl	Cl	Me
2,2-Cl2—cPr	H	H	Cl	Cl	Me
2,2-Cl2—cPr	H	H	CF3	Cl	Me
cPr	H	H	Cl	Cl	Me
cPr	H	H	CF3	Cl	Me
1-Me—cPr	H	H	Cl	Cl	Me
1-Me—cPr	H	H	CF3	Cl	Me
cHex	H	H	Cl	Cl	Me
cHex	H	H	CF3	Cl	Me
CH2Ph	H	H	Cl	Cl	Me
naphthyl-1	H	H	Cl	Cl	Me
naphthyl-l	H	H	CF3	Cl	Me
naphthyl-2	H	H	Cl	Cl	Me
CO2Me	H	H	Cl	Cl	Me
CO2Et	H	H	Cl	Cl	Me
2thienyl	H	H	Cl	Cl	Me
2-thienyl	H	H	CF3	Cl	Me
CH2OMe	H	H	Cl	Cl	Me
CH2OEt	H	H	Cl	Cl	Me
COCH3	H	H	Cl	Cl	Me
COtBu	H	H	Cl	Cl	Me
COPh	H	H	Cl	Cl	Me.

TABLE 5
	R1	R2	B	Y1	Y2
	2,6-F2—Ph	H	H	Me	H
	2,6-F2—Ph	H	H	Me	Me
	2,6-F2—Ph	H	H	Et	Me
	2,6-F2—Ph	Me	H	Et	Me
	2,6-F2—Ph	H	H	Cl	Cl
	2,6-F2—Ph	H	H	Cl	Me
	2,6-F2—Ph	H	H	Cl	CF3
	2,6-F2—Ph	H	H	Me	Cl
	2,6-F2—Ph	H	H	Br	Me
	2,6-F2—Ph	H	H	Me	CF3
	2,6-F2—Ph	H	H	OMe	Me
	2,6-F2—Ph	H	H	OCF3	Me
	2,6-F2—Ph	H	H	SMe	Me
	2,6-F2—Ph	H	H	CO2Me	Me
	2,6-F2—Ph	H	H	CO2Et	Me
	2,6-F2—Ph	H	H	CF3	Me
	2,6-F2—Ph	H	H	CF3	H
	2,6-F2—Ph	H	H	CF3	Br
	2,6-F2—Ph	H	H	CF3	NO2
	2,6-F2—Ph	H	H	CF3	CN
	2,6-F2—Ph	H	H	CF3	NHMe
	2,6-F2—Ph	H	H	CF3	NMe2
	2,6-F2—Ph	H	H	CF3	CO2Me
	2,6-F2—Ph	H	B3	CF3	Me
	2,6-F2—Ph	H	B6	CF3	Me
	2,6-F2—Ph	H	B7	CF3	Me
	tBu	H	H	Me	Me
	tBu	H	H	Et	Me
	tBu	H	H	Cl	Cl
	tHu	H	H	Cl	Me
	tBu	H	H	Me	Cl
	tBu	H	H	Cl	CF3
	tBu	H	H	Br	Me
	tBu	H	H	Me	Br
	tBu	H	H	Me	CF3
	tBu	H	H	OMe	Me
	tHu	H	H	OCF3	Me
	tBu	H	H	SMe	Me
	tBu	H	H	CO2Me	Me
	tBu	H	H	CO2Et	Me
	tBu	H	H	CF3	Me
	tBu	H	H	CF3	H
	tBu	H	H	CF3	Br
	tBu	H	H	CF3	NO2
	tBu	H	B2	CF3	Me
	tHu	H	B3	CF3	Me
	tBu	H	B4	CF3	Me
	tBu	H	B5	CF3	Me
	tBu	H	B6	CF3	Me
	tBu	H	B7	CF3	Me
	tBu	H	B8	CF3	Me
	tBu	H	B9	CF3	Me
	tBu	H	B10	CF3	Me
	tBu	H	B11	CF3	Me
	tBu	H	B14	CF3	Me
	tBu	H	B20	CF3	Me
	tBu	H	B23	CF3	Me
	tBu	H	B24	CF3	Me
	tBu	H	B25	CF3	Me
	tBu	H	B26	CF3	Me
	tBu	H	B28	CF3	Me
	tBu	H	B30	CF3	Me
	tBu	H	B31	CF3	Me
	tBu	H	B32	CF3	Me
	tBu	H	B33	CF3	Me
	tBu	H	B34	CF3	Me
	tBu	H	Na	CF3	Me
	tBu	H	K	CF3	Me
	2-pyridyl	H	H	Me	Me
	2-pyridyl	H	H	Et	Me
	2-pyridyl	H	H	Cl	Cl
	2-pyridyl	H	H	Cl	Me
	2-pyridyl	H	H	Me	Cl
	2-pyridyl	H	H	Br	Me
	2-pyridyl	H	H	Me	CF3
	2-pyridyl	H	H	CO2Me	Me
	2-pyridyl	H	H	CO2Et	Me
	2-pyridyl	H	H	CF3	Me
	2-pyridyl	H	H	CF3	Br
	2-pyridyl	H	H	CF3	NO2
	2-pyridyl	H	H	CF3	CN
	2-pyridyl	H	H	CF3	NMe2
	2-pyridyl	H	B3	CF3	Me
	2-pyridyl	H	B6	CF3	Me
	2-pyridyl	H	B7	CF3	Me
	3-pyridyl	H	H	Et	Me
	3-pyridyl	H	H	CF3	Me
	4-pyridyl	H	H	Et	Me
	4-pyridyl	H	H	CF3	Me
	2-F—Ph	H	H	Me	Me
	2-F—Ph	H	H	Et	Me
	2-F—Ph	H	H	CF3	Me
	2-F—Ph	H	H	CF3	Cl
	2-F—Ph	H	H	CF3	H
	2-F—Ph	H	B3	CF3	Me
	2-F—Ph	H	B6	CF3	Me
	2-F—Ph	H	B7	CF3	Me
	3-F—Ph	H	H	Et	Me
	3-F—Ph	H	H	CF3	Me
	4-F—Ph	H	H	Et	Me
	2,3-F2—Ph	H	H	Et	Me
	2,4-F2—Ph	H	H	Et	Me
	2,5-F2—Ph	H	H	Et	Me
	Ph	H	H	Me	Me
	Ph	H	H	Et	Me
	Ph	H	H	CF3	Me
	Ph	H	H	CF3	Cl
	Ph	H	H	CF3	H
	Ph	H	B3	CF3	Me
	Ph	H	B6	CF3	Me
	Ph	H	B7	CF3	Me
	3,4-F2—Ph	H	H	Et	Me
	3,5-F2—Ph	H	H	Et	Me
	2-Cl—Ph	H	H	Me	Me
	2-Cl—Ph	H	H	Et	Me
	2-Cl—Ph	H	H	CF3	Me
	2-Cl—Ph	H	H	CF3	Cl
	2-Cl—Ph	H	H	CF3	H
	2-Cl—Ph	H	B3	CF3	Me
	2-Cl—Ph	H	B6	CF3	Me
	2-Cl—Ph	H	B7	CF3	Me
	3-Cl—Ph	H	H	CF3	Me
	4-Cl—Ph	H	H	CF3	Me
	2,3-Cl2—Ph	H	H	CF3	Me
	2,4-Cl2—Ph	H	H	CF3	Me
	2,5-Cl2—Ph	H	H	CF3	Me
	2,6-Cl2—Ph	H	H	Me	Me
	2,6-Cl2—Ph	H	H	Et	Me
	2,6-Cl2—Ph	H	H	CF3	Me
	2,6-Cl2—Ph	H	H	CF3	Cl
	2,6-C12—Ph	H	H	CF3	H
	2,6-Cl2—Ph	H	B3	CF3	Me
	2,6-Cl2—Ph	H	B6	CF3	Me
	2,6-Cl2—Ph	H	B7	CF3	Me
	3,4-Cl2—Ph	H	H	CF3	Me
	3,5-Cl2—Ph	H	H	CF3	Me
	2-Me—Ph	H	H	Et	Me
	2-Me—Ph	H	H	CF3	Me
	2,6-Me2—Ph	H	H	Et	Me
	2,6-Me2—Ph	H	H	CF3	Me
	2-MeO—Ph	H	H	Et	Me
	2-MeO—Ph	H	H	CF3	Me
	2-CF3O—Ph	H	H	Et	Me
	2-CF3O—Ph	H	H	CF3	Me
	2-SMe—Ph	H	H	EL	Me
	2-SMe—Ph	H	H	CF3	Me
	2-SOMe—Ph	H	H	Et	Me
	2-SOMe—Ph	H	H	CF3	Me
	2-SO2Me—Ph	H	H	EL	Me
	2-SO2Me—Ph	H	H	CF3	Me
	2-CF3—Ph	H	H	EL	Me
	2-CF3—Ph	H	H	CF3	Me
	2-NO2—Ph	H	H	EL	Me
	2-NO2—Ph	H	H	CF3	Me
	2-CN—Ph	H	H	Et	Me
	2-NHMe—Ph	H	H	CF3	Me
	2-NMe2—Ph	H	H	EL	Me
	2-NMe2—Ph	H	H	CF3	Me
	4-benzyl-Ph	H	H	CF3	Me
	4-phenoxy-Ph	H	H	CF3	Me
	2-OH—Ph	H	H	CF3	Me
	2-CO2Me—Ph	H	H	Et	Me
	2-CO2Me—Ph	H	H	CF3	Me
	2-CO2Et—Ph	H	H	Et	Me
	2-CO2Et—Ph	H	H	CF3	Me
	H	H	H	CF3	Me
	Me	H	H	CF3	Me
	Et	H	H	CF3	Me
	nPr	H	H	CF3	Me
	iPr	H	H	Et	Me
	iPr	H	H	CF3	Me
	nBu	H	H	Et	Me
	nBu	H	H	CF3	Me
	iBu	H	H	Et	Me
	iBu	H	H	CF3	Me
	iBu	H	B7	Et	Me
	iBu	H	B7	CF3	Me
	secBu	H	H	Et	Me
	secBu	H	H	CF3	Me
	2,2-Me2-propyl	H	H	CF3	Me
	nHex	H	H	CF3	Me
	ethenyl	H	H	CF3	Me
	1-propenyl	H	H	Et	Me
	1-propenyl	H	H	CF3	Me
	ethynyl	H	H	CF3	Me
	1-propynyl	H	H	CF3	Me
	CF3	H	H	Et	Me
	CF3	H	H	CF3	Me
	CHF2	H	H	Et	Me
	C2F5	H	H	Et	Me
	2,2-Cl2—cPr	H	H	Et	Me
	2,2-Cl2—cPr	H	H	CF3	Me
	cPr	H	H	Et	Me
	cPr	H	H	CF3	Me
	1-Me—cPr	H	H	Et	Me
	1-Me—cPr	H	H	CF3	Me
	cHex	H	H	Et	Me
	cHex	H	H	CF3	Me
	CH2Ph	H	H	CF3	Me
	1-naphthyl	H	H	Et	Me
	1-naphthyl	H	H	CF3	Me
	2-naphthyl	H	H	CF3	Me
	CO2Me	H	H	CF3	Me
	CO2Et	H	H	CF3	Me
	2-thienyl	H	H	CF3	Me

TABLE 6
or
R1	R2	B	Y1	Y2	Y3
2,6-F2—Ph	H	B7	H	CF3	Me
2,6-F2—Ph	H	B7	Me	H	Me
2,6-F2—Ph	H	B7	Me	H	CF3
2,6-F2—Ph	H	B7	Me	H	H
2,6-F2—Ph	H	B7	Me	Me	Me
2,6-F2—Ph	H	B7	Me	Cl	Me
2,6-F2—Ph	H	B7	Me	Br	Me
2,6-F2—Ph	H	B7	Et	Me	Me
2,6-F2—Ph	H	B7	Cl	Me	Me
2,6-F2—Ph	H	B7	Cl	H	Me
2,6-F2—Ph	H	B7	Cl	H	CF3
2,6-F2—Ph	H	B7	Cl	H	H
2,6-F2—Ph	H	B7	Cl	Cl	CF3
2,6-F2—Ph	H	B7	Cl	Cl	CF2H
2,6-F2—Ph	H	B7	Cl	Cl	CH2OMe
2,6-F2—Ph	H	B7	Cl	Cl	COMe
2,6-F2—Ph	H	B7	Cl	CF3	Me
2,6-F2—Ph	H	B7	Br	Me	Me
2,6-F2—Ph	H	B7	Me	OMe	Me
2,6-F2—Ph	H	B7	OMe	H	H
2,6-F2—Ph	H	B7	OCF3	H	H
2,6-F2—Ph	H	B7	SMe	H	H
2,6-F2—Ph	H	B7	CF3	Me	Me
2,6-F2—Ph	H	B7	CF3	Cl	CF3
2,6-F2—Ph	H	B7	CF3	Cl	CF2H
2,6-F2—Ph	H	B7	CF3	Cl	CH2OMe
2,6-F2—Ph	H	B7	CF3	H	Me
2,6-F2—Ph	H	B7	CF3	Br	Me
2,6-F2—Ph	H	B7	CF3	NO2	Me
2,6-F2—Ph	H	B7	CF3	CN	Me
2,6-F2—Ph	H	B7	CF3	NHMe	Me
2,6-F2—Ph	H	B7	CF3	NMe2	Me
2,6-F2—Ph	H	B7	CF3	CO2Me	Me
2,6-F2—Ph	H	B7	CF3	OMe	Me
2,6-F2—Ph	H	B7	CF3	OCF2H	CF2H
2,6-F2—Ph	H	B7	Cl	NO2	Me
2,6-F2—Ph	H	B7	Cl	CN	Me
2,6-F2—Ph	H	B7	CO2Me	Me	Me
2,6-F2—Ph	H	B1	Cl	Cl	Me
2,6-F2—Ph	Me	B1	Cl	Cl	Me
2,6-F2—Ph	H	B3	Cl	Cl	Me
2,6-F2—Ph	H	B4	Cl	Cl	Me
2,6-F2—Ph	H	B5	Cl	Cl	Me
2,6-F2—Ph	H	B6	Cl	Cl	Me
2,6-F2—Ph	H	B7	Cl	Cl	Me
2,6-F2—Ph	Me	B7	Cl	Cl	Me
2,6-F2—Ph	H	B2	CF3	Cl	Me
2,6-F2—Ph	H	B3	CF3	Cl	Me
2,6-F2—Ph	H	B4	CF3	Cl	Me
2,6-F2—Ph	H	B5	CF3	Cl	Me
2,6-F2—Ph	H	B6	CF3	Cl	Me
2,6-F2—Ph	H	B7	CF3	Cl	Me
2,6-F2—Ph	Me	B7	CF3	Cl	Me
2,6-F2—Ph	H	B8	CF3	Cl	Me
2,6-F2—Ph	H	B9	CF3	Cl	Me
2,6-F2—Ph	H	B10	CF3	Cl	Me
2,6-F2—Ph	H	B11	CF3	Cl	Me
2,6-F2—Ph	H	B12	CF3	Cl	Me
2,6-F2—Ph	H	B13	CF3	Cl	Me
2,6-F2—Ph	H	B14	CF3	Cl	Me
2,6-F2—Ph	H	B15	CF3	Cl	Me
2,6-F2—Ph	H	B16	CF3	Cl	Me
2,6-F2—Ph	H	B17	CF3	Cl	Me
2,6-F2—Ph	H	B18	CF3	Cl	Me
2,6-F2—Ph	H	B19	CF3	Cl	Me
2,6-F2—Ph	H	B20	CF3	Cl	Me
2,6-F2—Ph	H	B21	CF3	Cl	Me
2,6-F2—Ph	H	B22	CF3	Cl	Me
2,6-F2—Ph	H	B23	CF3	Cl	Me
2,6-F2—Ph	H	B24	CF3	Cl	Me
2,6-F2—Ph	H	B25	CF3	Cl	Me
2,6-F2—Ph	H	B26	CF3	Cl	Me
2,6-F2—Ph	H	B27	CF3	Cl	Me
2,6-F2—Ph	H	B28	CF3	Cl	Me
2,6-F2—Ph	H	B29	CF3	Cl	Me
2,6-F2—Ph	H	B30	CF3	Cl	Me
2,6-F2—Ph	H	B31	CF3	Cl	Me
2,6-F2—Ph	H	B32	CF3	Cl	Me
2,6-F2—Ph	H	B33	CF3	Cl	Me
2,6-F2—Ph	H	B34	CF3	Cl	Me
2,6-F2—Ph	H	B7	Cl	H	H
2,6-F2—Ph	H	B9	Cl	H	H
2,6-F2—Ph	H	B10	Cl	H	H
2,6-F2—Ph	H	B11	Cl	H	H
2,6-F2—Ph	H	B45	CF3	Cl	Me
2,6-F2—Ph	H	B46	CF3	Cl	Me
tBu	H	B7	H	CF3	Me
tBu	H	B7	Me	H	Me
tBu	H	B7	Me	H	CF3
tBu	H	B7	Me	H	H
tHu	H	B7	Me	Me	Me
tBu	H	B7	Me	Cl	Me
tBu	H	B7	Me	Br	Me
tBu	H	B7	Et	Me	Me
tBu	H	B7	Cl	Me	Me
tBu	H	B7	Cl	H	Me
tBu	H	B7	Cl	H	CF3
tBu	H	B7	Cl	H	H
tBu	H	B7	Cl	Cl	CF3
tBu	H	B7	Cl	Cl	CF2H
tBu	H	B7	Cl	Cl	CH2OMe
tBu	H	B7	Cl	Cl	COMe
tBu	H	B7	Cl	CF3	Me
tBu	H	B7	Br	Me	Me
tBu	H	B7	Me	OMe	Me
tBu	H	B7	OMe	H	H
tBu	H	B7	OCF3	H	H
tBu	H	B7	SMe	H	H
tBu	H	B7	CF3	Me	Me
tBu	Br	B7	CF3	Cl	Me
tBu	Me	B7	CF3	Cl	Me
tBu	CF3	B7	CF3	Cl	Me
tBu	NO2	B7	CF3	Cl	Me
tBu	CN	B7	CF3	Cl	Me
tBu	CO2Me	B7	CF3	Cl	Me
tBu	CO2Et	B7	CF3	Cl	Me
tBu	H	B7	CF3	Cl	CF3
tBu	H	B7	CF3	Cl	CF2H
tBu	H	B7	CF3	Cl	CH2OMe
tBu	H	B7	CF3	H	Me
tBu	H	B7	CF3	Br	Me
tBu	H	B7	CF3	NO2	Me
tBu	H	B7	CF3	CN	Me
tBu	H	B7	CF3	NHMe	Me
tBu	H	B7	CF3	NMe2	Me
tBu	H	B7	CF3	CO2Me	Me
tBu	H	B7	CF3	OMe	Me
tBu	H	B7	CF3	OCF2H	CF2H
tBu	H	B7	Cl	NO2	Me
tBu	H	B7	Cl	CN	Me
tBu	H	B7	CO2Me	Me	Me
tBu	H	B1	Cl	Cl	Me
tBu	H	B2	Cl	Cl	Me
tBu	H	B3	Cl	Cl	Me
tBu	H	B4	Cl	Cl	Me
tBu	H	B5	Cl	Cl	Me
tBu	H	B6	Cl	Cl	Me
tBu	H	B7	Cl	Cl	Me
tBu	Me	B7	Cl	Cl	Me
tBu	H	B8	Cl	Cl	Me
tBu	H	B9	Cl	Cl	Me
tBu	H	B10	Cl	Cl	Me
tBu	H	B11	Cl	Cl	Me
tBu	H	B12	Cl	Cl	Me
tBu	H	B13	Cl	Cl	Me
tBu	H	B14	Cl	Cl	Me
tBu	H	B15	Cl	Cl	Me
tBu	H	B16	Cl	Cl	Me
tBu	H	B17	Cl	Cl	Me
tBu	H	B18	Cl	Cl	Me
tBu	H	B19	Cl	Cl	Me
tBu	H	B20	Cl	Cl	Me
tBu	H	B21	Cl	Cl	Me
tBu	H	B22	Cl	Cl	Me
tBu	H	B23	Cl	Cl	Me
tBu	H	B24	Cl	Cl	Me
tBu	H	B25	Cl	Cl	Me
tBu	H	B26	Cl	Cl	Me
tBu	H	B27	Cl	Cl	Me
tBu	H	B28	Cl	Cl	Me
tBu	H	B29	Cl	Cl	Me
tBu	H	B30	Cl	Cl	Me
tBu	H	B31	Cl	Cl	Me
tBu	H	B32	Cl	Cl	Me
tBu	H	B33	Cl	Cl	Me
tBu	H	B34	Cl	Cl	Me
tBu	H	B45	Cl	Cl	Me
tBu	H	B46	Cl	Cl	Me
tBu	H	B2	CF3	Cl	Me
tBu	H	B3	CF3	Cl	Me
tBu	H	B4	CF3	Cl	Me
tBu	H	B5	CF3	Cl	Me
tBu	H	B6	CF3	Cl	Me
tBu	H	B7	CF3	Cl	Me
tBu	H	B8	CF3	Cl	Me
tBu	H	B9	CF3	Cl	Me
tBu	H	B10	CF3	Cl	Me
tBu	H	B11	CF3	Cl	Me
tBu	H	B12	CF3	Cl	Me
tBu	H	B13	CF3	Cl	Me
tBu	H	B14	CF3	Cl	Me
tBu	H	B15	CF3	Cl	Me
tBu	H	B16	CF3	Cl	Me
tBu	H	B17	CF3	Cl	Me
tBu	H	B18	CF3	Cl	Me
tBu	H	B19	CF3	Cl	Me
tBu	H	B20	CF3	Cl	Me
tBu	H	B21	CF3	Cl	Me
tBu	H	B22	CF3	Cl	Me
tBu	H	B23	CF3	Cl	Me
tBu	H	B24	CF3	Cl	Me
tBu	H	B25	CF3	Cl	Me
tBu	H	B26	CF3	Cl	Me
tBu	H	B27	CF3	Cl	Me
tBu	H	B28	CF3	Cl	Me
tBu	H	B29	CF3	Cl	Me
tBu	H	B30	CF3	Cl	Me
tBu	H	B31	CF3	Cl	Me
tBu	H	B32	CF3	Cl	Me
tBu	H	B33	CF3	Cl	Me
tBu	H	B34	CF3	Cl	Me
tBu	H	B35	CF3	Cl	Me
tBu	H	B43	CF3	Cl	Me
tBu	H	B7	Cl	H	H
tBu	H	B9	Cl	H	H
tBu	H	B10	Cl	H	H
tBu	H	B11	Cl	H	H
2-pyridyl	H	B7	H	CF3	Me
2-pyridyl	H	B7	Me	H	Me
2-pyridyl	H	B7	Me	H	CF3
2-pyridyl	H	B7	Me	H	H
2-pyridyl	H	B7	Me	Me	Me
2-pyridyl	H	B7	Me	Cl	Me
2-pyridyl	H	B7	Cl	H	Me
2-pyridyl	H	B7	Cl	H	CF3
2-pyridyl	H	B7	OMe	H	H
2-pyridyl	H	B7	OCF3	H	H
2-pyridyl	H	B7	SMe	H	H
2-pyridyl	H	B7	NO2	H	H
2-pyridyl	H	B7	CO2Me	H	H
2-pyridyl	H	B7	CO2Et	H	H
2-pyridyl	H	B7	CF3	Me	Me
2-pyridyl	H	B7	CF3	H	Me
2-pyridyl	H	B7	CF3	Br	Me
2-pyridyl	H	B3	Cl	Cl	Me
2-pyridyl	H	B7	Cl	Cl	Me
2-pyridyl	H	B3	CF3	Cl	Me
2-pyridyl	H	B7	CF3	Cl	Me
2-pyridyl	H	B3	Cl	H	H
2-pyridyl	H	B4	Cl	H	H
2-pyridyl	H	B5	Cl	H	H
2-pyridyl	H	B6	Cl	H	H
2-pyridyl	H	B7	Cl	H	H
2-pyridyl	H	B8	Cl	H	H
2-pyridyl	H	B9	Cl	H	H
2-pyridyl	H	B10	Cl	H	H
2-pyridyl	H	B11	Cl	H	H
2-pyridyl	H	B20	Cl	H	H
2-pyridyl	H	B24	Cl	H	H
2-pyridyl	H	B25	Cl	H	H
2-pyridyl	H	B26	Cl	H	H
2-pyridyl	H	B28	Cl	H	H
2-pyridyl	H	B30	Cl	H	H
2-pyridyl	H	B31	Cl	H	H
2-pyridyl	H	B32	Cl	H	H
2-pyridyl	H	B33	Cl	H	H
2-pyridyl	H	B43	Cl	H	H
2-pyridyl	H	B46	Cl	H	H
3-pyridyl	H	B7	Cl	Cl	Me
3-pyridyl	H	B7	Cl	H	H
4-pyridyl	H	B7	Cl	Cl	Me
4 -pyridyl	H	B7	Cl	H	H
2-F—Ph	H	B7	Me	Me	Me
2-F—Ph	H	B7	Me	Cl	Me
2-F—Ph	H	B7	Cl	Me	Me
2-F—Ph	H	B7	Cl	H	H
2-F—Ph	H	B7	OMe	H	H
2-F—Ph	H	B7	SMe	H	H
2-F—Ph	H	B7	CF3	H	Me
2-F—Ph	H	B1	Cl	Cl	Me
2-F—Ph	H	B3	Cl	Cl	Me
2-F—Ph	H	B6	Cl	Cl	Me
2-F—Ph	H	B7	Cl	Cl	Me
2-F—Ph	H	B3	CF3	Cl	Me
2-F—Ph	H	B6	CF3	Cl	Me
2-F—Ph	H	B7	CF3	Cl	Me
2-F—Ph	H	B7	Cl	H	H
3-F—Ph	H	B7	Cl	Cl	Me
4-F—Ph	H	B7	Cl	Cl	Me
2,3-F2—Ph	H	B7	CF3	Cl	Me
2,4-F2—Ph	H	B7	Cl	Cl	Me
2,5-F2—Ph	H	B7	Cl	Cl	Me
Ph	H	B7	Me	Me	Me
Ph	H	B7	Me	Cl	Me
Ph	H	B7	Cl	Me	Me
Ph	H	B7	Cl	H	H
Ph	H	B7	OMe	H	H
Ph	H	B7	SMe	H	H
Ph	H	B7	CF3	H	Me
Ph	H	B1	Cl	Cl	Me
Ph	H	B3	Cl	Cl	Me
Ph	H	B6	Cl	Cl	Me
Ph	H	B7	Cl	Cl	Me
Ph	H	B3	CF3	Cl	Me
Ph	H	B6	CF3	Cl	Me
Ph	H	B7	CF3	Cl	Me
Ph	Me	B7	CF3	Cl	Me
Ph	H	B7	Cl	H	H
3,4-F2—Ph	H	B7	Cl	Cl	Me
3,5-F2—Ph	H	B7	Cl	Cl	Me
2-Cl—Ph	H	B7	Me	Me	Me
2-Cl—Ph	H	B7	Me	Cl	Me
2-Cl—Ph	H	B7	Cl	Me	Me
2-Cl—Ph	H	B7	Cl	H	H
2-Cl—Ph	H	B7	OMe	H	H
2-Cl—Ph	H	B7	SMe	H	H
2-Cl—Ph	H	B7	CF3	H	Me
2-Cl—Ph	H	B6	Cl	Cl	Me
2-Cl—Ph	H	B7	Cl	Cl	Me
2-Cl—Ph	H	B3	CF3	Cl	Me
2-Cl—Ph	H	B6	CF3	Cl	Me
2-Cl—Ph	H	B7	CF3	Cl	Me
2-Cl—Ph	H	B7	Cl	H	H
3-Cl—Ph	H	B7	Cl	Cl	Me
4-Cl—Ph	H	B7	Cl	Cl	Me
2,3-Cl2—Ph	H	B7	Cl	Cl	Me
2,4-Cl2—Ph	H	B7	Cl	Cl	Me
2,5-Cl2—Ph	H	B7	Cl	Cl	Me
2,6-Cl2—Ph	H	B7	Me	Me	Me
2,6-Cl2—Ph	H	B7	Me	Cl	Me
2,6-Cl2—Ph	H	B7	Cl	Me	Me
2,6-Cl2—Ph	H	B7	Cl	H	H
2,6-Cl2—Ph	H	B7	OMe	H	H
2,6-Cl2—Ph	H	B7	SMe	H	H
2,6-Cl2—Ph	H	B7	CF3	H	Me
2,6-Cl2—Ph	H	B1	Cl	Cl	Me
2,6-Cl2—Ph	H	B3	Cl	Cl	Me
2,6-Cl2—Ph	H	B6	Cl	Cl	Me
2,6-Cl2—Ph	H	B7	Cl	Cl	Me
2,6-Cl2—Ph	Me	B7	Cl	Cl	Me
2,6-Cl2—Ph	H	B3	CF3	Cl	Me
2,6-Cl2—Ph	H	B6	CF3	Cl	Me
2,6-Cl2—Ph	H	B7	CF3	Cl	Me
2,6-Cl2—Ph	Me	B7	CF3	Cl	Me
3,4-Cl2—Ph	H	B7	Cl	Cl	Me
3,5-Cl2—Ph	H	B7	Cl	Cl	Me
2-Me—Ph	H	B7	Cl	Cl	Me
2-Me—Ph	H	B7	CF3	Cl	Me
2,6-Me2—Ph	H	B7	Cl	Cl	Me
2,6-Me2—Ph	H	B7	CF3	Cl	Me
2-MeO—Ph	H	B7	Cl	Cl	Me
2-MeO—Ph	H	B7	CF3	Cl	Me
2-CF3O—Ph	H	B7	Cl	Cl	Me
2-CF3O—Ph	H	B7	CF3	Cl	Me
2-SMe—Ph	H	B7	Cl	Cl	Me
2-SOMe—Ph	H	B7	Cl	Cl	Me
2-SO2Me—Ph	H	B7	Cl	Cl	Me
2-CF3—Ph	H	B7	Cl	Cl	Me
2-NO2—Ph	H	B7	Cl	Cl	Me
2-NO2—Ph	H	B9	Cl	Cl	Me
2-CN—Ph	H	B7	Cl	Cl	Me
2-NHMe—Ph	H	B7	Cl	Cl	Me
2-NMe2—Ph	H	B7	Cl	Cl	Me
4-benzyl-Ph	H	B7	Cl	Cl	Me
4-phenoxy-Ph	H	B7	Cl	Cl	Me
4-tBu—Ph	H	B1	Cl	H	Me
2-OH—Ph	H	B7	Cl	Cl	Me
2-CO2Me—Ph	H	B7	Cl	Cl	Me
2-CO2Et—Ph	H	B7	Cl	Cl	Me
H	H	B7	Cl	Cl	Me
Me	H	B7	Cl	Cl	Me
Et	H	B7	Cl	Cl	Me
nPr	H	B7	Cl	Cl	Me
iPr	H	B7	Cl	Cl	Me
iPr	H	B7	CF3	Cl	Me
nBu	H	B7	Cl	Cl	Me
nBu	H	B7	CF3	Cl	Me
iBu	H	B7	Cl	Cl	Me
iBu	H	B7	CF3	Cl	Me
iBu	Me	B7	Cl	Cl	Me
iBu	Me	B7	CF3	Cl	Me
iBu	H	B7	Cl	H	H
secBu	H	B7	Cl	Cl	Me
secBu	H	B7	CF3	Cl	Me
pentyl-2	H	B1	Cl	Cl	Me
2,2-Me2-propyl	H	B7	Cl	Cl	Me
nHex	H	B7	Cl	Cl	Me
ethenyl	H	B7	Cl	Cl	Me
1-propenyl	H	B7	Cl	Cl	Me
1-propenyl	H	B7	CF3	Cl	Me
ethynyl	H	B7	Cl	Cl	Me
1-propynyl	H	B7	Cl	Cl	Me
CF3	H	B7	Cl	Cl	Me
CHF2	H	B7	Cl	Cl	Me
C2F5	H	B7	Cl	Cl	Me
2,2-Cl2—cPr	H	B7	Cl	Cl	Me
2,2-Cl2—cPr	H	B7	CF3	Cl	Me
cPr	H	B7	Cl	Cl	Me
cPr	H	B7	CF3	Cl	Me
1-Me—cPr	H	B7	Cl	Cl	Me
1-Me—cPr	H	B7	CF3	Cl	Me
cHex	H	B7	Cl	Cl	Me
cHex	H	B7	CF3	Cl	Me
CH2Ph	H	B7	Cl	Cl	Me
naphthyl-1	H	B7	Cl	Cl	Me
naphthyl-1	H	B7	CF3	Cl	Me
naphthyl-2	H	B9	Cl	H	H
naphthyl-2	H	B7	Cl	Cl	Me
CO2Me	H	B7	Cl	Cl	Me
CO2Et	H	B7	Cl	Cl	Me
2-thienyl	H	B7	Cl	Cl	Me
2-thienyl	H	B7	CF3	Cl	Me
CH2OMe	H	B7	Cl	Cl	Me
CH2OEt	H	B7	Cl	Cl	Me
COCH3	H	B7	Cl	Cl	Me
COtBu	H	B7	Cl	Cl	Me
COPh	H	B7	Cl	Cl	Me

TABLE 7
or
	R1	R2	B	Y1	Y2
	Ph	H	B7	Me	H
	Ph	H	B7	Me	Me
	Ph	H	B7	Et	Me
	Ph	Me	B7	Et	Me
	Ph	H	B7	Me	Cl
	Ph	H	B7	Cl	Me
	Ph	H	B7	Br	Me
	Ph	H	B7	Me	Br
	Ph	H	B7	Me	CF3
	Ph	H	B7	CF3	H
	Ph	H	B7	CF3	Br
	Ph	H	B7	CF3	NO2
	Ph	H	B7	CF3	CN
	Ph	H	B4	CF3	Me
	Ph	H	B7	CF3	Me
	Ph	H	B9	CF3	Me
	tBu	H	B7	Me	Me
	tBu	H	B7	Et	Me
	tBu	H	B7	Cl	Cl
	tBu	H	B7	Cl	Me
	tBu	H	B7	Me	Cl
	tBu	H	B7	Cl	CF3
	tBu	H	B7	Br	Me
	tBu	H	B7	Me	Br
	tBu	H	B7	Me	CF3
	tBu	H	B7	CF3	Me
	tBu	H	B7	CF3	H
	tBu	H	B7	CF3	Br
	tBu	H	B7	CF3	NO2
	tBu	H	B7	CF3	CN
	tBu	H	B4	CF3	Me
	tBu	H	B5	CF3	Me
	tBu	H	B6	CF3	Me
	tBu	H	B7	CF3	Me
	tBu	H	B9	CF3	Me
	tBu	H	B20	CF3	Me
	tBu	H	B24	CF3	Me
	tBu	H	B25	CF3	Me
	tBu	H	B26	CF3	Me
	2-pyridyl	H	B7	Me	Me
	2-pyridyl	H	B7	Et	Me
	2-pyridyl	H	B7	Cl	Cl
	2-pyridyl	H	B7	Cl	Me
	2-pyridyl	H	B7	Cl	CF3
	2-pyridyl	H	B7	Me	Cl
	2-pyridyl	H	B7	Br	Me
	2-thienyl	H	B7	Me	CF3
	2-pyridyl	H	B7	CF3	H
	2-pyridyl	H	B7	CF3	Br
	2-pyridyl	H	B7	CF3	Me
	3-pyridyl	H	B7	Et	Me
	4-pyridyl	H	B7	CF3	Me
	2-F—Ph	H	B7	Me	Me
	2-F—Ph	H	B7	Et	Me
	2-F—Ph	H	B7	CF3	Cl
	2-F—Ph	H	B7	CF3	H
	2-F—Ph	H	B4	CF3	Me
	2-F—Ph	H	B7	CF3	Me
	2-F—Ph	H	B9	CF3	Me
	3-F—Ph	H	B7	Et	Me
	4-F—Ph	H	B7	Et	Me
	2,3-F2—Ph	H	B7	Et	Me
	2,4-F2—Ph	H	B7	Et	Me
	2,5-F2—Ph	H	B7	Et	Me
	2,6-F2—Ph	H	B7	Me	Me
	2,6-F2—Ph	H	B7	Et	Me
	2,6-F2—Ph	H	B7	CF3	Cl
	2,6-F2—Ph	H	B7	CF3	H
	2,6-F2—Ph	H	B4	CF3	Me
	2,6-F2—Ph	H	B7	CF3	Me
	2,6-F2—Ph	H	B9	CF3	Me
	3,4-F2—Ph	H	B7	Et	Me
	3,5-F2—Ph	H	B7	Et	Me
	2-Cl—Ph	H	B7	Me	Me
	2-Cl—Ph	H	B7	Et	Me
	2-Cl—Ph	H	B7	CF3	Cl
	2-Cl—Ph	H	B7	CF3	H
	2-Cl—Ph	H	B4	CF3	Me
	2-Cl—Ph	H	B7	CF3	Me
	2-Cl—Ph	H	B9	CF3	Me
	3-Cl—Ph	H	B7	CF3	Me
	4-Cl—Ph	H	B7	CF3	Me
	2,3-Cl2—Ph	H	B7	CF3	Me
	2,4-Cl2—Ph	H	B7	CF3	Me
	2,5-Cl2—Ph	H	B7	CF3	Me
	2,6-Cl2—Ph	H	B7	Me	Me
	2,6-Cl2—Ph	H	B7	Et	Me
	2,6-Cl2—Ph	H	B7	CF3	Cl
	2,6-Cl2—Ph	H	B7	CF3	H
	2,6-Cl2—Ph	H	B4	CF3	Me
	2,6-Cl2—Ph	H	B7	CF3	Me
	2,6-Cl2—Ph	H	B9	CF3	Me
	3,4-Cl2—Ph	H	B7	CF3	Me
	3,5-Cl2—Ph	H	B7	CF3	Me
	2-Me—Ph	H	B7	Et	Me
	2-Me—Ph	H	B7	CF3	Me
	2,6-Me2—Ph	H	B7	Et	Me
	2,6-Me2—Ph	H	B7	CF3	Me
	2-MeO—Ph	H	B7	Et	Me
	2-MeO—Ph	H	B7	CF3	Me
	2-CF3O—Ph	H	B7	CF3	Me
	2-SMe—Ph	H	B7	CF3	Me
	2-SOMe—Ph	H	B7	CF3	Me
	2-SO2Me—Ph	H	B7	CF3	Me
	2-CF3—Ph	H	B7	CF3	Me
	2-NO2—Ph	H	B7	CF3	Me
	2-CN—Ph	H	B7	CF3	Me
	2-NMe2—Ph	H	B7	CF3	Me
	4-benzyl-Ph	H	B7	CF3	Me
	4-phenoxy-Ph	H	B7	CF3	Me
	2-OH—Ph	H	B7	CF3	Me
	2-CO2Me—Ph	H	B7	Et	Me
	2-CO2Me—Ph	H	B7	CF3	Me
	2-CO2Et—Ph	H	B7	Et	Me
	2-CO2Et—Ph	H	B7	CF3	Me
	H	H	B7	CF3	Me
	Me	H	B7	CF3	Me
	Et	H	B7	CF3	Me
	nPr	H	B7	CF3	Me
	iPr	H	B7	Et	Me
	iPr	H	B7	CF3	Me
	nBu	H	B7	Et	Me
	nBu	H	B7	CF3	Me
	iBu	H	B7	Et	Me
	iBu	H	B7	CF3	Me
	secBu	H	B7	Et	Me
	secBu	H	B7	CF3	Me
	2,2-Me2-propyl	H	B7	CF3	Me
	nHex	H	B7	CF3	Me
	ethenyl	H	B7	CF3	Me
	1-propenyl	H	B7	Et	Me
	1-propenyl	H	B7	CF3	Me
	ethynyl	H	B7	CF3	Me
	1-propynyl	H	B7	CF3	Me
	CF3	H	B7	Et	Me
	CHF2	H	B7	CF3	Me
	C2F5	H	B7	CF3	Me
	2,2-Cl2—cPr	H	B7	Et	Me
	2,2-Cl2—cPr	H	B7	CF3	Me
	cPr	H	B7	Et	Me
	cPr	H	B7	CF3	Me
	1-Me—cPr	H	B7	Et	Me
	1-Me—cPr	H	B7	CF3	Me
	cHex	H	B7	Et	Me
	cHex	H	B7	CF3	Me
	CH2Ph	H	B7	CF3	Me
	naphthyl-1	H	B7	Et	Me
	naphthyl-1	H	B7	CF3	Me
	naphthyl-2	H	B7	CF3	Me
	CO2Me	H	B7	CF3	Me
	CO2Et	H	B7	CF3	Me
	2-thienyl	H	B7	CF3	Me

TABLE 8
R1	R2	B	W
2-F—Ph	H	H	2-F
2,6-F2—Ph	H	CO(2,4-Me2—Ph)	2-F
tBu	H	H	2-F
tBu	H	B7	2-F
tBuCH2	H	B6	2-F
EtMe2C	H	B30	2-F
cHex	H	B31	2-Cl
1-Me-cHex	H	B32	2-Br
Ph	H	B33	2-F
2-F—Ph	H	B34	2-F
2-Cl	H	H	2-Me
2-Cl—Ph	H	CO2iPr	2-nBu
2,6-F2—Ph	H	CO(2-MeO—Ph)	2-OMe
2,6-Cl2—Ph	H	H	2-nBeO
1-naphthyl	Cl	CO(4-MeO—Ph)	2-CF3
2-naphthyl	Me	CO(2-Me—Ph)	2-OCHF2
tBu	H	Na	2-CF3
tBu	H	Ca	2-OCH2CH2CHFCHF2
2-pyridyl	H	H	2-OCF2CHF2
3-Pyridyl	H	H	2-SMe
4-pyridyl	H	B7	2-SOMe
Me2C═N-	H	B10	2-SO2Me
iPr	H	B13	2-SCBrF2
tBu	H	B19	2-SCF3
tBuCH2	H	B22	2-SOCBrF2
EtMe2C	H	B23	2-SO2CH2F
cHex	H	B7	2-SCF3
Ph	H	B25	2-SCBrF2
2-F-Ph	H	B26	2-SO2CHF2
2-F-Ph	H	B27	2-SCBrF2
2-CF3—Ph	H	B28	2-CH═CCl2
2,6-F2—Ph	H	CO(2,6-Me2—Ph)	2-OCH2CH═CH2
1-naphthyl	H	CO(2,6-(MeO)2—Ph)	2-OCH2CH═CCl2
PhCH2	H	CO(2-Me-6-N02—Ph)	2-OCH2CH═CHCl
2-thienyl	H	CO(3,4,5(MeO)3—Ph)	2-SCH2CH═CHMe
4-Cl-2-thienyl	H	SO2(4-Me—Ph)	2-SOCH2CH═CH2
3-MeO-2-pyridyl	H	CO(2,6-Cl2—Ph)	2-SO2CHMeCH═CH2
2-Cl-3-pyridyl	H	CO(2,5-Me2—Ph)	2-SCH2CMe═CF2
2,6-Cl2-4-pyridyl	H	CO(2,6-F2—Ph)	2-SOCH2CF═CF2
EtMeC═N—	H	B1	2-SO2CH2CH═CF2
Et	H	B2	2-CCH
tBu	H	B4	2-CCI
tBuCH2	H	H	2-OCH2CCH
EtMe2C	H	H	2-OCH2CCCl
cHex	H	H	2-SCH2CCMe
Ph	H	H	2-SOCH2CCH
2-MeO-Ph	H	B5	2-SO2CH2CCMe
2-F-Ph	H	B6	2-SCH2CCBr
2,6-F2—Ph	H	B7	2-SOCHMeCCCl
2,6-Me2—Ph	H	B8	2-SO2CH2CCI
1-naphthyl	H	Ba	2-NO2
PhCH2	H	K	2-CN
2-naphthyl	H	H	2-CO2Me
5-Br-3-thieflyl	H	B3	2-COMe
3-MeO-2-pyridyl	H	B14	2-O(CO)Me
2-Cl-3-pyridyl	H	B15	2-NHMe
2,6-Cl2-4-pyridyl	H	B16	2-NMe2
(CH2)4C═N—	H	B17	3-F
tBu	H	H	3-Cl
tBuCH2	H	H	3-nBu
EtMe2C	H	H	3-OEt
2-Me-cHex	H	H	3-CH2CH2CH2CHF2
Ph	H	B22	3-OCH2CH2CHFCHF2
Ph	H	B27	3-S-nBu
2-CF3—Ph	H	B28	3-SOnPr
2,6-F2—Ph	H	B30	3-SO2iPr
2,6-Me2—Ph	H	B31	3-SCF3
1-naphthyl	H	CO(3,4-(MeO)2—Ph)	3-SCH2CH2CHFCHF2
PhCH2	H	CO(2,4-Cl2—Ph)	3-SO2CF2CHF2
2-thienyl	H	CO(3-CF3—Ph)	3-SCH2CMe═CH2
3-Me-2-pyridyl	H	CO(2-Me2N—Ph)	3-SOCH2CH═CH2
3-NO2-2-pyridyl	H	COiPr	3-SO2CHMeCH═CH2
3,6-Cl2-2-pyridyl	H	CO2iPr	3-SCH2CMe═CF2
2-MeS-3-pyridyl	H	CO2tBu	3-SOCH2CF═CCl2
(CH2)5C═N—	H	CONHMe	3-SO2CH2CH═CH2Cl
sBu	H	CONHEt	3-OCH2CCH
tBuCH2	H	B19	3-SCH2CCMe
EtMe2C	H	B18	3-SOCH2CCH
2-Me-cHex	H	SO2(2-Me—Ph)	3-SO2CH2CCMe
Ph	H	H	3-NO2
2-CF3O—Ph	H	H	3-CN
2-MeS—Ph	H	H	3-CO2Et
2,6-F2—Ph	H	Na	3-COnPr
2,6-Cl2—Ph	H	K	3-O(CO)nPr
1-naphthyl	H	Mg	3-NHBu
3-F-2-pyridyl	H	Ca	3-NEt2
6-Me-2-pyridyl	H	Ba	4-F
4-CF3-3-pyridyl	H	COCEtMe2	4-Cl
3-NO2-3-pyridyl	H	CO(3-MeO—Ph)	4-Br
2,4-Me2-3-pyridyl	H	CO-2-naphtyl	4-I
iBuMeC═N—	H	CO(4-EtO-3-MeO—Ph)	4-Me
tBu	H	CO(3-Cl-4-MeO—Ph)	4-tBu
tBu	H	CO(3-F-4-nBuO—Ph)	4-OMe
tBu	H	CH2CO2Me	4-CF3
Ph	H	CH(Me)CO2Et	4-OCHF2
Ph	H	CMe2CO2nPr	4-SMe
2-pyridyl	H	CH2CN	4-SOMe
sBu	H	CH2CH2CH2CN	4-SO2nBu
tBuCH2	H	CH2CO2iPr	4-SCF3
EtMe2C	H	H	4-SOCBrF2
2-Me-cHex	H	H	4-SO2CH2F
Ph	H	H	4-OCH2CH═CH2
2-CF3—Ph	H	H	4-OCH2CH═CCl2
2-NO2—Ph	H	B3	4-OCH2CCH
2,6-F2—Ph	H	B4	4-OCH2CCCl
2-Cl-6-F—Ph	H	B5	4-SCH2CCMe
1-naphthyl	H	B6	4-SO2CH2CCMe
2-pyridyl	H	B7	4-NO2
3-pyridyl	H	B8	4-CN
PhCH2	H	B12	4-CO2nBu
2-thienyl	H	B21	4-COiBu
3-thienyl	H	B28	4-O(CO)nPr
iBuMeC═N—	H	CO(2-MeO—Ph)	4-NHnBu
tBu	H	H	2,3-Cl2
tBu	H	H	2,4-Cl2
tBu	H	H	3,4-Cl2
Ph	H	H	3,5-Cl2
Ph	H	H	2,5-Cl2
2-pyridyl	H	B7	2,6-Cl2
sBu	H	B8	2,6-Cl2
tBuCH2	H	B12	2,6-Cl2
EtMe2C	H	B23	2,3-F2
2-Me-cHex	H	B26	2,3-F2
Ph	H	B28	2,3-F2
2-Me—Ph	H	CONHiPr	2,4-F2
2-MeO—Ph	H	Ca	2,4-F2
2,6-F2—Ph	H	Ba	2,5-F2
2,6-Cl2—Ph	H	H	2,6-F2
1-naphthyl	H	H	2,6-F2
2-pyridyl	H	H	2,6-F2
PhCH2	H	CO(2,3-Me2—Ph)	2,6-F2
3-pyridyl	H	CO(3,4-Me2—Ph)	2,6-F2
4-pyridyl	H	CH2CO2Et	2,6-F2
2-thienyl	H	CHMeCO2Me	2,6-F2
iBuMeC═N—	H	CH2CN	2,6-F2
tBu	H	H	2,6-F2
tBu	H	B7	2,6-F2
tBu	H	B8	2,6-F2
tBu	H	B28	2,6-F2
tBu	Me	B31	2,6-F2
tBu	H	B34	2,6-F2
tBu	H	CO(2-MeO—Ph)	2,6-F2
tBu	H	CO(2-Cl—Ph)	2,6-F2
tBu	H	CO(2,6-Me2—Ph)	2,6-F2
tBuCH2	H	CO(2,6-(MeO)2—Ph)	2,6-F2
EtMe2C	H	CO(3,4,5-(MeO)3—Ph)	2,6-F2
cHex	H	B28	2,6-F2
cHex	H	B30	2,6-F2
cHex	H	B34	2,6-F2
1-Me-cHex	H	SO2(4-Cl—Ph)	2,6-F2
Ph	H	H	2,6-F2
Ph	H	B5	2,6-F2
Ph	H	B6	2,6-F2
2-F—Ph	H	B14	2,6-F2
3-F—Ph	H	B19	2,6-F2
4-F—Ph	H	B23	2,6-F2
2-Cl—Ph	H	B24	2,6-F2
2,6-F2—Ph	H	H	2,6-F2
2,6-F2—Ph	H	Ca	2,6-F2
2,6-F2—Ph	Me	B7	2,6-F2
2,6-F2—ph	H	B9	2,6-F2
1-naphthyl	H	B10	2,6-F2
2-naphthyl	H	B16	2,6-F2
2-thienyl	H	B22	2,6-F2
3-thienyl	H	B24	2,6-F2
2-pyridyl	Cl	H	3,4-F2
3-pyridyl	H	B7	3,5-F2
4-pyridyl	H	B18	2,5-(CF3)2
nPr2C═N—	H	B31	2,6-(CF3)2
tBu	Et	H	3,5-(CF3)2
tBu	Br	H	5-Br-2-Cl
tBu	H	SO2(4-Me—Ph)	3-Br-4-Me
tBu	H	COnHex	2-Cl-4-F
tBu	H	CO(2-Cl-6-F—Ph)	2-Cl-6-F
tBuCH2	H	CO(3,5-Cl2-4-MeO—Ph)	2-Cl-6-F
EtMe2C	H	CO(3-Br-4-Me—Ph)	2-Cl-6-F
cHex	H	H	2-Cl-6-F
cHex	H	B6	2-Cl-6-F
Ph	H	B7	2-Cl-6-F
Ph	H	B8	2-Cl-6-F
2-F—Ph	H	B34	2-Cl-6-F
3-F—Ph	H	CO2tBu	2-Cl-6-F
2-Cl—Ph	H	CHMeCO2Me	2-Cl-6-F
2,6-F2—Ph	H	B31	3-Cl-4-F
2,6-F2—Ph	H	K	4-Cl-3-F
tBu	H	Ba	2-F-6-I
2,6-F2—Ph	H	CO(4-nBuO—Ph)	2-F-6-I
2,6-F2—Ph	H	CO(4-Et2N—Ph)	2-F-6-I
2,6-F2—Ph	Br	CO(3-Me2N—Ph)	2-Cl-5-SMe
1-naphthyl	H	CO(4-Et-Ph)	2-Cl-5-SCBrF2
2-naphthyl	H	CO(3-F-4-Me—Ph)	2-Cl-5-SCF3
2-thienyl	H	CO(3-MeO-4-Me—Ph)	2-Cl-5-SOMe
3-thienyl	H	CO(2,3,6F3—Ph)	2-Cl-5-SO2Me
2-pyridyl	H	CO(2-MeO-5-N02—Ph)	2-Cl-4-NO2
3-pyridyl	H	CO(3,5-Me2—Ph)	2,4-(OMe)2
4-pyridyl	H	H	2,6-(OMe)2
nPr2C═N—	H	H	2,6-(OMe)2
tBu	H	H	2,3-Me2
tBu	H	B1	2,4-Me2
tBu	H	B2	2,5-Me2
tBuCH2	H	B3	2,6-Me2
EtMe2C	H	B4	2,6-Me2
cHex	H	B5	2,6-Me2
cHex	H	B6	3,4-Me2
1-Me-cHex	H	B7	3,5-Me2
Ph	H	B8	2-F-4-Me
Ph	H	B9	2-F-4-Me
Ph	H	B10	2-F-4-Me
2-F—Ph	H	B11	3-F-4-Me
2-F—Ph	H	B12	3-I-4-Me
3-F—Ph	H	B13	2-OMe-4-SMe
4-F—Ph	H	B14	3-OMe-4-NO2
2-Cl—Ph	H	CH2CN	2-Me-4-NO2
2,6-F2—Ph	H	CMe2CO2Et	2-Me-6-N02
2,6-F2—Ph	H	CONHMe	2,3,6-F3
tBu	H	SO2(4-Cl-Ph)	2,3,6-F3
cHex	H	CO(2-MeO—Ph)	2,3,6-F3
1-naphthyl	H	CO(2-Me—Ph)	2,3,6-F3
2-F—Ph	H	CO(2-Cl—Ph)	2,3,6-F3
2-pyridyl	H	CO(2,6-(MeO)2—Ph)	2,4,5-F3
3-pyridyl	H	CO(3,4-Me2—Ph)	2,4,5-F3
4-pyridyl	H	CO(3-MeO-4-EtO—Ph)	2,4,5-F3
nPr2C═N—	H	B15	2,3,5-I3
tBu	H	B16	2,3,5-I3
tBu	H	B17	2,3,4-(OMe)3
tBu	H	B18	2,4,5-(OMe)3
tBu	H	B19	3,4,5-(OMe)3
tBu	H	B20	2,4,6-Me3
tBuCH2	H	B21	2,3,4,5-F4
EtMe2C	H	B24	2,3,4,5-F4
cHex	H	B25	2,3,4,5-F4
cHex	H	B27	2,3,5,6-F4
cHex	H	B28	2,3,5,6-F4
1-Me-cHex	H	B29	2,3,5,6-F4
Ph	H	B30	2,3,5,6-F4
Ph	H	B31	2,3,4,5,6-F5
Ph	H	B32	2,3,4,5,6-F5
2-F—Ph	H	B33	2,3,4,5,6-F5
3-F—Ph	H	B34	2,3,5,6-F4-4-Me
4-F—Ph	H	H	2,3,5,6-F4-4-Me
2-Cl—Ph	H	H	2,3,5,6-F4-4-Me
2,6-F2—Ph	H	B27	2,3,5,6-F4-4-Me
2,6-F2—Ph	H	Ca	2,3,5,6-F4-4-Me

TABLE 9
	R1	B	Y1
	Me	H	H
	Et	B1	Me
	iPr	B2	Et
	nBu	B3	nPr
	sBu	B4	iBu
	tBu	H	nHex
	tBu	B7	Me
	tBu	B8	MeO
	tBu	B8	MeS
	tBu	B7	CF3
	tBu	B5	CF3
	tBu	B7	CClF2
	tBu	B8	CF3CF2
	tBu	4-Cl—PhCO2	CF3CF2CF2
	tPen	B6	MeO
	nHex	B7	EtO
	nHep	B8	iPrO
	nOct	B9	sBuO
	nNon	B10	MeS
	nDec	B11	EtS
	PhCH2	B12	nPrS
	Ph(Me)CH	B13	tBuS
	PhMe2C	B14	Ph
	PhMe2C	B7	Me
	PhMe2C	B8	Me
	PhMe2C	B33	Me
	PhMe2C	B34	Me
	PhMe2C	B41	Me
	PhMe2C	B7	CF3
	PhMe2C	B8	CF3
	PhMe2C	B34	CF3
	4-Cl—PhMe2C	B15	Me2N
	3-Br—PhEtMeC	B16	Et2N
	4-Me—Ph(CH2)3	B17	H
	CH2═CMe	B18	Me
	CF3CF2 CF2	B19	Et
	cPr	B20	nPr
	cPen	B21	iBu
	cPen	B22	nHex
	cPen	B23	CF3
	cHex	B24	CClF2
	cHex	B7	CF3
	cHex	B8	CF3
	cHex	B33	CF3
	cHex	B34	CF3
	cHex	B7	Me
	cHex	B8	Me
	cHex	B34	Me
	1-Me—cHex	B7	Me
	1-Me—cHex	B8	CF3
	1-Me—cHex	B7	CF3
	1-Me—cHex	iBuOC(O)	CF3
	1-Me—cHex	B28	EtO
	1-Me—cHex	B29	iPrO
	EtO	B30	sBuO
	iPrO	B31	MeS
	CF3O	B32	EtS
	tBuOC(O)	B33	nPrS
	Ph	B34	tBuS
	2-F—Ph	B35	Ph
	2-F—Ph	B36	Me2N
	2-Cl—Ph	B37	Et2N
	2-Cl—Ph	B38	Cl
	2-Br—Ph	B39	Br
	2-I—Ph	B40	I
	2-CF3—Ph	B41	H
	2-MeO—Ph	B42	CF3
	3,4-Cl2—Ph	CClF2C(O)	MeO
	2,4-Me2—Ph	PhSC(O)	MeS
	2,6-F2—Ph	B7	Me
	2,6-F2—Ph	B7	CF3
	2,6-F2—Ph	B8	Me
	2,6-F2—Ph	B8	CF3
	2,6-F2—Ph	EtSC(O)	H
	2,6-F2—Ph	tBuC(S)	Me
	2,6-F2—Ph	cPenOC(O)	Et
	2-pyridyl	cHexOC(O)	nPr
	2-pyridyl	B7	Me
	2-pyridyl	B8	Me
	2-pyridyl	B7	CF3
	2-pyridyl	B8	CF3
	2-pyridyl	iBuOC(O)	CF3
	2-pyridyl	B33	CF3
	2-pyridyl	B34	CF3
	2-pyridyl	B34	Me
	2-pyridyl	2-pyridyl-C(O)	CClF2
	2-pyridyl	2-pyridyl-C(O)	CF3CF2
	2-thienyl	3-pyridyl-C(O)	CF3CF2CF2
	1-naphthyl	4-pyridyl-C(O)	MeO
	2-naphthyl	H	EtO
	tBu	CClF2C(O)	H
	tBu	PhSC(O)	Me
	tBu	EtSC(O)	Et
	tBu	tBuC(S)	npr
	cPr	cPenOC(O)	iBu
	cPen	cHexOC(O)	nHex
	cHex	B7	CF3
	1-Et—cPr	B8	CClF2
	1-Me—cPen	iBuOC(O)	CF3CF2
	1-Me—cPen	2-pyridyl-C(O)	CF3CF2CF2
	2,6-F2—Ph	2-pyridyl-C(O)	MeO
	2,6-F2—Ph	2-pyridyl-C(O)	MeO
	2,6-F2—Ph	4-pyridyl-C(O)	Me
	2,6-F2—Ph	2-pyridyl-C(O)	CF3

TABLE 10
	R1	B	A
	Et	H	A1
	iPr	B7	A2
	iBu	B7	A1
	sBu	B7	A2
	tBu	B7	A1
	tBu	B8	A1
	tBu	B15	A1
	tBu	B34	A1
	tBu	B7	A2
	tBu	B8	A2
	tBu	B15	A2
	tBu	B34	A2
	tBu	CO2—iBu	A2
	tBu	B7	A3
	tBu	B7	A4
	tBu	B7	A5
	tBu	B7	A6
	tBu	H	A7
	tBu	B7	A7
	tBu	B8	A7
	tBu	B15	A7
	tBu	B34	A7
	tBu	H	A8
	tBu	B15	A8
	tBu	B34	A8
	tBu	H	A9
	tBu	B7	A9
	tBu	B8	A9
	tBu	B15	A9
	tBu	B34	A9
	tBu	CO2—iBu	A9
	tBu	H	A10
	tBu	B7	A10
	tBu	B8	A10
	tBu	B15	A10
	tBu	B34	A10
	tBu	CO2—iBu	A10
	tBu	H	A11
	tBu	B7	A11
	tBu	B8	A11
	tBu	B15	A11
	tBu	H	A12
	tBu	B7	A12
	tBu	B8	A12
	tBu	B15	A12
	tBu	B34	A12
	tBu	B7	A8
	tBu	B8	A8
	tBu	B7	A13
	tBu	B8	A13
	tBu	B15	A13
	tBu	B34	A13
	tBu	CO2—iBu	A13
	tBu	H	A14
	tBu	H7	A14
	tBu	B16	A14
	tBu	H17	A14
	tBu	H7	A15
	tBu	B8	A16
	tBu	B9	A17
	tBu	B10	A18
	tBu	B11	A19
	tBu	H12	A20
	tBu	B13	A21
	tBu	B7	A22
	tBu	B8	A22
	tBu	H7	A23
	tBu	B8	A23
	tBu	B15	A23
	tBu	CO2—iBu	A12
	tBu	H	A13
	tBu	B17	A27
	tBu	B18	A28
	tBu	B19	A29
	tBu	B7	A30
	tBu	B8	A30
	tBu	B15	A30
	tBu	B20	A31
	tBu	H	A32
	tBu	H7	A32
	tBu	B8	A32
	tBu	H15	A32
	tBu	B34	A32
	tBu	CO2—iBu	A32
	tBu	B21	A33
	tBu	B22	A34
	tBu	B23	A35
	tBu	B24	A36
	tBuCH2	B3	A1
	tBuCH2	B7	A2
	tBuCH2	B8	A2
	Et(Me)2C	B15	A2
	tBu	B34	A23
	tBu	B14	A24
	tBu	B15	A25
	tBu	B16	A26
	nHex	B7	A1
	nHep	B7	A2
	nOct	B7	A1
	nNon	B7	A2
	nDec	B7	A7
	cPr	B7	A8
	1-Me—cPr	B7	A1
	1-Me—cPr	B7	A2
	1-Me—cPr	B8	A2
	1-Me—cPr	B34	A2
	1-Me—cPr	H	A2
	cPen	B7	A2
	cHex	B7	A1
	cHex	B7	A2
	cHex	B8	A2
	cHex	B15	A2
	cHex	B34	A2
	cHex	B35	A2
	cHex	B36	A1
	Et(Me)2C	B16	A2
	Et(Me)2C	B34	A2
	Et(Me)2C	H	A2
	Et(Me)2C	B7	A2
	Ph	B7	A10
	Ph	B7	A13
	Ph	B7	A32
	2-F—Ph	B7	A1
	2-F—Ph	B7	A2
	2-F—Ph	B7	A7
	2-F—Ph	B7	A8
	2-F—Ph	B7	A9
	2-F—Ph	B7	A10
	2-F—Ph	B7	A13
	2-F—Ph	B7	A32
	2-Cl—Ph	B7	A1
	2-Cl—Ph	B7	A2
	2-Cl—Ph	B7	A7
	2-Cl—Ph	B7	A8
	2-Cl—Ph	B7	A9
	2-Cl—Ph	B7	A10
	2-Cl—Ph	B7	A13
	2-Cl—Ph	B8	A30
	cHex	B37	A2
	Ph	H	A2
	Ph	B7	A2
	Ph	B7	A7
	Ph	B7	A8
	Ph	B7	A9
	2-Me—Ph	B7	A1
	2-Me—Ph	B7	A2
	2-MeO—Ph	B2	A7
	2-CF3—Ph	B3	A8
	2-N02—Ph	B4	A9
	2-CN—Ph	B5	A10
	2-CBrF2O—Ph	B6	A11
	2-CF3O—Ph	B7	A12
	2-MeS—Ph	B8	A13
	2-nBuS—Ph	B9	A14
	2-MeSO—Ph	B10	A15
	2-MeSO2—Ph	B11	A16
	2-CH2═CHCH2S—Ph	B12	A17
	2-CH2═CHCH2SO—Ph	B13	A18
	2-CH2═CHCH2SO2—Ph	B14	A19
	2-CF3S—Ph	B15	A20
	2-CHF2S—Ph	B16	A21
	2-Cl—Ph	B34	A32
	2-Br—Ph	B7	A1
	2-I—Ph	B7	A2
	2-Me-Ph	B7	A7
	2-Me-Ph	B7	A8
	2-Me-Ph	B7	A9
	2,6-Cl2—Ph	B7	A1
	2,6-Cl2—Ph	B7	A2
	2,6-Cl2—Ph	B7	A7
	2,6-F2—Ph	B7	A1
	2,6-F2—Ph	B7	A2
	2,6-F2—Ph	B7	A7
	2,6-F2—Ph	B7	A8
	2,6-F2—Ph	B7	A9
	2,6-F2—Ph	B7	A10
	2,6-F2—Ph	B7	A13
	2,6-F2—Ph	B7	A21
	2,6-F2—Ph	B7	A32
	2,6-F2—Ph	B3	A2
	2,6-F2—Ph	B4	A2
	2,6-F2—Ph	B5	A2
	2,6-F2—Ph	B8	A2
	2,6-F2—Ph	B15	A2
	2-CBrF2SO—Ph	B17	A22
	2-CF3SO2—Ph	B18	A23
	2-CHO—Ph	B19	A24
	2-OH—Ph	B20	A25
	2-Me2—NPh	B21	A26
	3-Ph—Ph	B22	A27
	4-PhO—Ph	B23	A28
	2-MeOC(O)—Ph	B24	A29
	Cl	B7	A1
	PhCH2	B7	A1
	PhCH2	B7	A2
	PhCH2	B8	A2
	PhCH2	B34	A2
	(4-Cl—Ph)CH2	B7	A30
	(4-Me—Ph)CH2	B7	A31
	(3,4-Cl2—Ph)CH2	B7	A32
	(2,4-Me2—Ph)CH2	B7	A33
	PhMeCH	B7	A34
	Ph(Me)2C	B3	A1
	Ph(Me)2C	B7	A1
	Ph(Me)2C	B3	A2
	Ph(Me)2C	B7	A2
	Ph(Me)2C	B8	A2
	2,6-F2—Ph	B19	A2
	2,6-F2—Ph	B32	A2
	2,6-F2—Ph	B33	A2
	2,6-F2—Ph	B34	A2
	2,6-F2—Ph	B35	A2
	2,6-F2—Ph	B37	A2
	2,6-F2—Ph	B40	A2
	2,6-F2—Ph	B43	A2
	ClCC	B3	A23
	2,2-Cl2—cPr	B4	A23
	2,2-F2—cBu	B5	A23
	MeO	B6	A24
	nHexO	B7	A25
	CH2═CHCH2O	B8	A26
	CHCCH2O	B9	A27
	CF3O	B10	A28
	ClCH═CHCH2O	B11	A29
	MeS	B12	A30
	MeSO	B13	A30
	MeSO2	B14	A30
	Me2C═CHCH2S	B15	A31
	Me2C═CHCH2SO	B16	A32
	Me2C═CHCH2SO2	B17	A32
	Ph(Me)2C	B33	A2
	Ph(Me)2C	B34	A2
	Ph(Me)2C	B35	A2
	Ph(Me)2C	B7	A13
	Ph(Me)2C	B8	A13
	Ph(Me)2C	B34	A13
	CF3	B15	A35
	CF3CH2	B6	A36
	CH2═CMe	B6	A1
	Cl2C═CH	B29	A2
	BrCCCH2SO	B28	A1
	ClCCH2SO2	B29	A2
	1-naphthyl	B30	A2
	2-naphthyl	B31	A13
	MeC(O)	B32	A13
	MeC(O)O	B33	A1
	CF3C(O)O	B34	A1
	2-thienyl	B35	A2
	3-thienyl	B36	A2
	Me2C═N	B37	A1
	EtMeC═N	B38	A1
	PhCH═N	B39	A2
	PhMeC═N	B40	A2
	CHCCH2S	B18	A32
	CHCCH2SO	B19	A1
	CHCCH2SO2	B20	A2
	CF3S	B21	A2
	CF3SO	B22	A13
	CF3SO2	B23	A13
	ClCH═CHCH2S	B24	A1
	ClCH═CHCH2SO	B25	A1
	ClCH═CHCH2SO2	B26	A2
	ClCCCH2S	B27	A2
	2-pyridyl	H	A7
	2-pyridyl	B7	A7
	2-pyridyi	B8	A7
	2-pyridyl	B15	A7
	2-pyridyl	B34	A7
	2-pyridyl	H	A8
	2-pyridyl	B7	A8
	2-pyridyl	B8	A8
	2-pyridyl	B15	A8
	2-pyridyl	B34	A8
	2-pyridyl	H	A9
	2-pyridyl	B7	A9
	2-pyridyl	B8	A9
	2-pyridyl	B7	A1
	2-pyridyl	B8	A1
	2-pyridyl	B15	A1
	2-pyridyl	B34	A1
	2-pyridyl	B7	A2
	2-pyridyl	B8	A2
	2-pyridyl	B15	A2
	2-pyridyl	B34	A2
	2-pyridyl	CO2—iBu	A2
	2-pyridyl	B7	A3
	2-pyridyl	B7	A4
	2-pyridyl	B7	A5
	2-pyridyl	B7	A6
	2-pyridyl	H	A12
	2-pyridyl	B7	A12
	2-pyridyl	B8	A12
	2-pyridyl	B15	A12
	2-pyridyl	B34	A12
	2-pyridyl	CO2—iBu	A12
	2-pyridyl	H	A13
	2-pyridyl	B7	A13
	2-pyridyl	B8	A13
	2-pyridyl	B15	A13
	2-pyridyl	B15	A9
	2-pyridyl	B34	A9
	2-pyridyl	CO2—iBu	A9
	2-pyridyl	H	A10
	2-pyridyl	B7	A10
	2-pyridyl	B8	A10
	2-pyridyl	B15	A10
	2-pyridyl	B34	A10
	2-pyridyl	CO2—iBu	A10
	2-pyridyl	H	A11
	2-pyridyl	B7	A11
	2-pyridyl	B8	A11
	2-pyridyl	B15	A11
	2-pyridyl	B8	A23
	2-pyridyl	B15	A23
	2-pyridyl	B34	A23
	2-pyridyl	B14	A24
	2-pyridyl	B15	A25
	2-pyridyl	B16	A26
	2-pyridyl	B17	A27
	2-pyridyl	B18	A28
	2-pyridyl	B19	A29
	2-pyridyl	B7	A30
	2-pyridyl	B34	A13
	2-pyridyl	CO2—iBu	A13
	2-pyridyl	H	A14
	2-pyridyl	B7	A14
	2-pyridyl	B16	A14
	2-pyridyl	B17	A14
	2-pyridyl	B7	A15
	2-pyridyl	B8	A16
	2-pyridyl	B9	A17
	2-pyridyl	B10	A18
	2-pyridyl	B11	A19
	2-pyridyl	B12	A20
	2-pyridyl	B13	A21
	2-pyridyl	B7	A22
	2-pyridyl	B8	A22
	2-pyridyl	B8	A30
	2-pyridyl	B15	A30
	2-pyridyl	B20	A31
	2-pyridyl	H	A32
	2-pyridyl	B7	A32
	2-pyridyl	B8	A32
	3-pyridyl	B7	A1
	3-pyridyl	B34	A2
	3-pyridyl	CO2—iBu	A2
	3-pyridyl	B7	A13
	3-pyridyl	B8	A13
	4-pyridyl	B7	A1
	4-pyridyl	B8	A1
	4-pyridyl	B15	A2
	4-pyridyl	B34	A2

TABLE 11
or
G	B	Y1	Y2	Y3
2-Cl	H	Me	Me	Me
3-Cl	B1	Me	Cl	Me
4-Cl	B2	Cl	Me	Me
4-Br	B3	Cl	Cl	Me
4-I	B4	CF3	Cl	Me
4-F	B5	CF3	H	Me
4-Me	B6	H	CF3	Me
4-Et	B7	H	Cl	Me
4-iPr	B8	Cl	H	Me
4-nBu	B9	H	H	Me
4-iBu	B10	OMe	Cl	Me
4-sBu	B11	SMe	Cl	Me
4-sBu	H	Me	Me	Me
4-sBu	B16	Me	Me	Me
4-sBu	B17	Me	Me	Me
4-sBu	B7	Me	Cl	Me
4-sBu	B8	Me	Cl	Me
4-sBu	B16	Me	Cl	Me
4-sBu	B17	Me	Cl	Me
4-sBu	B34	Me	Cl	Me
4-sBu	B3	CF3	Cl	Me
4-sBu	B7	CF3	Cl	Me
4-sBu	B8	CF3	Cl	Me
4-sBu	B34	CF3	Cl	Me
4-sBu	B7	Cl	Cl	Me
4-sBu	B17	Cl	Cl	Me
4-tBu	B12	SCF3	Cl	Me
4-tBu	H	Me	Me	Me
4-tBu	B3	Me	Cl	Me
4-tBu	B7	Cl	Me	Me
4-tBu	B8	Cl	Cl	Me
4-tBu	B15	Cl	Cl	Me
4-tBu	B16	Cl	Cl	Me
4-tBu	B28	Cl	Cl	Me
4-tBu	B30	Cl	Cl	Me
4-tBu	B34	Cl	Cl	Me
4-tBu	CO—nC8H17	Cl	Cl	Me
4-tBu	CO—nC15H31	Cl	Cl	Me
4-tBu	CO2-nHex	Cl	Cl	Me
4-tBu	CO2—nC10H21	Cl	Cl	Me
4-tBu	H	CN	Cl	Me
4-tBu	H	CF3	Cl	Me
4-tBu	B3	CF3	Cl	Me
4-tBu	B7	CF3	Cl	Me
4-tBu	B8	CF3	Cl	Me
4-tBu	B15	CF3	Cl	Me
4-tBu	B16	CF3	Cl	Me
4-tBu	B28	CF3	Cl	Me
4-tBu	B30	CF3	Cl	Me
4-tBu	B16	Cl	Cl	Me
4-tBu	B16	CF3	Cl	Me
4-tBu	B17	CF3	Cl	Me
4-tBu	B17	Cl	Cl	Me
4-tBu	CO2—nC10H21	CF3	Cl	Me
4-tBu	CH2OEt	CF3	Cl	Me
4-tBu	B7	Me	Cl	Me
4-tBu	B7	Me	Me	Me
4-tBu	B7	CN	Cl	Me
4-tBu	B16	CN	Cl	Me
4-tBu	B3	CN	Cl	Me
4-tBu	2-(4-tBu—Ph)-3,3-Me2—cPrC(O)	CF3	Cl	Me
4-tBu	B45	CF3	Cl	Me
4-tBuCH2	B3	CF3	Cl	Me
4-tBuCH2	B7	Me	Me	Me
4-tBuCH2	B16	Me	Cl	Me
4-tBuCH2	B7	CF3	Cl	Me
4-tBuCH2	B8	CF3	Cl	Me
4-tBuCH2	B7	Cl	Cl	Me
4-Et(Me)2C	H	CF3	Cl	Me
4-Et(Me)2C	B3	CF3	Cl	Me
4-Et(Me)2C	B7	CF3	Cl	Me
4-Et(Me)2C	B8	CF3	Cl	Me
4-Et(Me)2C	B34	CF3	Cl	Me
4-Et(Me)2C	B42	CF3	Cl	Me
4-Et(Me)2C	B16	Me	Me	Me
4-Et(Me)2C	B17	Me	Me	Me
4-Et(Me)2C	H	Cl	Me	Me
4-Et(Me)2C	B7	Cl	Cl	Me
4-Et(Me)2C	B8	Cl	Cl	Me
4-Et(Me)2C	B7	CF3	Me	Me
4-Et(Me)2C	B7	CN	Cl	Me
4-Et(Me)2C	B4	H	Cl	Me
4-Et(Me)2C	B5	Cl	H	Me
4-Et(Me)2C	B6	H	H	Me
4-Et(Me)2C	B3	Cl	Cl	Me
4-Et(Me)2C	B16	Cl	Cl	Me
4-Et(Me)2C	B17	Cl	Cl	Me
4-Et(Me)2C	B24	Cl	Cl	Me
4-nHex	B34	CF3	Cl	Me
4-nHep	B42	CF3	Cl	Me
4-nOct	B43	Me	Me	Me
4-nNon	B43	Me	Cl	Me
4-nDec	H	Cl	Me	Me
4-(Me)2(CN)C	B7	Cl	Cl	Me
4-PhCH2	B7	CF3	Cl	Me
4-Ph(Me)2C	B7	CF3	Me	Me
4-(4-F—Ph)(Me)2C	B7	CN	Cl	Me
4-MeCH═CH	B4	H	Cl	Me
4-MeCC	B5	Cl	H	Me
3-CF3	B6	H	H	Me
4-CF3	B7	OMe	Cl	Me
4-CF3	B8	SMe	Cl	Me
4-CF3	B9	SCF3	Cl	Me
4-CF3	B16	Me	Me	Me
4-CF3	B17	Me	Me	Me
4-CF3	B16	Me	Cl	Me
4-CF3	B17	Cl	Me	Me
4-CF3	B7	Cl	Cl	Me
4-CF3	B7	CF3	Cl	Me
4-CF3	B7	CN	Cl	Me
4-CF3	B3	Cl	Cl	Me
4-CF3CH2	B7	Me	Cl	Me
4-Cl2C═CHCH2	B8	Cl	Me	Me
4-BrCC	B7	Cl	Cl	Me
4-(2,2-F2)cBuCH2	B7	CF3	Cl	Me
4-(1-Me)cPr	B16	CN	Cl	Me
4-cHex	B7	Cl	Cl	Me
4-(1-Me)cHex	B8	CF3	Cl	Me
4-MeO	B7	Cl	H	Me
4-iPrO	B7	Cl	Cl	Me
4-iPrO	B7	CF3	Cl	Me
4-iPrO	B15	CF3	Cl	Me
4-iPrO	B7	Me	Me	Me
4-iPrO	B16	Me	Me	Me
4-iPrO	B17	Me	Me	Me
4-iPrO	B23	SCF3	Cl	Me
4-tBuO	B7	Cl	Cl	Me
4-tBuO	B8	Cl	Cl	Me
4-tBuO	B7	CF3	Cl	Me
4-nHexO	B8	CF3	Cl	Me
4-nOctO	B34	CF3	Cl	Me
4-nDecO	H	CF3	Cl	Me
4-CH2═CHCH2O	B7	CF3	Cl	Me
4-CHCCH2O	B8	CF3	Cl3	Me
4-CHF2O	B34	CF3	Cl	Me
4-CHF2O	B7	Me	Me	Me
4-CHF2O	B35	Me	Cl	Me
4-CHF2O	B36	Cl	Cl	Me
4-CHF2O	B7	Cl	Cl	Me
4-CBrF2O	B8	Cl	Cl	Me
4-CBrF2O	B34	Cl	Cl	Me
4-CBrF2O	B40	Me	Me	Me
4-CBrF2O	B41	Me	Cl	Me
4-CBrF2O	B42	Cl	Me	Me
4-CBrF2O	B43	Cl	Cl	Me
4-CBrF2O	B44	CF3	Cl	Me
4-CBrF2O	COCO2Me	CF3	H	Me
4-CBrF2O	H	H	CF3	Me
4-CBrF2O	B1	H	Cl	Me
4-CF3O	B2	Cl	H	Me
4-CF3O	B3	H	H	Me
4-CF3O	B4	OMe	Cl	Me
4-CF3O	B5	SMe	Cl	Me
4-CF3O	B6	SCF3	Cl	Me
4-CF3O	B7	Me	Me	Me
4-CF3CH2O	B8	Me	Me	Me
4-CF2═CHCH2CH2O	B9	Me	Cl	Me
4-CCl2═CHCH2O	B10	Cl	Me	Me
4-ClCCCH2O	B11	Cl	Cl	Me
4-MeS	B12	CF3	Cl	Me
4-sBuS	H	CF3	H	Me
4-EtSO	B3	H	CF3	Me
4-MeSO2	H	CF3	Cl	Me
4-MeSO2	B3	CF3	Cl	Me
4-MeSO2	B32	CF3	Cl	Me
4-MeSO2	B33	CF3	Cl	Me
4-EtSO2	H	CF3	Cl	Me
4-EtSO2	B3	Cl	Cl	Me
4-iPrSO2	B32	Cl	Cl	Me
4-iPrSO2	B33	Cl	Cl	Me
4-tBuSO2	B7	Cl	Cl	Me
4-tBuSO2	B33	CF3	Cl	Me
4-MeCH═CHCH2S	B15	H	H	Me
4-CH2═CHCH2SO	B16	OMe	Cl	Me
4-CH2═CHCH2SO2	B28	SMe	Cl	Me
4-CHCCH2S	B30	SCF3	Cl	Me
4-CHCCH2SO	B34	Me	Me	Me
4-CHCCH2SO2	CO—nC8H17	Me	Me	Me
4-CHF2S	H	CF3	Cl	Me
4-CHF2S	B7	CF3	Cl	Me
4-CHF2S	B8	CF3	Cl	Me
4-CHF2S	B15	CF3	Cl	Me
4-CHF2S	B29	CF3	Cl	Me
4-CHF2S	H	Cl	Cl	Me
4-CHF2S	B7	Cl	Cl	Me
4-CHF2S	B15	Cl	Cl	Me
4-CBrF2S	B7	Cl	Cl	Me
4-CBrF2S	B15	Cl	CL	Me
4-CBrF2S	B30	Cl	Cl	Me
4-CBrF2S	B43	Cl	Cl	Me
4-CBrF2S	CO—nC15H31	Me	Cl	Me
4-CBrF2S	CO2-nHex	CF3	Cl	Me
4-CBrF2S	H	CF3	Cl	Me
4-CBrF2S	B7	CF3	Cl	Me
4-CBrF2S	B8	CF3	Cl	Me
4-CBrF2S	B15	CF3	Cl	Me
4-CBrF2S	B28	CF3	Cl	Me
4-CBrF2S	B34	CF3	Cl	Me
4-CBrF2S	B7	Me	Cl	Me
4-CF3S	CO2—nC10H21	Cl	Cl	Me
4-CF3S	H	Cl	Cl	Me
4-CF3S	B3	Cl	Cl	Me
4-CF3S	B7	Cl	Cl	Me
4-CF3S	B8	Cl	Cl	Me
4-CF3S	B15	Cl	Cl	Me
4-CF3S	H	CF3	Cl	Me
4-CF3S	B7	CF3	Cl	Me
4-CF3S	B8	CF3	Cl	Me
4-CF3S	B15	CF3	Cl	Me
4-CF3S	B34	CF3	Cl	Me
4-CF3S	CO2—nC12H25	CF3	Cl	Me
4-CF3S	CO—nC15H31	CF3	Cl	Me
4-CF3S	CO—nC16H33	Me	Me	Me
4-CF3S	CO—nC17H35	Me	Cl	Me
4-CF3CH2S	CO—nC18H33	CF3	Cl	Me
4-CHF2CF2S	CO—nC19H39	CF3	H	Me
4-CHF2SO	CO—nC20H41	H	CF3	Me
4-CBrF2SO	H	H	Cl	Me
4-CBrF2SO	B3	CF3	Cl	Me
4-CBrF2SO	B7	CF3	Cl	Me
4-CBrF2SO	B24	CF3	Cl	Me
4-CBrF2SO	B32	CF3	Cl	Me
4-CBrF2SO	B33	CF3	Cl	Me
4-CF3SO	H	Cl	Cl	Me
4-CF3SO	B3	Cl	Cl	Me
4-CF3SO	B7	Cl	Cl	Me
4-CF3SO	B33	Cl	H	Me
4-CF3CH2SO2	B15	H	H	Me
4-CHF2CF2SO2	B16	OMe	Cl	Me
4-CHF2SO2	B28	SMe	Cl	Me
4-CHF2SO2	B7	CF3	Cl	Me
4-CHF2SO2	B24	CF3	Cl	Me
4-CHF2SO2	B32	CF3	Cl	Me
4-CHF2SO2	B33	CF3	Cl	Me
4-CHF2SO2	H	Cl	Cl	Me
4-CHF2SO2	B3	Cl	Cl	Me
4-CHF2SO2	B7	Cl	Cl	Me
4-CHF2SO2	B33	Cl	H	Me
4-CBrF2SO2	H	SCF3	Cl	Me
4-CBrF2SO2	B2	Cl	Cl	Me
4-CBrF2SO2	B3	Cl	Cl	Me
4-CBrF2SO2	B18	Cl	Cl	Me
4-CBrF2SO2	B19	Cl	Cl	Me
4-CBrF2SO2	B33	Cl	Cl	Me
4-CBrF2SO2	H	CF3	Cl	Me
4-CBrF2SO2	B3	CF3	Cl	Me
4-CBrF2SO2	B7	CF3	Cl	Me
4-CBrF2SO2	B20	CF3	Cl	Me
4-CBrF2SO2	B32	CF3	Cl	Me
4-CBrF2SO2	B33	CF3	Cl	Me
4-CBrF2SO2	B37	CF3	Cl	Me
4-CBrF2SO2	B7	Me	Me	Me
4-CBrF2SO2	B15	Me	Me	Me
4-CBrF2SO2	B17	Me	Me	Me
4-CBrF2SO2	B7	Me	Cl	Me
4-CBrF2SO2	B16	Me	Cl	Me
4-CF3SO2	B16	Me	Me	Me
4-CF3SO2	B7	Cl	Cl	Me
4-CF3SO2	B15	Cl	Cl	Me
4-CF3SO2	B3	CF3	Cl	Me
4-CF3SO2	B7	CF3	Cl	Me
4-CF3SO2	B15	Me	Me	Me
4-CF3SO2	B7	Me	Cl	Me
4-CF3SO2	B8	Me	Cl	Me
4-Cl2C═CHCH2S	B16	Me	Me	Me
4-Cl2C═CHCH2SO	B17	Me	Cl	Me
4-Cl2C═CHCH2SO2	B17	Cl	Me	Me
4-CBrCCH2S	CO2—nC10H21	Cl	Cl	Me
4-CBrCCH2SO	B33	CF3	Cl	Me
4-CBrCCH2SO2	B7	CF3	H	Me
4-CHO	B7	H	CF3	Me
4-NO2	B8	H	Cl	Me
4-CN	B16	Cl	H	Me
4-(Me)2N	B3	H	H	Me
4-Me(MeCO)N	B7	OMe	Cl	Me
4-PhMeN	B8	SMe	Cl	Me
4-PhCH2(MeCO)N	B15	SCF3	Cl	Me
4-(1-naphthyl)	B16	Me	Me	Me
4-(2-naphthyl)	B28	Me	Me	Me
4-(2-Cl—Ph)CH2O	B30	Me	Cl	Me
4-(3-Cl—Ph)CH2O	B34	Cl	Me	Me
4-(4-Cl-Ph)CH2O	B7	CF3	Cl	Me
4-(4-Cl—Ph)CH2O	B7	Cl	Cl	Me
4-(4-Cl—Ph)CH2O	B37	Cl	Cl	Me
4-(4-F—Ph)CH2O	B42	CF3	Cl	Me
4-(2-Me—Ph)CH2O	B43	CF3	H	Me
4-(4-Me—Ph)CH2O	B43	H	CF3	Me
4-(4-Et—Ph)CH2O	H	H	Cl	Me
3-(2,4-Cl2—Ph)CH2O	B7	Cl	H	Me
4-(3,4-Cl2—Ph)CH2O	B7	H	H	Me
4-(2,5-Me2—Ph)CH2O	B7	OMe	Cl	Me
4-(2,3,4,5,6-F5—Ph)CH2O	B7	SMe	Cl	Me
4-MeOC(O)	B4	SCF3	Cl	Me
4-EtOC(O)	B5	Me	Me	Me
4-nPrOC(O)	B6	Me	Me	Me
4-iPrOC(O)	B7	Me	Cl	Me
4-iBuOC(O)	B8	Cl	Me	Me
4-tBuOC(O)	B9	Cl	Cl	Me
4-tBuCH2OC(O)	B7	Cl	Cl	Me
4-tBuCH2OC(O)	B15	Cl	Cl	Me
4-tBuCH2OC(O)	B34	Cl	Cl	Me
4-tBuCH2OC(O)	B7	CF3	Cl	Me
4-tBuCH2OC(O)	B15	CF3	Cl	Me
4-tBuCH2OC(O)	B34	CF3	Cl	Me
4-tBuCH2OC(O)	B10	CF3	Cl	Me
4-Et(Me)2COC(O)	B11	CF3	H	Me
4-nHexOC(O)	B7	H	CF3	Me
4-MeOCH2	B8	H	Cl	Me
4-EtOCH2	B7	Cl	H	Me
4-iPrOCH2	B7	H	H	Me
4-MeC(O)	B16	OMe	Cl	Me
4-EtC(O)	B7	SMe	Cl	Me
4-iPrC(O)	B8	SCF3	Cl	Me
4-tBuC(O)	H	Cl	Cl	Me
4-tBuC(O)	B3	Cl	Cl	Me
4-tBuC(O)	B7	Cl	Cl	Me
4-tBuC(O)	B3	CF3	Cl	Me
4-tBuC(O)	B7	CF3	Cl	Me
4-tBuC(O)	B15	CF3	Cl	Me
4-tBuC(O)	B7	Me	Me	Me
4-tBuC(O)	B17	Me	Me	Me
4-tBuC(O)	B16	Me	Cl	Me
4-CF3C(O)	B7	Me	Me	Me
4-CF3CF2C(O)	B8	Me	Cl	Me
4-CF2CF2CF2C(O)	B22	Cl	Me	Me
4-MeC(O)O	B23	Cl	Cl	Me
4-iPrC(O)O	B7	CF3	Cl	Me
4-tBuC(O)O	B8	CF3	H	Me
4-CF3C(O)O	B7	H	CF3	Me
4-CF2CF2CF2C(O)O	B8	H	Cl	Me
4-Me2NC(O)O	B34	Cl	H	Me
4-Et2NC(O)O	H	H	H	Me
4-(nPr)2NC(O)O	B7	OMe	Cl	Me
3-Ph	B8	SMe	Cl	Me
4-Ph	B34	SCF3	Cl	Me
4-(4-F—Ph)	B7	Cl	Cl	Me
4-(4-F—Ph)	B7	CF3	Cl	Me
3-PhO	B7	Cl	Cl	Me
3-PhO	B15	CF3	Cl	Me
4-PhO	B7	Me	Me	Me
4-(4-F—Ph)O	B35	Me	Cl	Me
4-(4-Cl—Ph)O	B36	Cl	Me	Me
4-(4-Br—Ph)O	B7	Cl	Cl	Me
4-(4-Me—Ph)	B8	CF3	Cl	Me
4-(2-Cl—Ph)O	B34	CF3	H	Me
4-(2-F—Ph)O	B40	H	CF3	Me
4-(3-Cl—Ph)O	B41	H	Cl	Me
4-(4-Cl—Ph)O	B42	Cl	H	Me
4-(2,4-Cl2Ph)O	B43	H	H	Me
4-(3,4-Cl2—Ph)O	B44	OMe	Cl	Me
4-(3,4,5-Cl3—Ph)O	COCO2Me	SMe	Cl	Me
4-(2-Me—Ph)O	H	SCF3	Cl	Me
4-(4-Me—Ph)O	B1	Me	Me	Me
4-(3-Cl-4-Me—Ph)O	B2	H	CF3	Me
4-(2-pyridyl)	B3	H	Cl	Me
4-(5-CF3-pyridin-2-yl)	B4	Cl	H	Me
4-(2-pyridyl)O	B7	Cl	Cl	Me
4-(2-pyridyl)O	B15	Cl	Cl	Me
4-(2-pyridyl)O	B7	CF3	Cl	Me
4-(2-pyridyl)O	B8	CF3	Cl	Me
4-(2-pyridyl)O	B34	CF3	Cl	Me
4-(2-pyridyl)O	B5	Cl	Cl	Me
4-(5-CF3-pyridin-2-yl)O	B7	Cl	Cl	Me
4-(5-CF3pyridin-2-yl)O	B8	Cl	Cl	Me
4-(5-CF3pyridin-2-yl)O	B15	CF3	Cl	Me
4-(5-CF2-pyridin-2-yl)O	B7	CF3	Cl	Me
4-(5-CF3-pyridin-2-yl)O	B15	CF3	Cl	Me
4-(5-CF3pyridin-2-yl)O	B34	Me	Cl	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B7	Cl	Cl	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B15	Cl	Cl	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B34	Cl	Cl	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B7	CF3	Cl	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B15	CF3	Cl	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B17	CF3	Cl	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	H	Cl	Cl	Me
4-(5-Cl-thiophen-2-yl)	B8	Cl	Cl	Me
3-OCH2O-4	B9	Cl	Cl	Me
4-OCF2O-4	B10	CF3	Cl	Me
4-MeCH═N	B11	CF3	Cl	Me
4-Me2C═N	B12	CF3	Cl	Me
4-MeEtC═N	H	Cl	Cl	Me
4-PhCH═N	B3	Cl	Cl	Me
4-PhMeC═N	B7	Cl	Cl	Me
4-PhCH2CH═N	B8	CF3	Cl	Me
4-cC6H10═N	B15	CF3	Cl	Me
3-CH2CH2CH2-4	B16	CF3	Cl	Me
3-CH2CH2CH2CH2-4	B28	Cl	Cl	Me
4-PhC(O)	H	Cl	Cl	Me
4-PhC(O)	B7	Cl	Cl	Me
4-PhC(O)	B7	Cl	Cl	Me
4-PhC(O)	B33	CF3	Cl	Me
4-(2-Cl—Ph)C(O)	B7	CF3	Cl	Me
4-(4-F—Ph)C(O)	H	CF3	Cl	Me
4-(4-Cl—Ph)C(O)	B7	Cl	Cl	Me
4-(4-Cl—Ph)C(O)	B15	Cl	Cl	Me
4-(4-Cl—Ph)C(O)	B34	Cl	Cl	Me
4-(4-Me—Ph)C(O)	B3	CF3	Cl	Me
4-(4-Me—Ph)C(O)	B16	CF3	Cl	Me
4-(3,4-Cl2—Ph)C(O)	B45	CF3	Cl	Me
3,4-Cl2	B15	Cl	Cl	Me
3-Cl-4-F	B7	Cl	Cl	Me
2,6-F2	B15	CF3	Cl	Me
3-Cl-4-CF3	B7	CF3	Cl	Me
4-tBu-3-Cl	B7	Cl	Cl	Me
4-tBu-3-Cl	B15	CF3	Cl	Me
4-tBuCH2-3-Cl	B7	Cl	Cl	Me
4-nHep-3-Cl	B15	CF3	Cl	Me
3-Cl-4-iPrO	B7	Cl	Cl	Me
3-Cl-4-iPrO	B7	CF3	Cl	Me
3-Cl-4-nHepO	B15	CF3	Cl	Me
3-Cl-4-(3,4-Cl2—PhCH2)O	H	CF3	Cl	Me
3-Cl-4-PhCH2O	B7	CF3	Cl	Me
3,4-(MeO)2	B16	CF3	Cl	Me
4-MeO-3-Me	B17	CF3	Cl	Me
4-OH-3,5-(tBu)2	B3	CF3	Cl	Me
3,4,5-Cl3b	B15	CF3	Cl	Me
2,6-Cl2-4-CF3	B7	CF3	Cl	Me
2,6-F2-4-CF3	B15	Cl	Cl	Me
2,6-F2-4-CF3O	B7	CF3	Cl	Me
3,5-Cl2-4-tBu	B7	Cl	Cl	Me
3,5-Cl2-4-tBuCH2	B15	CF3	Cl	Me
3,5-Cl2-4-nDec	B7	Cl	Cl	Me
3,5-Cl2-4-PhCH2O	B15	CF3	Cl	Me
2,3,5,6-F4-4-Me	B3	CF3	Cl	Me
2,3,4,5,6-F5	B33	CF3	Cl	Me

TABLE 12
or
G	B	Y1	Y2
2-Cl	H	Me	Me
3-Cl	B1	H	H
4-Cl	B2	Me	H
4-Br	B3	H	Me
4-I	B4	Me	Me
4-F	B5	CF3	Me
4-Me	B6	Cl	Me
4-Et	B7	H	Me
4-iPr	B8	Cl	Me
4-nBu	B9	H	Me
4-iBu	B10	OMe	Me
4-sBu	B11	SMe	Me
4-sBu	H	Me	Me
4-sBu	B16	Et	Me
4-sBu	B17	Cl	Me
4-sBu	B7	Cl	Cl
4-sBu	B8	CF3	Me
4-sBu	B16	Me	CF3
4-sBu	B17	Me	Me
4-sBu	B34	CF3	Me
4-sBu	B3	CF3	Me
4-sBu	B7	CF3	Me
4-sBu	B8	Cl	Me
4-sBu	B34	Me	Cl
4-sBu	B7	H	H
4-sBu	B17	CF3	Me
4-tBu	B12	SCF3	Me
4-tBu	H	Me	Me
4-tBu	B3	Me	Me
4-tBu	B7	Me	Me
4-tBu	B8	Et	Me
4-tBu	B15	Me	nPr
4-tBu	B16	OMe	OMe
4-tBu	B28	Cl	Cl
4-tBu	B30	OCHF2	Me
4-tBu	B34	CF3	CF3
4-tBu	CO—nC8H17	H	H
4-tBu	CO—nC15H31	Cl	Cl
4-tBu	CO2-nHex	Me	Me
4-tBu	CO2—nC10H21	Me	Me
4-tBu	H	CN	Me
4-tBu	H	CF3	Me
4-tBu	B3	CF3	Me
4-tBu	B7	CF3	Me
4-tBu	B8	CF3	Me
4-tBu	B15	CF3	Me
4-tBu	B16	CF3	Me
4-tBu	B28	CF3	Me
4-tBu	B30	CF3	Me
4-tBu	B16	Cl	Cl
4-tBu	B16	CF3	Me
4-tBu	B17	CF3	Me
4-tBu	B17	Me	Me
4-tBu	CO2—nC10H21	CF3	Me
4-tBu	CH2OEt	CF3	Me
4-tBu	B7	Me	CF3
4-tBu	B7	Cl	Cl
4-tBu	B7	CN	Me
4-tBu	B16	CN	Me
4-tBu	B3	CN	Me
4-tBu	2-(4-tBu—Ph)-3,3-Me2—cPrC(O)	CF3	Me
4-tBu	B45	CF3	Me
4-tBuCH2	B3	CF3	Me
4-tBuCH2	B7	Me	Me
4-tBuCH2	B16	Me	Me
4-tBuCH2	B7	CF3	Me
4-tBuCH2	B8	CF3	Me
4-tBuCH2	B7	Cl	Me
4-Et(Me)2C	H	CF3	Me
4-Et(Me)2C	B3	CF3	Me
4-Et(Me)2C	B7	CF3	Me
4-Et(Me)2C	B8	CF3	Me
4-Et(Me)2C	B34	CF3	Me
4-Et(Me)2C	B42	CF3	Me
4-Et(Me)2C	B16	CF3	Me
4-Et(Me)2C	B17	CF3	Me
4-Et(Me)2C	H	Cl	Me
4-Et(Me)2C	B7	Cl	Me
4-Et(Me)2C	B8	Cl	Me
4-Et(Me)2C	B7	Me	CF3
4-Et(Me)2C	B7	CN	Me
4-Et(Me)2C	B4	H	Me
4-Et(Me)2C	B5	Me	Me
4-Et(Me)2C	B6	Me	Me
4-Et(Me)2C	B3	Me	Cl
4-Et(Me)2C	B16	Me	Cl
4-Et(Me)2C	B17	Me	Cl
4-Et(Me)2C	B24	Me	Cl
4-nHex	B34	CF3	Me
4-nHep	B42	CF3	Me
4-nOct	B43	Me	Me
4-nNon	B43	Me	Me
4-nDec	H	Cl	Me
4-(Me)2(CN)C	B7	Cl	Me
4-PhCH2	B7	CF3	Me
4-Ph(Me)2C	B7	CF3	Me
4-(4-F—Ph)(Me)2C	B7	CN	Me
4-MeCH═CH	B4	H	Me
4-MeCC	B5	Cl	Me
3-CF3	B6	H	Me
4-CF3	B7	OMe	Me
4-CF3	B8	SMe	Me
4-CF3	B9	SCF3	Me
4-CF3	B16	Me	Me
4-CF3	B17	Me	Me
4-CF3	B16	Me	Me
4-CF3	B17	Cl	Me
4-CF3	B7	Cl	Me
4-CF3	B7	CF3	Me
4-CF3	B7	Me	Me
4-CF3	B3	Cl	Me
4-CF3CH2	B7	Me	Me
4-Cl2C═CHCH2	B8	Cl	Me
4-BrCC	B7	Cl	Me
4-(2,2-F2)cBuCH2	B7	CF3	Me
4-(1-Me)cPr	B16	CN	Me
4-cHex	B7	CF3	Me
4-(1-Me)cHex	B8	CF3	Me
4-MeO	B7	CF3	Me
4-iPrO	B7	Cl	Me
4-iPrO	B7	CF3	Me
4-iPrO	B15	CF3	Me
4-iPrO	B7	Me	Me
4-iPrO	B16	Me	Me
4-iPrO	B17	Me	Me
4-iPrO	B23	SCF3	Me
4-tBuO	B7	Me	Me
4-tBuO	B8	CF3	Me
4-tBuO	B7	CF3	Me
4-nHexO	B8	CF3	Me
4-nOctO	B34	CF3	Me
4-nDecO	H	CF3	Me
4-CH2═CHCH2O	B7	CF3	Me
4-CHCCH2O	B8	CF3	Me
4-CHF2O	B34	CF3	Me
4-CHF2O	B7	Et	Me
4-CHF2O	B35	Me	Me
4-CHF2O	B36	Cl	Me
4-CHF2O	B7	CF3	Me
4-CBrF2O	B8	Cl	Me
4-CBrF2O	B34	Cl	Me
4-CBrF2O	B40	Me	Me
4-CBrF2O	B41	Me	Me
4-CBrF2O	B42	Cl	Me
4-CBrF2O	B7	CF3	Me
4-CBrF2O	B8	CF3	Me
4-CBrF2O	COCO2Me	CF3	Me
4-CBrF2O	H	H	Me
4-CBrF2O	B1	CF3	Me
4-CF3O	B2	Cl	Me
4-CF3O	B3	H	Me
4-CF3O	B4	OMe	Me
4-CF3O	B5	SMe	Me
4-CF3O	B6	SCF3	Me
4-CF3O	B7	CF3	Me
4-CF3CH2O	B8	Me	Me
4-CF2═CHCH2CH2O	B9	Me	Me
4-CCl2═CHCH2O	B10	Cl	Me
4-ClCCCH2O	B11	Cl	Me
4-MeS	B12	CF3	Me
4-sBuS	H	CF3	Me
4-EtSO	B3	H	Me
4-MeSO2	H	CF3	Me
4-MeSO2	B3	CF3	Me
4-MeSO2	B32	CF3	Me
4-MeSO2	B33	CF3	Me
4-EtSO2	H	CF3	Me
4-EtSO2	B3	Et	Me
4-iPrSO2	B32	CF3	Me
4-iPrSO2	B33	CF3	Me
4-tBuSO2	B7	CF3	Me
4-tBuSO2	B33	CF3	Me
4-MeCH═CHCH2S	B15	H	Me
4-CH2═CHCH2SO	B16	OMe	Me
4-CH2═CHCH2SO2	B28	SMe	Me
4-CHCCH2S	B30	SCF3	Me
4-CHCCH2SO	B34	Me	Me
4-CHCCH2SO2	CO—nC8H17	Me	Me
4-CHF2S	H	CF3	Me
4-CHF2S	B7	CF3	Me
4-CHF2S	B8	CF3	Me
4-CHF2S	B15	CF3	Me
4-CHF2S	B29	CF3	Me
4-CHF2S	H	Me	Me
4-CHF2S	B7	Me	Me
4-CHF2S	B15	Me	Me
4-CBrF2S	B7	Me	CF3
4-CBrF2S	B15	Me	CF3
4-CBrF2S	B30	Me	CF3
4-CBrF2S	B43	Me	CF3
4-CBrF2S	CO—nC15H31	nPr	Me
4-CBrF2S	CO2-nHex	CF3	Me
4-CBrF2S	H	CF3	Me
4-CBrF2S	B7	CF3	Me
4-CBrF2S	B8	CF3	Me
4-CBrF2S	B15	CF3	Me
4-CBrF2S	B28	CF3	Me
4-CBrF2S	B34	CF3	Me
4-CBrF2S	B7	Me	Me
4-CF3S	CO2—nC10H21	Cl	Me
4-CF3S	H	Me	Me
4-CF3S	B3	Me	Me
4-CF3S	B7	Me	Me
4-CF3S	B8	Me	Me
4-CF3S	B15	Me	Me
4-CF3S	H	CF3	Me
4-CF3S	B7	CF3	Me
4-CF3S	B8	CF3	Me
4-CF3S	B15	CF3	Me
4-CF3S	B34	CF3	Me
4-CF3S	CO2—nC12H25	CF3	Me
4-CF3S	CO—nC15H31	CF3	Me
4-CF3S	CO—nC16H33	Me	Me
4-CF3S	CO—nC17H35	Me	Me
4-CF3CH2S	CO—nC16H37	CF3	Me
4-CHF2CF2S	CO—nC19H39	CF3	Me
4-CHF2SO	CO—nC20H41	Cl	Cl
4-CBrF2SO	H	H	Me
4-CBrF2SO	B3	CF3	Me
4-CBrF2SO	B7	CF3	Me
4-CBrF2SO	B24	CF3	Me
4-CBrF2SO	B32	CF3	Me
4-CBrF2SO	B33	CF3	Me
4-CF3SO	H	Me	Me
4-CF3SO	B3	Me	Me
4-CF3SO	B7	Me	Me
4-CF3SO	B33	Me	Me
4-CF3CH2SO2	B15	H	Me
4-CHF2CF2SO2	B16	OMe	Me
4-CHF2SO2	B28	SMe	Me
4-CHF2SO2	B7	CF3	Me
4-CHF2SO2	B24	CF3	Me
4-CHF2SO2	B32	CF3	Me
4-CHF2SO2	B33	CF3	Me
4-CHF2SO2	H	Me	Me
4-CHF2SO2	B3	Me	Me
4-CHF2SO2	B7	Me	Me
4-CHF2SO2	B33	Me	Me
4-CBrF2SO2	H	SCF3	Me
4-CBrF2SO2	B2	Me	Me
4-CBrF2SO2	B3	Me	Me
4-CBrF2SO2	B18	Me	Me
4-CBrF2SO2	B19	Me	Me
4-CBrF2SO2	B33	Me	Me
4-CBrF2SO2	H	CF3	Me
4-CBrF2SO2	B3	CF3	Me
4-CBrF2SO2	B7	CF3	Me
4-CBrF2SO2	B20	CF3	Me
4-CBrF2SO2	B32	CF3	Me
4-CBrF2SO2	B33	CF3	Me
4-CBrF2SO2	B37	CF3	Me
4-CBrF2SO2	B7	Me	CF3
4-CBrF2SO2	B15	Me	CF3
4-CBrF2SO2	B17	Me	CF3
4-CBrF2SO2	B7	Me	CF3
4-CBrF2SO2	B16	Me	CF3
4-CF3SO2	B16	Me	Me
4-CF3SO2	B7	Cl	Me
4-CF3SO2	B15	Cl	Cl
4-CF3SO2	B3	CF3	Me
4-CF3SO2	B7	CF3	Me
4-CF3SO2	B15	Me	Me
4-CF3SO2	B7	Me	Me
4-CF3SO2	B8	Me	Me
4-Cl2C═CHCH2S	B16	Me	Me
4-Cl2C═CHCH2SO	B17	Me	Me
4-Cl2C═CHCH2SO2	B17	Cl	Me
4-CBrCCH2S	CO2—nC10H21	Cl	Me
4-CBrCCH2SO	B33	CF3	Me
4-CBrCCH2SO2	B7	CF3	Me
4-CHO	B7	H	Me
4-NO2	B8	H	Me
4-CN	B16	Cl	Me
4-(Me)2N	B3	H	Me
4-Me(MeCO)N	B7	OMe	Me
4-PhMeN	B8	SMe	Me
4-PhCH2(MeCO)N	B15	SCF3	Me
4-(1-naphthyl)	B16	Me	Me
4-(2-naphthyl)	B28	Me	Me
4-(2-Cl—Ph)CH2O	B30	Me	Me
4-(3-Cl—Ph)CH2O	B34	Cl	Me
4-(4-Cl—Ph)CH2O	B7	CF3	Me
4-(4-Cl—Ph)CH2O	B7	Cl	Me
4-(4-Cl—Ph)CH2O	B37	Cl	Me
4-(4-F—Ph)CH2O	B42	CF3	Me
4-(2-Me—Ph)CH2O	B43	CF3	Me
4-(4-Me—Ph)CH2O	B43	CF3	Me
4-(4-Et—Ph)CH2O	H	CF3	Me
3-(2,4-Cl2—Ph)CH2O	B7	CF3	Me
4-(3,4-Cl2—Ph)CH2O	B7	H	Me
4-(2,5-Me2—Ph)CH2O	B7	OMe	Me
4-(2,3,4,5,6-F5—Ph)CH2O	B7	SMe	Me
4-MeOC(O)	B4	SCF3	Me
4-EtOC(O)	B5	Me	Me
4-nPrOC(O)	B6	Me	Me
4-iPrOC(O)	B7	Me	Me
4-tBuOC(O)	B7	Me	Me
4-tBuOC(O)	B3	CF3	Me
4-tBuOC(O)	B5	CF3	Me
4-tBuOC(O)	B33	CF3	Me
4-tBuOC(O)	H	CF3	Me
4-tBuOC(O)	B7	CF3	Me
4-tBuOC(O)	B8	CF3	Me
4-tBuOC(O)	B34	CF3	Me
4-tBuCH2OC(O)	B10	CF3	Me
4-Et(Me)2COC(O)	B11	CF3	Me
4-nHexOC(O)	B7	H	Me
4-MeOCH2	B8	H	Me
4-EtOCH2	B7	Cl	Me
4-iPrOCH2	B7	H	Me
4-MeC(O)	B16	OMe	Me
4-EtC(O)	B7	SMe	Me
4-iPrC(O)	B8	SCF3	Me
4-tBuC(O)	H	Cl	Cl
4-tBuC(O)	B3	Cl	Cl
4-tBuC(O)	B7	Cl	Cl
4-tBuC(O)	B3	CF3	Me
4-tBuC(O)	B7	CF3	Me
4-tBuC(O)	B15	CF3	Me
4-tBuC(O)	B7	Me	Me
4-tBuC(O)	B17	Me	Me
4-tBuC(O)	B16	Me	Me
4-CF3C(O)	B33	Me	Me
4-CF3CF2C(O)	B8	Me	Me
4-CF2CF2CF2C(O)	B22	Cl	Me
4-MeC(O)O	B23	Cl	Me
4-iPrC(O)O	B7	CF3	Me
4-tBuC(O)O	B8	CF3	Me
4-CF3C(O)O	B7	H	Me
4-CF2CF2CF2C(O)O	B8	H	Me
4-Me2NC(O)O	B34	Cl	Me
4-Et2NC(O)O	H	H	Me
4-(nPr)2NC(O)O	B7	OMe	Me
3-Ph	B8	SMe	Me
4-Ph	B34	SCF3	Me
4-(4-F—Ph)	B7	Et	Me
4-(4-F—Ph)	B7	CF3	Me
3-PhO	B7	Me	Me
3-PhO	B15	CF3	Me
4-PhO	B7	Me	Me
4-(4-F—Ph)O	B35	Me	Me
4-(4-Cl—Ph)O	B36	Et	Me
4-(4-Br—Ph)O	B7	CF3	Me
4-(4-Me—Ph)	B8	CF3	Me
4-(2-Cl—Ph)O	B34	CF3	Me
4-(2-F—Ph)O	B40	H	Me
4-(3-Cl—Ph)O	B41	H	Me
4-(4-Cl—Ph)O	B42	Cl	Me
4-(2,4-Cl2—Ph)O	B43	H	Me
4-(3,4-Cl2—Ph)O	B44	OMe	Me
4-(3,4,5-Cl3—Ph)O	COCO2Me	SMe	Me
4-(2-Me—Ph)O	H	SCF3	Me
4-(4-Me—Ph)O	B1	Me	Me
4-(3-Cl-4-Me—Ph)O	B2	H	Me
4-(2-pyridyl)	B3	H	Me
4-(5-CF3-pyridin-2-yl)	B4	Cl	Me
4-(2-pyridyl)O	B7	Me	Me
4-(2-pyridyl)O	B15	Me	Me
4-(2-pyridyl)O	B7	CF3	Me
4-(2-pyridyl)O	B8	CF3	Me
4-(2-pyridyl)O	B34	CF3	Me
4-(2-pyridyl)O	B5	CF3	Me
4-(5-CF3-pyridin-2-yl)O	B7	Me	Me
4-(5-CF3-pyridin-2-yl)O	B8	Me	Me
4-(5-CF3-pyridin-2-yl)O	B15	CF3	Me
4-(5-CF3-pyridin-2-yl)O	B7	CF3	Me
4-(5-CF3-pyridin-2-yl)O	B15	CF3	Me
4-(5-CF3-pyridin-2-yl)O	B34	CF3	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B7	Me	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B15	Me	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B34	Me	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B7	CF3	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B15	CF3	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	B17	CF3	Me
4-(3-Cl-5-CF3-pyridin-2-yl)	H	CF3	Me
4-(5-Cl-thiophem-2-yl)	B8	Cl	Me
3-OCH2O-4	B9	Cl	Me
4-OCF2O-4	B10	CF3	Me
4-MeCH═N	B11	CF3	Me
4-Me2C═N	B12	CF3	Me
4-MeEtC═N	H	Cl	Me
4-PhCH═N	B3	Cl	Me
4-PhMeC═N	B7	Cl	Me
4-PhCH2CH═N	B8	CF3	Me
4-cC6H10═N	B15	CF3	Me
3-CH2CH2CH2-4	B16	CF3	Me
3-CH2CH2CH2CH2-4	B28	Cl	Me
4-PhC(O)	H	CF3	Me
4-PhC(O)	B7	Et	Me
4-PhC(O)	B7	CF3	Me
4-PhC(O)	B33	CF3	Me
4-(2-Cl—Ph)C(O)	B7	CF3	Me
4-(4-F—Ph)C(O)	H	CF3	Me
4-(4-Cl—Ph)C(O)	B7	CF3	Me
4-(4-Cl—Ph)C(O)	B15	CF3	Me
4-(4-Cl—Ph)C(O)	B34	CF3	Me
4-(4-Me—Ph)C(O)	B3	CF3	Me
4-(4-Me—Ph)C(O)	B16	CF3	Me
4-(3,4-Cl2—Ph)C(O)	B45	CF3	Me
2,4-Cl2	B7	CF3	Me
3,4-Cl2	B7	CF3	Me
4-Cl-2-F	B7	CF3	Me
3-Cl-4-nHex	B7	CF3	Me
4-tBu-3-Cl	B7	CF3	Me
4-tBu-3-Cl	B15	CF3	Me
3-Cl-4-iPrO	B7	Me	Me
3-Cl-4-iPrO	B7	CF3	Me
3-Cl-4-nHepO	B15	CF3	Me
3-Cl-4-(3,4-Cl2—PhCH2)O	H	CF3	Me
3-Cl-4-PhCH2O	B7	CF3	Me
3-Cl-4-Me3CCH2	B7	CF3	Me
3,4-(MeO)2	B7	CF3	Me
4-MeO-3-Me	B17	CF3	Me
4-OH-3,5-(tBu)2	B3	CF3	Me
3,4,5-Cl3	B15	CF3	Me
3,5-Cl2-4-F	B7	CF3	Me
4-Cl-2,6-F2	B7	CF3	Me
2,6-F2-4-CF3	B7	CF3	Me
2,6-F2-4-CF3O	B7	CF3	Me
3,5-Cl2-4-nOct	B7	CF3	Me
3,5-Cl2-4-PhCH2O	B15	CF3	Me
2,3,5,6-F4-Me	B3	CF3	Me
2,3,4,5,6-F5	B33	CF3	Me

TABLE 13
	R1	B	A
	iPr	H	2,5-Me2-1-pyrrolyl
	iPr	B3	1-Me-2-pyrrolyl
	tBu	B5	3,5-Me2-2-pyrrolyl
	tBu	B6	3,4-Me2-2-pyrrolyl
	tBu	B7	3,4,5-Me3-2-pyrrolyl
	1-Me-cPr	B8	3,5-Me2-4-MeO-2-pyrrolyl
	1-Me-cPr	B15	4-MeC(O)-3,5-Me2-2-pyrrolyl
	1-Me-cPr	B16	4-NO2-pyrrolyl
	1-Me-cPr	B17	2-Me-3-pyrrolyl
	1-Me-cHex	B22	4-Me-3-pyrrolyl
	1-Me-cHex	B31	2,4,5-Me33-pyrrolyl
	1-Me-cHex	B32	2,4-Me2-5-EtO2C-3-pyrrolyl
	1-Me-cHex	B33	1,2,3-triazol-4-yl
	PhCH2	B34	1-Me-1,2,3-triazol-4-yl
	PhCH2	B35	2-Me-1,2,3-triazol-4-yl
	PhCH2	B36	3-Me-1,2,3-triazol-4-yl
	PhMe2C	B40	2-EtO2C-1,2,3-triazol-4-yl
	PhMe2C	B41	5-Me-2-Ph-1,2,3-triazol-4-yl
	PhMe2C	pyridin-2-yl-C(O)	5-CF3-2-Me-1,2,3-triazol-4-yl
	PhMe2C	pyridin-2-yl-C(O)	2,5-Me2-1,2,3-triazol-4-yl
	Ph	pyridin-2-yl-C(O)	1-PhCH2-5-Me-1,2,3-trizol-4-yl
	2-F—Ph	H	1-PhCH2-5-CF3-1,2,3-trizol-4-yl
	2-F—Ph	B3	1-PhCH2-5-Cl-1,2,3-trizol-4-yl
	2-F—Ph	B5	4-Me-1,2,3-triazol-1-yl
	2-F—Ph	B6	5-Me-1,2,3-triazol-2-yl
	2-Cl—Ph	B7	4-MeO2C-1,2,3-triazol-1-yl
	2-Cl—Ph	B8	4,5-EtO2C-1,2,3-trizaol-2-yl
	2-Cl—Ph	B15	4,5-Me2-1,2,3-triazol-1-yl
	2-Me—Ph	B16	4,5-(MeO2C)2-1,2,3-triazol-2-yl
	2-Me—Ph	B17	4,5-Me2-1,2,4-triazol-3-yl
	2-Me—Ph	B22	2,4-Me2-1,2,4-triazol-3-yl
	4-NO2—Ph	B31	1,5-Me2-1,2,4-trizo1-3-yl
	2,6-F2—Ph	B32	5-Me-3-CF3-1,2,4-triazol-2-yl
	2,6-F2—Ph	B33	3-Cl-5-CF3-1,2,4-triazol-2-yl
	2,6-F2—Ph	B34	5-Cl-3-CF3-1,2,4-triazol-2-yl
	2,6-F2—Ph	B35	3,5-Me31,2-4-triazol-4-yl
	2,6-F2—Ph	B36	3,5-Cl2-1,2-4-triazol-4-yl
	2,6-Cl2—Ph	B40	3,5-(CF3)2-1,2-4-triazol-4-yl
	2,6-Cl2—Ph	B41	5-tetrazolyl
	2,6-Cl2—Ph	pyridin-2-yl-C(O)	5-Ph-1-tetrazolyl
	2,6-Cl2—Ph	pyridin-2-yl-C(O)	5-Ph-2-tetrazolyl
	2-pyridyl	pyridin-2-yl-C(O)	3,4,4,5-Me4-2-pyrazolin-1-yl
	2-pyridyl	B8	3-Me-5-CF3-2-pyrazolin-1-yl
	2-pyridyl	B15	1,5-Me2-3-CF3-2-pyrazolin-4-yl
	2-pyridyl	B16	1,4-Me2-3-Ph-2-pyrazolin-4-yl
	2-pyridyl	B17	1,4-Me2-5-Ph-2-pyrazolin-4-yl
	2-pyridyl	B22	1,3-Me2-2-pyrazolin-5-yl
	1-naphthyl	B31	1,5-Me2-2-pyrazolin-3-yl
	1-naphthyl	B32	2-Me-2-imizolin-1-yl
	1-naphthyl	B33	2-CF3-2-imizolin-1-yl
	iPr	B34	2-MeS-2-imizolin-1-yl
	iPr	B35	2-MeO-2-imizolin-1-yl
	tBu	B36	5-Me-2-Ph-2-oxazolin-4-yl
	1-Me—cPr	B40	2,5-Me2-2-oxazolin-4-yl
	cHex	B41	5-Me-2-CF3-2-oxazolin-4-yl
	1-Me-cHex	pyridin-2-yl-C(O)	2-thiazolin-2-yl
	PhCH2	pyridin-2-yl-C(O)	2-Me2N-2-thiazolin-4-yl
	PhMe2C	pyridin-2-yl-C(O)	2,4-Me2-2-thiazolin-5-yl
	Ph	B8	2-Me-4-CF3-2-thiazolin-5-yl
	2-F—Ph	B15	5-Me-2-isoxazolin-3-yl
	2-Cl—Ph	B16	3-Cl-5-Me-2-isoxazolin-4-yl
	2-Me—Ph	B17	3,5-(MeS)2-2-isothiazolin-4-yl
	4-NO2—Ph	B22	5-Cl-2-Me-3(2H)-pyridazinon-4-yl
	2,6-F2—Ph	B31	5,6-Cl2-2-Me-pyridazinon-4-yl
	2,6-Cl2—Ph	B32	4-Cl-2-Me-pyridazinon-4-yl
	2-pyridyl	B33	4,6-Cl2-2-Me-pyridazinon-4-yl
	1-naphthyl	B34	4,5-Cl2-2-Me-pyridazinon-4-yl

TABLE 14
	R1	E	B	A
	tBu	oxazol-2-yl	H	A1
	tBu	thiazol-2-yl	B3	A2
	tBu	imidazol-2-yl	B7	A3
	tBu	1,5-Me2-1,2,4-triazol-3-yl	B8	A4
	tBu	5-Me-1,2,4-oxadiazol-3-yl	B15	A5
	tBu	5-CF3-1,2,4-thiadiazol-3-yl	B16	A6
	tBu	5-Me-1,3,4-oxadiazol-2-yl	B17	A7
	tBu	tetrazol-5-yl	B18	A8
	tBu	2-oxazolin-2-yl	B32	A9
	tBu	1,2,4,5-tetrazin-3-yl	B33	A10
	tBu	F	B34	A11
	tBu	Cl	H	A12
	tBu	Br	B7	A13
	tBu	I	B8	A14
	tBu	CHC	H	A15
	tBu	CHC	B7	A2
	2,6-F2—Ph	CHC	B7	A2
	tBu	MeCC	B7	A16
	tBu	EtCC	B7	A17
	tBu	PhCC	B7	A2
	tBu	PhCC	B8	A13
	2,6-F2—Ph	PhCC	H	A2
	2,6-F2—Ph	PhCC	B7	A2
	pyridin-2-yl	PhCC	B7	A2
	tBu	(2-Cl—Ph)CC	B15	A19
	tBu	(3-Cl—Ph)CC	B15	A20
	2,6-F2—Ph	(4-Cl—Ph)CC	B16	A21
	2,6-F2—Ph	(4-F—Ph)CC	B17	A22
	2,6-F2—Ph	(4-Me—Ph)CC	B18	A23
	2,6-F2—Ph	(4-nHex-Ph)CC	B34	A24
	2,6-F2—Ph	(2,6-Cl2—Ph)CC	H	A25
	2,6-F2—Ph	(2,4-Cl2—Ph)CC	(EtO)2P(S)	A26
	2,6-F2—Ph	(3,4-Cl2—Ph)CC	B3	A27
	2,6-F2—Ph	(2,4,6-Me3—Ph)CC	B7	A28
	2,6-F2—Ph	(4-CF3—Ph)CC	B15	A29
	2,6-F2—Ph	CF3	B7	A2
	2,6-F2—Ph	CF3CF2	H	A31
	2,6-F2—Ph	NO2	B3	A32
	2,6-F2—Ph	N3	B7	A33
	2,6-F2—Ph	N3	H	A2
	2,6-F2—Ph	N3	B7	A1
	tBu	N3	B7	A2
	tBu	N3	H	A2
	pyridin-2-yl	N3	B7	A2
	2,6-F2—Ph	CHO	B8	A34
	2,6-F2—Ph	C(O)Me	B15	A35
	2,6-F2—Ph	C(O)Et	B16	A36
	2,6-F2—Ph	C(O)iPr	B17	A1
	2,6-F2—Ph	C(O)nBu	B18	A2
	2,6-F2—Ph	C(O)sBu	B32	A3
	2,6-F2—Ph	C(O)tBu	H	A2
	2,6-F2—Ph	C(O)tBu	H	A1
	2,6-F2—Ph	C(O)tBu	B7	A1
	tBu	C(O)tBu	H	A2
	tBu	C(O)tBu	B7	A2
	tBu	CO2Me	H	A2
	tBu	CO2Me	B7	A2
	tBu	CO2Me	B8	A2
	2,6-F2—Ph	CO2Me	H	A2
	2,6-F2—Ph	CO2Me	B7	A2
	2,6-F2—Ph	CO2Me	B8	A2
	pyridin-2-yl	CO2Me	H	A2
	pyridin-2-yl	CO2Me	B7	A2
	pyridin-2-yl	CO2Me	B8	A2
	tBu	CO2Me	B34	A5
	tBu	CO2Et	H	A2
	tBu	CO2Et	B7	A2
	tBu	CO2Et	B8	A2
	2,6-F2—Ph	CO2Et	H	A2
	2,6-F2—Ph	CO2Et	B7	A2
	2,6-F2—Ph	CO2Et	B8	A2
	pyridin-2-yl	CO2Et	H	A2
	pyridin-2-yl	CO2Et	B7	A2
	pyridin-2-yl	CO2Et	B8	A2
	pyridin-2-yl	CO2Et	H	A6
	pyridin-2-yl	CO2nPr	B7	A7
	pyridin-2-yl	CO2iPr	B8	A8
	pyridin-2-yl	CO2nBu	H	A9
	pyridin-2-yl	CO2iBu	B7	A10
	pyridin-2-yl	CO2sBu	B7	A11
	pyridin-2-yl	CO2tBu	B8	A12
	pyridin-2-yl	CO2CH2CH═CH2	B15	A13
	pyridin-2-yl	CO2CH2CH═CH2	B7	A2
	tBu	CO2CH2CH═CH2	B8	A2
	tBu	CO2CH2CH═CH2	H	A2
	tBu	CO2CH2CH═CH2	B7	A2
	2,6-F2—Ph	CO2CH2CH═CH2	B8	A2
	2,6-F2—Ph	CO2CH2CH═CH2	H	A2
	2,6-F2—Ph	CO2CH2CH═CH2	B7	A2
	pyridin-2-yl	C(O)NHMe	B8	A2
	2,6-F2—Ph	C(O)NHMe	H	A2
	tBu	C(O)NHMe	H	A2
	pyridin-2-yl	C(O)NHEt	B16	A15
	pyridin-2-yl	C(O)NHnPr	B17	A16
	tBu	C(O)NHiPr	B18	A17
	tBu	C(O)NHiBu	B34	A18
	tBu	C(O)NHtBu	H	A19
	tBu	C(O)NMe2	(EtO)2P(S)	A20
	tBu	C(O)NMe2	H	A2
	tBu	C(O)NMe2	B7	A2
	2,6-F2—Ph	C(O)NMe2	B7	A2
	pyridin-4-yl	C(O)NMeEt	B3	A21
	2,6-F2—Ph	C(O)NEt2	B7	A22
	tBu	C(O)N(nPr)2	B15	A23
	tBu	PhC(O)	H	A24
	tBu	PhC(O)	H	A2
	tBu	PhC(O)	B7	A2
	tBu	PhC(O)	B8	A2
	2,6-F2—Ph	PhC(O)	H	A2
	2,6-F2—Ph	PhC(O)	B7	A2
	2,6-F2—Ph	PhC(O)	B8	A2
	pyridin-2-yl	PhC(O)	H	A2
	pyridin-2-yl	PhC(O)	B7	A2
	2,6-F2—Ph	(4-F—Ph)C(O)	B8	A2
	2,6-F2—Ph	(3,4-Cl2—Ph)C(O)	H	A6
	pyridin-3-yl	(3-Cl-4-F—Ph)C(O)	B8	A27
	pyridin-3-yl	(4-Me—Ph)C(O)	B15	A28
	tBu	C(S)NH2	B16	A29
	tBu	C(S)NH2	H	A2
	tBu	C(S)NH2	B7	A2
	2,6-F2—Ph	C(S)NH2	B8	A2
	2,6-F2—Ph	C(S)NH2	H	A2
	2,6-F2—Ph	C(S)NH2	B7	A2
	pyridin-2-yl	C(S)NH2	B8	A2
	pyridin-2-yl	C(S)NH2	H	A2
	2,6-F2—Ph	MeS	B7	A2
	2,6-F2—Ph	EtS	B18	A31
	pyridin-2-yl	nPrS	B32	A32
	pyridin-2-yl	tBuS	B33	A33
	tBu	MeSO	B34	A34
	tBu	EtSO	H	A35
	tBu	nPrSO	B7	A36
	2,6-F2—Ph	tBuSO	B8	A1
	2,6-F2—Ph	MeSO2	H	A2
	2,6-F2—Ph	EtSO2	B7	A3
	pyridin-2-yl	iPrSO2	B7	A4
	pyridin-2-yl	nBuSO2	B8	A5
	tBu	PhS	B15	A6
	tBu	PhS	H	A2
	tBu	PhS	B7	A2
	2,6-F2—Ph	PhS	B8	A2
	2,6-F2—Ph	PhS	H	A2
	2,6-F2—Ph	PhS	B7	A2
	pyridin-2-yl	PhS	B8	A2
	pyridin-2-yl	PhS	H	A2
	pyridin-2-yl	PhS	B7	A2
	tBu	(4-Me—Ph)S	B8	A2
	tBu	(4-Cl—Ph)SO	H	A6
	tBu	(2-F—Ph)SO2	B17	A9
	2,6-F2—Ph	(MeO)2P(O)	B18	A10
	2,6-F2—Ph	(EtO)2P(O)	B34	A11
	2,6-F2—Ph	(nPrO)2P(O)	H	A12
	pyridin-2-yl	(PhO)(MeO)P(O)	(EtO)2P(S)	A13
	pyridin-2-yl	(MeO)2P(S)	B3	A14
	tBu	(EtO)2P(S)	B7	A15
	tBu	(nPrO)2P(S)	B15	A16
	tBu	(PhO)(MeO)P(S)	B7	A17

Where the compounds of the present invention are used as pesticides, in general, they can be mixed with a suitable carrier, for example a solid carrier, such as clay, talc, bentonite, diatomaceous earth or white carbon, or a liquid carrier such as water, alcohols (e.g., isopropanol, butanol, benzyl alcohol, furfuryl alcohol), aromatic hydrocarbons (e.g., toluene, xylene), ethers (e.g., anisole), ketones (e.g., cyclohexanone, isophorone), esters (e.g., butyl acetate), acid amides (e.g., N-methylpyrrolidone) or halogenated hydrocarbons (e.g., chlorobenzene), optionally along with other additives such as surfactant, emulsifier, dispersing agent, penetrating agent, spreading agent, thickener, anti-freezing agent, anti-caking agent and stabilizer, and can be formulated into any desired forms for practical use, such as liquid preparations, emulsions, wettable powders, dry flowables, flowables, dusts and granules.

Where the compounds of the present invention are used as agricultural chemicals, they can be combined with any other herbicides, various insecticides, acaricides, nematecides, fungicides, plant growth regulators, synergists, fertilizer and soil improvers, when they are formulated into preparations for practical use or while they are actually used through spraying or the like.

In particular, the combination of the compounds of the invention and other agricultural chemicals or plant hormones will be advantageous in that the amount of the chemicals to be used can be reduced thereby resulting in the reduction of the costs for the treatment, and that the mixed chemicals exhibit synergistic effects to broaden the insecticidal spectrum while displaying higher pesticidal activities. If desired, the compounds of the invention can be combined with a plurality of known agricultural chemicals. For the agricultural chemicals capable of being combined with the compounds of the invention, for example, the compounds described in Farm Chemicals Handbook, 1994 are referred.

Their concrete general names are raised below. However, the present invention is not necessarily limited by them. Fungicide: acibenzolar, ampropylos, anilazine, azaconazole, azoxystrobin, benalaxyl, benodanil, benomyl, benzamacril, binapacryl, biphenyl, bitertanol, bethoxazine, bordeaux mixture, blasticidin-S, bromoconazole, bupirimate, buthiobate, calcium polysulfide, captafol, captan, copper oxychloride, carpropamid, carbendazim, carboxin, chinomethionat, chlobenthiazone, chlorfenazol, chloroneb, chlorothalonil, chlozolinate, cufraneb, cymoxanil, cyproconazol, cyprodinil, cyprofuram, debacarb, dichlorophen, diclobutrazol, dichlofluanid, diclomezine, dicloran, diethofencarb, diclocymet, difenoconazole, diflumetorim, dimethirimol, dimethomorph, diniconazole, diniconazole-M, dinocap, diphenylamine, dipyrithione, ditalimfos, dithianon, dodemorph, dodine, drazoxolon, edifenphos, epoxiconazole, etaconazole, ethirimol, etridiazole, famoxadone, fenarimol, febuconazole, fenfuram, fenpiclonil, fenpropidin, fenpropimorph, fentin, ferbam, ferimzone, fluazinam, fludioxonil, fluoroimide, fluquinconazole, flusilazole, flusulfamide, flutolanil, flutriafol, folpet, fosetyl-aluminium, fuberidazole, furalaxyl, fenamidone, fenhexamid, guazatine, hexachlorobenzene, hexaconazole, hymexazol, imazalil, imibenconazole, iminoctadine, ipconazole, iprobenfos, iprodione, isoprothiolane, iprovalicarb, kasugamycin, kresoxim-methyl, mancopper, mancozeb, maneb, mepanipyrim, mepronil, metalaxyl, metconazole, metiram, metominostrobin, myclobutanil, nabam, nickel bis(dimethyldithiocarbamate), nitrothal-isopropyl, nuarimol, octhilinone, ofurace, oxadixyl, oxycarboxin, oxpoconazole fumarate, pefurzoate, penconazole, pencycuron, phthalide, piperalin, polyoxins, probenazole, prochloraz, procymidone, propamocarb hydrochloride, propiconazole, propineb, pyrazophos, pyrifenox, pyrimethanil, pyroquilon, quinoxyfen, quintozene, sulfur, spiroxamine, tebuconazole, tecnazene, tetraconazole, thiabendazole, thifluzamide, thiophanate-methyl, thiram, tolclofos-methyl, tolylfluanid, triadimefon, toriadimenol, triazoxide, tricyclazole, tridemorph, triflumizole, triforine, triticonazole, validamycin, vinclozolin, zineb, ziram.

Bacteriazide: streptomycin, oxyterracycline, oxolinic acid.

Nematicide: aldoxycarb, cadusafos, fosthiazate, fosthietan, oxamyl, fenamiphos.

Acaricide: acequinocyl, acrinathrin, amitraz, bifenazate, bromopropylate, chinomethionat, chlorobezilate, clofentezine, cyhexatine, dicofol, dienochlor, etoxazole, fenazaquin, fenbutatin oxide, fenpropathrin, fenproximate, halfenprox, hexythiazox, milbemectin, phenisobromolate, polynactins, propargite, pyridaben, pyrimidifen, tebufenpyrad, tetradifon.

Insecticide: abamectin, acephate, acetamipirid, alanycarb, azinphos-methyl, bendiocarb, benfuracarb, bensultap, bifenthrin, Batillus thuringiensis, buprofezin, butocarboxim, carbaryl, carbofuran, carbosulfan, cartap, chlorfenapyr, chlorpyrifos, chlorfenvinphos, chlorfluazuron, clothianidin, chromafenozide, chlorpyrifos-methyl, cyanox, cycloprothrin, cyfluthrin, beta-cyfluthrin, cypermethrin, cyromazine, cyhalothrin, lambda-cyhalothrin, deltamethrin, diafenthiuron, diazinon, diacloden, dichlorvos, diflubenzuron, dimethylvinphos, diofenolan, disulfoton, dimethoate, emamectin-benzoate, EPN, esfenvalerate, ethiofencarb, endosulfan, ethiprole, ethylthiometone, etofenprox, etrimfos, fenitrothion, fenobucarb, fenothiocarb, fenthion, fenoxycarb, fenpropathrin, fenvalerate, fipronil, flucythrinate, flufenoxuron, flufenprox, tau-fluvalinate, fonophos, formetanate, formothion, furathiocarb, halofenozide, hexaflumuron, hydramethylnon, imidacloprid, isofenphos, indoxacarb, isoprocarb, isoxathion, lufenuron, malathion, metaldehyde, methamidophos, methidathion, methacrifos, metalcarb, methomyl, methoprene, methoxychlor, methoxyfenozide, monocrotophos, muscalure, nicotin-sulfate, nitenpyram, omethoate, oxydemeton-methyl, oxamyl, parathion, parathion-methyl, permethrin, phenthoate, phoxim, phorate, phosalone, phosmet, phosphamidon, pirimicarb, pirimiphos-methyl, profenofos, propafos, prothiofos, pymetrozine, pyraclofos, pyridafenthion, pyriproxyfen, rotenone, sulprofos, silafluofen, spinosad, sulfotep, tebfenozide, teflubenzuron, tefluthorin, terbufos, tetrachlorvinphos, thiodicarb, thiamethoxam, thiocyclam, thiofanox, thiometon, tolfenpyrad, tralomethrin, trichlorfon, triazuron, triflumuron, vamidothion.

The dose of the compounds of the present invention varies depending on an application place, an application time, an application method, cultivation crops, etc. In general, it may be between approximately 0.005 kg and 50 kg per hectare (ha) in terms of the amount of the active ingredient.

Now, formulation examples comprising the compounds of the invention are mentioned below, which, however, are not intended to restrict the scope of the invention. In the following formulation examples, “part” or “parts” are by weight.

[Wettable Powders]
Compound of the invention 5 to 80 parts
Solid carrier             10 to 85 parts
Surfactant                1 to 10 parts
Others                    1 to 5 parts

The others include, for example, anti-caking agent, etc.

[Emulsions]
Compound of the invention 1 to 30 parts
Liquid carrier            30 to 95 parts
Surfactant                5 to 15 parts
[Flowables]
Compound of the invention 5 to 70 parts
Liquid carrier            15 to 65 parts
Surfactant                5 to 12 parts
Others                    5 to 30 parts

The others include, for example, anti-freezing agent, thickener, etc.

[Dry Flowables (wettable granules)]
Compound of the invention 20 to 90 parts
Solid carrier             10 to 60 parts
Surfactant                1 to 20 parts
[Granules]
Compound of the invention 0.1 to 10 parts
Solid carrier             90 to 99.99 parts
Others                    1 to 5 parts
[Dusts]
Compound of the invention 0.01 to 30 parts
Solid carrier             67 to 99.5 parts
Others                    0 to 3 parts

Where the compounds of the present invention are used as an agent for preventing the attachment of aquatic organisms, they may be formulated into various preparations of, for example, coating paints, solutions, emulsions, pellets or flakes to be applicable to various objects. Depending on the application place, the object and the form, the preparations can be used in any ordinary manners of, for example, coating, spraying, dipping, adding to water or installing in water. To prepare such coating paints, solutions, emulsions and others, employable are any ordinary methods. Apart from the above-mentioned preparations and modes of using the compounds of the present invention, the compounds may also be used, for example, by incorporating them into ropes or fiber materials for fishingnets in the stage of preparing the ropes or fiber materials to thereby making them have the ability to prevent the attachment of aquatic organisms thereto. The agents for preveting the attachment of aquatic organisms according to the present invention can be used either singly or as combined with any other agents for preventing the attachment of aquatic organisms.

Where the aquatic adhesion inhibitors of the invention are used in the form of antifouling coatings, for example, the compounds of the invention may be mixed with film-forming agents to prepare coatings. The film-forming agents include oil varnishes, synthetic resins, artificial rubbers, etc. If desired, solvents, pigments and others can be added to the coatings. To prepare the paints, the uppermost limit of the concentration of the compounds of the invention to be therein is not specifically limited, provided that the resulting coatings can form film, but may be from 1 to 50% by weight, preferably from 5 to 20% by weight, relative to the weight of the antifouling coatings.

Where the agents for preventing the attachment of aquatic organisms of the present invention are used in the form of solutions, for example, the compounds of the invention may be dissolved in solvents along with film-forming agents to prepare solutions. The film-forming agents include synthetic resins, artificial rubbers, natural resins, etc. The solvents include xylene, toluene, cumene, methyl ethyl ketone, methyl isobutyl ketone, acetone, etc. If desired, additives such as plasticizer may be added to the solutions. To prepare the solutions, the uppermost limit of the concentration of the compounds of the invention to be therein is not specifically limited, provided that the compounds are dissolved to give solutions, but may be from 1 to 50% by weight, preferably from 5 to 30% by weight, relative to the weight of the solutions.

Where the agents for preventing the attachment of aquatic organisms of the present invention are used in the form of emulsions, surfactants areadded to the compounds of the invention to prepare the intended emulsions according to ordinary methods of preparing general emulsions. In this, the type of the surfactants to be used is not specifically limited. To prepare the emulsions, the uppermost limit of the concentration of the compounds of the invention to be therein is not specifically limited, provided that the compounds are emulsified to give emulsions, but may be from 1 to 50% by weight, preferably from 5 to 30% by weight, relative to the weight of the emulsions.

Where the agents for preventing the attachment of aquatic organisms of the present invention are used in the form of pellets or flakes, for example, the constitutive components of the compounds of the invention and optionally plasticizers, surfactants and others are added to the base of hydrophilic resins which are solid at room temperature, such as polyethylene glycol in a solid form, and the resulting mixtures are shaped into pellets or flakes through meltting molding, compression molding or the like. To prepare the pellets or flakes, the uppermost limit of the concentration of the compounds to be therein is not specifically limited, provided that the compounds can be shaped into pellets or flakes, but may be from 20 to 95% by weight, preferably from 30 to 90% by weight, relative to the weight of the pellets or flakes.

EXAMPLES

The present invention is illustrated specifically by referring to the following Synthesis Examples, Formulation Examples and Test Examples, which, however, are not intended to restrict the scope of the invention.

Synthesis Example 1

Synthesis of 2-{3-(2,6-difluorophenyl)pyrazol-1-yl}-3-(1-methyl-3,5-dichloropyrazol-4-yl)-3-hydroxyacrylonitrile (Compound No. I-40)

1) 3.0 g of 3-(2,6-difluorophenyl)pyrazole was dissolved in 20 ml of acetonitrile, and 2.52 g of chloroacetonitrile and 4.61 g of potassium carbonate were added thereto at room temperature, and heated under reflux for 5 hours. After acetonitrile was distilled off under reduced pressure, ethyl acetate was added to the residue, which was then washed with a small amount of water. The organic layer was dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was recrystallized from a mixed solvent of isopropylether and diethyl ether to obtain 1.74 g of 1-cyanomethyl-3-(2,6-difluorophenyl)pyrazole.

2) A solution of 0.5 g of 1-cyanomethyl-3-(2,6-difluorophenyl)pyrazole dissolved in 10 ml of THF was dropwise added to a suspension of 0.15 g of 55% sodium hydride in 10 ml of THF, at 50° C. After the resulting product was stirred for 30 minutes, a solution of 0.67 g of 1-(1-methyl-3,5-dichloropyrazole-4-carbonyl)pyrazole dissolved in 10 ml of THF was dropwise added thereto at 50° C. and then stirred overnight at room temperature. The reaction mixture was poured into water, then extracted with ethyl acetate and washed with a small amount of water. The resulting product was dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was recrystallized from a mixed solvent of isopropyl ether/ethyl acetate=3/1 to obtain 0.52 g of 2-{3-(2,6-difluorophenyl)pyrazol-1-yl}-3-(1-methyl-3,5-dichloropyrazol-4-yl)-3-hydroxyacrylonitrile.

Synthesis Example 2

Synthesis of 3-(1-methyl-3,5-dichloropyrazol-4-yl)-2-(2-phenylthiazol-4-yl)-3-hydroxyacrylonitrile (Compound No. II-1)

1) 2.33 g of thiobenzamide was dissolved in 20 ml of dry methanol, and 2.16 g of 1,3-dichloroacetone was added thereto at room temperature and then heated under reflux for 1 hour. The solvent was distilled off under reduced pressure, and ice water was added to the remaining product, which was then neutralized with an aqueous solution of sodium hydrogen carbonate. The resulting product was extracted with ethyl acetate, washed with saturated saline, and dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was purified through silica gel column chromatography to obtain 2.03 g of 4-chloromethyl-2-phenylthiazole was obtained from the fraction eluted with chloroform/n-hexane=1/2.

2) 1.39 g of 4-chloromethyl-2-phenylthiazole was dissolved in 10 ml of acetonitrile, and 0.65 g of potassium cyanide and 0.05 g of dibenzo-18-crown-6-ether were added thereto at room temperature, and then heated under reflux for 10 hours. After the temperature was returned to room temperature, ethyl acetate was added the resulting mixture, and the insoluble solid was removed through filtration. The resulting ethyl acetate solution was washed with saturated saline and water, and dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was purified through silica gel column chromatography to obtain 0.98 g of 4-cyanomethyl-2-phenylthiazole from the fraction eluted with chloroform.

3) 0.72 g of 4-cyanomethyl-2-phenylthiazole was dissolved in 10 ml of dry THF, and 4.6 ml of n-butyl lithium (1.56 M hexane solution) was dropwise added thereto at −60° C. or lower in an argon atmosphere. After the resulting product was stirred at −60° C. or lower for 20 minutes, 0.84 g of 1-methyl-3,5-dichloropyrazole-4-carbonyl chloride as dissolved in 3 ml of dry THF was dropwise added thereto at −60° C. or lower. Then, the resulting product was gradually heated, and stirred for 4 hours at room temperature. The reaction mixture was poured into ice water, acidified with diluted hydrochloric acid, extracted with ethyl acetate, and washed with saturated saline. The resulting product was dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was purified through silica gel column chromatography to obtain the intended product from the fraction eluted with chloroform. The resulting product was crystallized and washed with diethyl ether to obtain 0.8.6 g of 3-(1-methyl-3,5-dichloropyrazol-4-yl)-2-(2-phenylthiazol-4-yl)-3-hydroxyacrylonitrile.

Synthesis Example 3

Synthesis of 3-(1-methyl-3-trifluoromethyl-5-chloropyrazol-4-yl)-2-(4-tert-butylthiazol-2-yl)-3-pivaloyloxyacrylonitrile (Compound No. III-6, III-15)

0.5 g of 3-(1-methyl-3-trifluoromethyl-5-chloropyrazol-4-yl)-2-(4-tert-butylthiazol-2-yl)-3-hydroxyacrylonitrile and 0.14 g of triethylamine were added to 15 ml of THF at room temperature and stirred to give a uniform solution. 0.16 g of pivaloyl chloride was dropwise added to the solution with cooling with ice, then gradually heated, and stirred at room temperature for 8 hours. The reaction mixture was poured into ice water, extracted with ethyl acetate, and washed thrice with saturated saline. After having been dried over sodium sulfate, the resulting product was passed through a short column filled with silica gel. The solvent was distilled off under reduced pressure, and the residual product was applied to silica gel thin-layer chromatography (developer solvent: chloroform) to obtain 0.16 g of 3-(1-methyl-3-trifluoromethyl-5-chloropyrazol-4-yl)-2-(4-tert-butylthiazol-2-yl)-3-pivaloyloxyacrylonitrile (III-6) and 0.35 g of its geometric isomer (III-15).

Compound No. III-6:

¹H-NMR (CDCl₃, δ ppm); 1.18 (9H, s), 1.32 (9H, s), 3.85 (3H, s), 6.88 (1H, s)

Compound No. III-15:

¹H-NMR (CDCl₃, δ ppm); 1.33 (9H, s), 1.39 (9H, s), 3.94 (3H, s), 7.03 (1H, s)

Reference Example

Synthesis of 1-methyl-3-trifluoromethyl-5-chloropyrazole-4-carboxylic acid

1) 21.35 g of phosphorus oxychloride was dropwise added to 4.72 g of DMF at 10° C. or lower. After the temperature of the reaction solutio was returned to room temperature, the reaction mixture was stirred for 1 hour, and 10.71 g of 1-methyl-3-trifluoromethyl-5-pyrazolone was added thereto. The resulting mixture was heated up to 110° C., and stirred for 7 hours. After having been left to be at 70° C. the reaction mixture was poured into ice water. After pH of the mixture was made to be about 4 with an aqueous solution of sodium hydroxide added thereto, and precipitated crystals were taken out through filtration and dried to obtain 10.55 g of 1-methyl-3-trifluoromethyl-5-chloropyrazole-4-carbaldehyde.

2) 8.88 g of 1-methyl-3-2-(tert-trifluoromethyl-5-chloropyrazole-4-carbaldehyde and 7.24 g of potassium permanganate were added to an aqueous solution of 0.23 g of potassium hydroxide in 85 ml of water, at room temperature. After having been heated up to 60° C., the resulting mixture was stirred for 2 hours. Next, the temperature of the mixture was return to room temperature, and the solid was removed through filtration. The resulting filtrate was acidified with an aqueous solution of hydrochloric acid, and precipitated crystals were taken out through filtration, washed with water, and dried. The thus-obtained crystals were added to 150 ml of chloroform, and heated under reflux, and the insoluble solid was removed through filtration at a heating time. Chloroform was distilled off under reduced pressure, and 6.24 g of 1-methyl-3-trifluoromethyl-5-chloropyrazole-4-carboxylic acid was obtained.

Synthesis Example 4

Synthesis of 2-(2-tert-butylthiazol-4-yl)-3-(2-methyl-4-trifluoromethylthiazol-5-yl)-3-benzoyloxyacrylonitrile (Compound No. II-75)

In the same manner as above, the above-mentioned compound was synthesized (viscous liquid, E-Z mixture).

¹H-NMR (CDCl₃, δ ppm); 1.09 (9H, s), 2.75 (3H, s), 7.3-7.6 (4H, m), 8.05-8.25 (2H, m): major 1.19 (9H, s), 2.70 (3H, s), 7.3-7.6 (4H, m), 8.05-8.25 (2H, m): minor

Synthesis Example 5

Synthesis of 2-(4-trifluoromethylphenyl)-3-(1-methyl-3,5-dichloropyrazol-4-yl)-3-(1-methyl-3,5-dichloropyrazole-4-carbonyloxy)acrylonitrile (Compound No. IV-5)

1.0 g of 4-(trifluoromethyl)phenylacetonitrile and 2.31 g of 1-methyl-3,5-dichloropyrazole-4-carbonyl chloride were dissolved in 30 ml of dry THF, and 0.61 g of potassium t-butoxide was added thereto at room temperature. After having been heated, the resulting product was kept heated under reflux for 3 hours. 0.61 g of potassium t-butoxide was again added thereto and further heated under reflux for 2 hours. THF was distilled off under reduced pressure, and water was added to the residual product, which was then extracted with ethyl acetate. The resulting organic layer was washed with a dilute aqueous solution of sodium hydroxide and then with water. This was dried with sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified through silica gel column chromatography to obtain 1.92 g of 3-(1-methyl-3,5-dichloropyrazol-4-yl)-2-(4-trifluoromethylphenyl)-3-(1-methyl-3,5-dichloropyrazole-4-carbonyloxy)acrylonitrile from the fraction eluted with n-hexane:ethyl acetate=2:1.

Synthesis Example 6

Synthesis of 2-(4-tert-butylphenyl)-3-(1-methyl-3,5-dichloropyrazol-4-yl)-3-hydroxyacrylonitrile (Compound No. IV-18):

0.22 g of dibenzo-18-crown-6-ether and 1.57 g of sodium cyanide were suspended in 20 ml of DMSO, and 5.00 g of 4-tert-butylbenzyl bromide was dropwise added thereto with cooling with water. After having been stirred overnight at room temperature, the resulting mixture was further stirred at 50° C. for 5 hours. After this was left to be at room temperature, water was added thereto and extracted with ether. The organic layer was washed with water, and dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was purified through silica gel column chromatography to obtain 1.19 g of 4-tert-butylphenylacetonitrile was obtained from the fraction eluted with n-hexane:ethyl acetate=5:1.

1.00 g of 4-tert-butylphenylacetonitrile and 1.23 g of 1-methyl-3,5-dichloropyrazole-4-carbonyl chloride were dissolved in 20 ml of THF, and 1.01 g of potassium t-butoxide was added thereto with cooling with ice. After the resulting mixture was stirred overnight at room temperature, water was added thereto, acidified with diluted hydrochloric acid, and extracted with ethyl acetate. The organic layer was washed with water, and dried with sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was dissolved in a mixed solvent of 10 ml of water and 10 ml of dioxane, and 0.38 g of potassium hydroxide was added thereto and heated under reflux for 4 hours. After having been left to be at room temperature, this was acidified with diluted hydrochloric acid, and extracted with ethyl acetate. The organic layer was washed with water, and dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was purified through silica gel column chromatography to obtain 0.64 g of 2-(4-tert-butylphenyl)-3-(1-methyl-3,5-dichloropyrazol-4-yl)-3-hydroxyacrylonitrile from the fraction eluted with n-hexane:ethyl acetate=2:1.

Synthesis Example 7

Synthesis of 2-(4-tert-butylphenyl)-3-(1-methyl-3-trifluoromethyl-5-chloropyrazol-4-yl)-3-pivaloyloxyacrylonitrile (Compound No. V-24)

In the same manner as above, the above-mentioned compound was synthesized (viscous liquid).

¹H-NMR (CDCl₃, δ ppm); 1.13 (9H, s), 1.33 (9H, s), 3.98 (3H, s), 7.48 (4H, brs)

Synthesis Example 8

Synthesis of 2-(4-tert-butylphenyl)-3-(3,5-dichloro-1-methylpyrazol-4-yl)-3-methoxycarbonyloxyacrylonitrile (Compound No. IV-36)

In the same manner as above, the above-mentioned compound was synthesized (vitreous, E-Z mixture).

¹H-NMR (CDCl₃, δ ppm); 1.32 (9H, s), 3.75 (3H, s), 3.87 (3H, s), 7.49 (2H, d, J=8 Hz), 7.58 (2H, d, J=8 Hz): 75% 1.27 (9H, s), 3.88 (3H, s), 3.96 (3H, s), 7.49 (2H, d, J=8 Hz), 7.58 (2H, d, J=8 Hz): 25%

Synthesis Example 9

Synthesis of 2-{2-tert-butyloxazol-4-yl}-3-(3,5-dichloro-1-methyl-pyrazol-4-yl)-3-hydroxyacrylonitrile (Compound No. V-40)

1) 25 g of pivalic acid amide and 25 g of 1,3-dichloro-2-propanone were mixed and heated on an oil bath at 135° C. for 2.5 hours. After having been cooled with ice, the mixture was made alkaline with an aqueous solution of sodium hydroxide added thereto. Then, the resulting product was extracted with ethyl acetate, washed with water, and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was purified through column chromatography (silica gel; ethyl acetate:n-hexane=1:8) to obtain 17.5 g of 2-tert-butyl-4-chlbromethyloxazole.

2) 6.2 g of sodium cyanide was weighed, 50 ml of dimethylsulfoxide was added thereto, and a dimethylsulfoxide solution of 16.9 g of 2-tert-butyl-4-chloromethyloxazole was dropwise added thereto, and heated on an oil bath at 65° C. for 1 hour with stirring. After the resulting product was cooled to room temperature, 150 ml of a dilute aqueous solution of sodium hydroxide was added thereto, and extracted with toluene. The organic layer was fully washed with water, and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain 14.8 g of 2-tert-butyl-4-cyanomethyloxazole.

3) 2.87 g of potassium tert-butoxide was suspended in 20 ml of THF, and a solution of 2.00 g of 2-tert-butyl-4-cyanomethyloxazole and 2.37 g of 3,5-dichloro-1-methylpyrazole-4-carbonyl chloride as dissolved in 10 ml of THF was dropwise added thereto with cooling with ice, and then stirred overnight at room temperature. The reaction mixture was poured into ice water, extracted with ethyl acetate, and washed with a small amount of water. After the resulting product was dried with anhydrous sodium sulfate, the solvent was evaporated out under reduced pressure. The residual product was purified through column chromatography (silica gel; n-hexane:ethyl acetate=4:1) to obtain 3.26 g of the intended compound.

Synthesis Example 10

Synthesis of 2-(2-tert-butyloxazol-4-yl)-3-(5-chloro-1-methyl-3-trifluoromethylpyrazol-4-yl)-3-ethoxymethoxyacrylonitrile (Compound No. V-44)

0.6 g of 2-{2-tert-butyloxazol-4-yl}-3-(5-chloro-3-trifluoromethyl-1-methyl-pyrazol-4-yl)-3-hydroxyacrylonitrile was dissolved in 5 ml of THF, and 0.07 g of 60% sodium hydride was added thereto with cooling with ice, and then stirred for 15 minutes at room temperature. 0.17 g of ethoxymethyl chloride was added thereto and stirred for 6 days at room temperature. The reaction mixture was poured into ice water, extracted with ethyl acetate, and washed with saturated saline. The resulting product was dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The resulting residual product was purified through silica gel thin-layer chromatography (ethyl acetate:n-hexane=1:4) to obtain 0.1 g of the intended compound in vitreous state.

¹H-NMR (CDCl₃, δ ppm); 1.17 (3H, t), 1.41 (9H, s), 3.98 (3H, s), 5.03 (2H, s), 8.00 (1H, s)

Synthesis Example 11

Synthesis of ethyl 2-phenyl-3-(3,5-dichloro-1-methylpyrazol-4-yl)-3-hydroxyacrylate (Compound No. IV-91)

8.2 g (50 mmols) of ethyl phenylacetate and 10.7 g (50 mmols) of 3,5-dichloro-1-methylpyrazole-4-carboxylic acid chloride were dissolved in 100 ml of dry tetrahydrofuran, and 14 g (125 mmols) of potassium tert-butoxide at room temperature. The reaction mixture was stirred at room temperature for 1 hour, and 300 ml of water was added thereto, and extracted with ethyl acetate. The organic layer was washed with water and saturated saline, and dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure to obtain 17 g of the intended ethyl 2-phenyl-3-(3,5-dichloro-1-methylpyrazol-4-yl)-3-hydroxyacrylate.

¹H-NMR (CDCl₃, δ ppm); 1.1-1.5 (3H, m), 3.59 (1.5H, s), 3.73 (1.5H, s), 3.95-4.45 (2H, m), 5.58 (0.5H, s), 7.0-7.35 (5H, m), 13.21 (0.5H, s)

Synthesis Example 12

Synthesis of 1-(3,5-dichloro-1-methylpyrazol-4-yl)-2-phenyl-2-bromoethanone (Compound No. IV-90)

1) 17 g (50 mmols) of ethyl 2-phenyl-3-(3,5-dichloro-1-methylpyrazol-4-yl)-3-hydroxyacrylate was dissolved in 50 ml of 6 N HCl and 250 ml of 1,4-dioxane, and heated under reflux for 15 hours. The reaction mixture was poured into 500 ml of ice water, and precipitated crystals were taken out through filtration to obtain 8 g of the intended 1-(3,5-dichloro-1-methylpyrazol-4-yl)-2-phenylethanone as white crystals. m.p.: 94-96° C.

2) 5.38 g (20 mmols) of 1-(3,5-dichloro-1-methylpyrazol-4-yl)-2-phenylethane was dissolved in 50 ml of chloroform, and stirred at room temperature for 1 hour, and the solvent was distilled off under reduced pressure to obtain the intended 1-(3,5-dichloro-1-methylpyrazol-4-yl)-2-phenyl-2-bromoethanone as white crystals. m.p.: 74.5-75.5° C.

Synthesis Example 13

Synthesis of 1-(3,5-dichloro-1-methylpyrazol-4-yl)-1-pivaloyloxy-2-phenyl-2-bromoethylene (Compound No. IV-92)

0.55 g (1.58 mmols) of 1-(3,5-dichloro-1-methylpyrazol-4-yl)-2-phenyl-bromoethane and 0.18 g (1.74 mmols) of triethylamine were dissolved in 4 ml of dry tetrahydrofuran, and 0.19 g (1.58 mmols) of pivalic acid chloride was added thereto at room temperature. After the reaction mixture was stirred for 16 hours at room temperature, 10 ml of water was added thereto, and extracted with ethyl acetate. The organic layer was washed with water and saturated saline, and dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure. The obtained residue was purified through silica gel column chromatography to obtain 0.23 g of the intended 1-(3,5-dichloro-1-methylpyrazol-4-yl)-1-pivaloyloxy-2-phenyl-2-bromoethylene as a colorless liquid (E-Z mixture).

¹H-NMR (CDCl₃, δ ppm); 1.05 (9H, s), 3.81 (3H, s), 7.37 (5H, m): major 1.32 (9H, s), 3.62 (3H, s), 7.24 (5H, m): minor

Synthesis Example 14

Synthesis of 1-(3,5-dichloro-1-methylpyrazol-4-yl)-2-{2-(1-methylcyclohexan-1-yl)-thiazol-4-yl}-2-diethylphosphonoethanone (Compound No. II-156)

1) 4.15 g (18.1 mmols) of 2-(1-methyl-cyclohexan-1-yl)-4-chloromethylthiazole and 3.32 g (20 mmols) of trimethyl phosphite were mixed and heated under reflux for 16 hours. The reaction mixture was cooled to room temperature, and purified through silica gel column chromatography to obtain 4.63 g of the intended diethyl {2-(1-methylcyclohexan-1-yl)-thiazol-4-yl}methylphosphonate as a colorless liquid.

¹H-NMR (CDCl₃, δ ppm); 1.25 (3H, t, J=7.2 Hz), 1.31 (3H, s), 1.1-2.3 (10H, m), 3.33 (2H, d, J=20.4 Hz), 4.04 (4H, dd, J=7.2, 7.2 Hz), 7.01 (1H, m)

2) 0.85 g (4 mmols) of 3,5-dichloro-1-methylpyrazole-4-carboxylic acid chloride and 1.32 g (4 mmols) of diethyl {2-(1-methylcyclohexan-1-yl)-thiazol-4-yl}methylphosphonate were dissolved in 15 ml of dry tetrahydrofuran, and 1.12 g (10 mmols) of potassium t-butoxide was added thereto at room temperature. The reaction mixture was stirred for 1 hour at room temperature, and 20 ml of water was added thereto, and extracted with ethyl acetate. The organic layer was washed with water and saturated saline, and dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure. The obtained residue was purified through silica gel column chromatography to obtain 0.4 g of the intended 1-(3,5-dichloro-1-methylpyrazol-4-yl)-2-{2-(1-methylcyclohexan-1-yl)-thiazol-4-yl}-2-diethylphosphonoethanone.

¹H-NMR (CDCl₃, δ ppm); 1.23 (3H, t, J=7.2 Hz), 1.23 (3H, s), 1.1-2.3 (10H, m), 3.79 (3H, s), 4.09 (2H, dd, J=7.2, 7.2 Hz), 5.90 (1H, d, J=22.8 Hz), 7.43 (1H, m)

Synthesis Example 15

Synthesis of allyl 2-{3-(2,6-difluorophenyl)pyrazol-1-yl}-3-(5-chloro-1-methyl-3-trifluoromethylpyrazol-4-yl)-3-hydroxyacrylate (Compound No. I-133)

1) Potassium carbonate (1.53 g) was added to an acetonitrile (10 mL) solution of 3-(2,6-difluorophenyl)-pyrazole (1 g) and allyl 2-bromoacetate (1.49 g), and refluxed for 3 hours. The resulting product was extracted with acetate and diluted hydrochloric acid added thereto at room temperature. The organic layer was dried over anhydrous magnesium sulfate and concentrated, and the resulting concentrate was purified through silica gel column chromatography (chloroform) to obtain allyl 2-(3-(2,6-difluorophenyl)pyrazol-1-yl)acetate (1.5 g).

¹H-NMR (CDCl₃, δ ppm); 4.70 (2H, d, J=6.0 Hz), 5.10 (2H, s), 5.30-5.60 (2H, m), 5.70-6.40 (1H, m), 6.50-7.80 (5H, m)

2) Potassium butoxide (0.5 g) was added to a THF (10 mL) solution of allyl 2-(3-(2,6-difluorophenyl)pyrazol-1-yl)acetate (0.5 g) and 5-chloro-1-methyl-3-trifluoromethylpyrazole-4-carbonyl chloride (0.44 g) at 0° C. and stirred for 5 minutes. Water (5 ml) was added thereto, and then extracted with diluted hydrochloric acid and ethyl acetate. After the organic layer was dried over anhydrous magnesium sulfate, and then concentrated, and the resulting concentrate was purified through silica gel column chromatography (chloroform) to obtain the intended product, Compound No. I-133 (0.89 g).

¹H-NMR (CDCl₃, δ ppm): 3.95 (3H, s), 4.80 (2H, d, J=6.0 Hz), 5.20-5.60 (2H, m), 5.60-6.40 (1H, m), 6.45-7.90 (6H, m)

Synthesis Example 16

Synthesis of 2-bromo-2-{3-(2,6-difluorophenyl)pyrazol-1-yl}-1-(5-chloro-1-methyl-3-trifluoromethylpyrazol-4-yl)-1-hydroxyethylene (Compound No. I-134)

1) Formic acid (60 mg) was added to a THF (1 mL) solution of palladium acetate (7 mg) and triphenylphosphine (17 mg) and stirred for 5 minutes at room temperature in a nitrogen atmosphere. A THF (5 mL) solution of Compound I-133 (0.32 g) was added thereto and refluxed for 1 hour. The reaction mixture was left to be at room temperature, and concentrated, and the resulting concentrate was purified through silica gel column chromatography (chloroform) and recrystallization (chloroform-diisopropyl ether) to obtain 2-(3-(2,6-difluorophenyl)pyrazol-1-yl)-3-(5-chloro-1-methyl-3-trifluoromethylpyrazol-4-yl)ethan-1-one (0.1 g).

m.p.: 152-154° C.

2) A THF solution (0.27 mL) of 1M lithium hexamethyldisilazide was added to a THF solution of 2-{3-(2,6-difluorophenyl)pyrazol-1-yl}-3-(5-chloro-1-methyl-3-trifluoromethylpyrazol-4-yl)ethan-1-one (0.1 g) at −78° C. and stirred at the same temperature in a nitrogen atmosphere. To the resulting solution was added a THF (2 mL) solution of carbon tetrabromide (0.098 g), and then gradually heated up to room temperature. Water (1 mL) was added thereto, and then extracted with diluted hydrochloric acid and ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate, concentrated, and recrystallized from chloroform-diethyl ether) to obtain the intended product, Compound No. I-134 (0.062 g). m.p.: 123-125° C.

Synthesis Example 17

Synthesis of 2-bromo-2-{3-(2,6-difluorophenyl)pyrazol-1-yl}-1-(5-chloro-1-methyl-3-trifluoromethylpyrazol-4-yl)-1-pivaloyloxyethylene (Compound No. I-135)

Triethylamine (0.3 g) and pivalic acid chloride (0.23 g) were added in that order to a chloroform (25 mL) solution of Compound No. I-134 (0.47 g) at 0° C., and stirred at room temperature for 1 hour. The resulting product was extracted with water and chloroform. The organic layer was dried with anhydrous magnesium sulfate, concentrated, and purified through silica gel column chromatography (chloroform) to obtain the intended product, Compound No. I-135 (0.4 g).

¹H-NMR (CDCl₃, δ ppm); 1.25 (9H, s), 3.90 (3H, s), 6.55-7.80 (5H, m)

In accordance with the above-mentioned reaction schemes or Examples, various compounds of the present invention were produced, of which the structure and the melting point are shown in Table 15 to Table 19 below. Unless otherwise specifically indicated, the compounds shown in these are in the form of a mixture of E-form and Z-form. The abbreviations in these have the same meanings as those mentioned above.

TABLE 15
							m.p.
No.	R1	R2	R3	E	B	A	(° C.)
I-1	Ph	H	H	CN	H	A1	144-145
I-2	Ph	Cl	H	CN	H	A1	300<
I-3	Ph	H	Me	CN	H	A1	300<
I-4	Ph	Me	H	CN	H	A1	141-143
I-5	Ph	H	H	CN	B1	A1	75-77*
I-6	Ph	H	H	CN	B2	A1	viscous oil
I-7	Ph	CO2Et	H	CN	H	A1	202-203
I-8	Ph	H	H	CN	H	A2	300<
I-9	Ph	H	H	CN	H	A7	124-125
I-10	Ph	H	H	CN	H	A8	265-267
I-11	2-pyridyl	H	H	CN	H	A1	290<
I-12	2-pyridyl	H	H	CN	H	A2	300<
I-13	2-pyridyl	H	H	CN	H	A3	260-267
I-14	2-pyridyl	H	H	CN	H	A4	300
I-15	2-pyridyl	H	H	CN	H	A6	297-298
I-16	2-pyridyl	H	H	CN	H	A7	163-165
I-17	2-pyridyl	H	H	CN	H	A8	300<
I-18	2-pyridyl	H	H	CN	H	A9	240-245
I-19	2-pyridyl	H	H	CN	H	A10	261-266
I-20	2-pyridyl	H	H	CN	H	A11	232-234
I-21	2-pyridyl	H	H	CN	H	A12	284-287
I-22	2-pyridyl	H	H	CN	H	A13	300<
I-23	2-pyridyl	H	H	CN	B7	A7	103-110*
I-24	2-pyridyl	H	H	CN	B8	A1	viscous oil
I-25	3-pyridyl	H	H	CN	H	A1	298-300
I-26	3-pyridyl	H	H	CN	H	A2	158-160
I-27	3-pyridyl	H	H	CN	H	A7	168-169
I-28	4-pyridyl	H	H	CN	H	A1	251-253
I-29	2-F—Ph	H	H	CN	H	A1	125-126
I-30	2-F—Ph	H	H	CN	H	A2	281-282
I-31	2-F—Ph	Cl	H	CN	H	A1	281-287
I-32	3-F—Ph	H	H	CN	H	A2	300<
I-33	4-F—Ph	H	H	CN	H	A2	169-173
I-34	2-Cl—Ph	H	H	CN	H	A1	viscous oil
I-35	2-Cl—Ph	H	H	CN	H	A2	viscous oil
I-36	3-Cl—Ph	H	H	CN	H	A1	141-149
I-37	3-Cl—Ph	H	H	CN	H	A7	291-293
I-38	4-Cl—Ph	H	H	CN	H	A1	186-188
I-39	4-Cl—Ph	H	H	CN	H	A7	300<
I-40	2,6-F2—Ph	H	H	CN	H	A1	267-269
I-41	2,6-F2—Ph	H	H	CN	H	A2	300<
I-42	2,6-F2—Ph	H	H	CN	H	A7	242-243
I-43	2,6-Cl2—Ph	H	H	CN	H	A1	147-148
I-44	2,6-Cl2—Ph	H	H	CN	H	A2	100-102
I-45	tBu	H	H	CN	H	A1	viscous oil
I-46	tBu	H	H	CN	H	A2	65-67
I-47	2-MeO—Ph	H	H	CN	H	A1	300<
I-48	2-MeO—Ph	H	H	CN	H	A2	300<
I-49	H	CO2Et	Ph	CN	H	A1	236-237
I-50	Me	Ph	H	CN	H	A1	viscous oil
I-51	cHex	H	H	CN	H	A1	204-205
I-52	1-naphthyl	H	H	CN	H	A1	225-227
I-53	2-thienyl	H	H	CN	H	A1	146-147
I-54	2-thienyl	H	H	CN	H	A7	271-273
I-55	Ph	H	H	CN	H	A34	173.3-174.1
I-56	Ph	H	H	CN	B1	A34	viscous oil*
I-57	Ph	H	H	CN	B7	A1	140-141*
I-58	Ph	H	H	CN	B8	A1	50-51*
I-59	Ph	H	H	CN	CO2tBu	A1	viscous oil
I-60	tBu	CO2Me	H	CN	H	A1	105-106
I-61	tBu	CO2Me	H	CN	B7	A1	125-126
I-62	Ph	H	H	CN	B7	A2	viscous oil
I-63	2,6-F2—Ph	H	H	CN	B8	A2	200-201
I-64	Ph	H	H	CN	B6	A2	viscous oil
I-65	2,6-F2—Ph	H	H	CN	Na	2,6-(MeO)2—Ph	300<
I-66	2,6-F2—Ph	H	H	CN	Na	2-CF3O—Ph	282.8-287.2
I-67	2,6-F2—Ph	H	H	CN	Na	2-MeO—Ph	300<
I-68	2,6-F2—Ph	H	H	CN	H	2-CF3O—Ph	157.9-160.1
I-69	2-pyridyl	H	H	CN	B8	A7	118-119*
I-70	2,6-F2—Ph	H	H	CN	B7	A2	viscous oil
I-71	Ph	H	H	CN	H	2-Cl—Ph	108-109
I-72	Ph	H	H	CN	H	2,6-F2—Ph	167-168
I-73	Ph	H	H	CN	H	2,6-Cl2—Ph	170-171
I-74	Ph	H	H	CN	H	2-CF3—Ph	viscous oil
I-75	Ph	H	H	CN	H	1-naphthyl	137-138
I-76	Ph	Ph	H	CN	H	A2	145-147
I-77	Ph	H	H	CN	H	2-Cl-4-F—Ph	94-95
I-78	Ph	H	H	CN	B35	A2	164-165
I-79	2,6-F2—Ph	H	H	CN	H	2-Me—Ph	113.1-119.8
I-80	2,6-F2—Ph	H	H	CN	H	2-Cl-6-F—Ph	144-146
I-81	2,6-F2—Ph	H	H	CN	H	2-NO2—Ph	176-179
I-82	2,6-F2—Ph	H	H	CN	H	2-AcO—Ph	vitreous state
I-83	2,6-F2—Ph	H	H	CN	H	2,6-Me—Ph	vitreous state
I-84	2-pyridyl	H	H	CN	H	2,6-F2—Ph	188-189
I-85	2-pyridyl	H	H	CN	H	2,6-Cl2—Ph	278-280
I-86	2-pyridyl	H	H	CN	H	2-NO2—Ph	285-287
I-87	2-pyridyl	H	H	CN	H	2-MeO—Ph	275-276
I-88	2-pyridyl	H	H	CN	H	2-CO2Me—Ph	248-249
I-89	2-pyridyl	H	H	CN	B7	2-Cl—Ph	124-125
I-90	2-pyridyl	H	H	CN	Na	2-Cl—Ph	278-280
I-91	2-pyridyl	H	H	CN	H	pyridin-2-yl	216-217
I-92	2-pyridyl	H	H	CN	COnC17H35	A7	58-59
I-93	t-Bu	CO2Me	H	CN	H	2-Cl-4-F—Ph	114-115
I-94	t-Bu	CO2Me	H	CN	B7	A2	105-106
I-95	t-Bu	CO2Me	H	CN	H	A2	102-103
I-96	t-Bu	H	H	CN	B7	A2	viscous oil
I-97	t-Bu	H	H	CN	B7	A2	viscous oil#1
I-98	t-Bu	NO2	H	CN	B7	A2	viscous oil
I-99	t-Bu	Br	H	CN	B7	A2	viscous oil
I-100	t-Bu	CN	H	CN	H	A2	178-180
I-101	t-Bu	CN	H	CN	CO2tBu	A2	vitreous state
I-102	t-Bu	CN	H	CN	CO2tBu	A2	201-202.5#2
I-103	t-Bu	CN	H	CN	CO2Ph	A2	vitreous state
I-104	t-Bu	Cl	H	CN	B7	A2	viscous oil
I-105	t-Bu	CO2Me	H	CN	CO2iBu	A2	155.8-156.9
I-106	t-Bu	Cl	H	CN	H	A2	viscous oil
I-107	t-Bu	NO2	H	CN	H	A2	87-88
I-108	t-Bu	CO2nHex	H	CN	H	A2	vitreous state
I-109	t-Bu	CO2Me	H	CN	B8	A2	152.1-153.5
I-110	t-Bu	Me	H	CN	H	A2	vitreous state
I-111	t-Bu	CO2Me	H	CN	COnC17H35	A14	viscous oil
I-112	t-Bu	CO2Me	H	CN	B7	A14	viscous oil
I-113	t-Bu	CO2Me	H	CN	H	A14	101-102
I-114	t-Bu	Me	H	CN	B7	A2	vitreous state
I-115	t-Bu	CO2Me	H	CN	B7	A3	131-132
I-116	t-Bu	CO2Me	H	CN	Me	A2	166-167*
I-117	t-Bu	CO2Me	H	CN	B3	A14	viscous oil
I-118	t-Bu	CO2Me	H	CN	H	A21	152.6-154
I-119	t-Bu	CO2Me	H	CN	COnC9H19	A3	viscous oil
I-120	t-Bu	CO2Me	H	CN	B7	A15	125-127*
I-121	t-Bu	CO2Me	H	CN	H	A15	138-139
I-122	t-Bu	CO2Me	H	CN	B7	A21	viscous oil
I-123	t-Bu	CO2Me	H	CN	COnC5H11	A21	viscous oil
I-124	t-Bu	CO2Me	H	CN	COnC5H11	A21	viscous oil#3
I-125	H	H	2,6-F2—Ph	CN	H	A2	157.4-162.4
I-126	H	Ph	H	CN	H	A1	vitreous state
I-127	H	t-Bu	H	CN	B7	A2	vitreous state
I-128	H	t-Bu	H	CN	H	A2	vitreous state
I-129	Ph	H	H	CO2Me	H	A1	158-160
I-130	Ph	H	H	CO2Me	B7	A2	viscous oil
I-131	2,6-F2—Ph	H	H	CO2Me	H	A2	248-250
I-132	2,6-F2—Ph	H	H	COMe	H	A2	vitreous state
I-133	2,6-F2—Ph	H	H	CO2CH2CH═CH2	H	A2	vitreous state
I-134	2,6-F2—Ph	H	H	Br	H	A2	123-125
I-135	2,6-F2—Ph	H	H	Br	B7	A2	vitreous state
I-136	2-pyridyl	H	H	CN	B7	A37	86-94#4
I-137	2-pyridyl	H	H	CN	B7	A10	92-93
I-138	2-pyridyl	Cl	H	CN	B7	A7	viscous oil*
*E-form or Z-form
#1geometric isomer of I-96
#2geometric isomer of I-101
#3geometric isomer of I-123
#4mixture of E/Z = 2/1

TABLE 16
					m.p.
No.	R	E	B	A	(° C.)
II-1	Ph	CN	H	A1	200-205
II-2	2-Cl—Ph	CN	H	A2	137-138
II-3	t-Bu	CN	H	A2	151-153
II-4	t-Bu	CN	B3	A2	147-150*
II-5	t-Bu	CN	B7	A2	89.5-92*
II-6	t-Bu	CN	H	A1	viscous oil*
II-7	t-Bu	CN	B7	A1	viscous oil*
II-8	t-Bu	CN	H	2,6-F2—Ph	90-92.5
II-9	t-Bu	CN	H	2-Cl—Ph	96.2-98.6
II-10	t-Bu	CN	B6	A2	vitreous state*
II-11	t-Bu	CN	B5	A2	viscous oil
II-12	t-Bu	CN	B8	A2	viscous oil
II-13	t-Bu	CN	SO2(4-Cl—Ph)	A2	vitreous state*
II-14	t-Bu	CN	H	2,6-Cl2—Ph	150.3-151.7
II-15	t-Bu	CN	H	2-CF3—Ph	71.9-79.6
II-16	t-Bu	CN	H	A3	viscous oil
II-17	t-Bu	CN	B7	A3	viscous oil*
II-18	t-Bu	CN	CO2Et	A2	viscous oil
II-19	t-Bu	CN	CO2CH2Ph	A2	viscous oil
II-20	t-Bu	CN	CONMe2	A2	136.7-138.2
II-21	t-Bu	CN	CH2CO2Me	A2	viscous oil
II-22	t-Bu	CN	PO(OEt)2	A2	viscous oil
II-23	2-pyridyl	CN	H	A2	184.5-188.5
II-24	2-pyridyl	CN	H	A7	210.3-218.8
II-25	2-pyridyl	CN	B7	A7	162.7-167*
II-26	2-pyridyl	CN	B7	A2	vitreous state*
II-27	2-pyridyl	CN	H	A3	148-151
II-28	2-pyridyl	CN	B7	A3	vitreous state*
II-29	2-pyridyl	CN	H	A35	188-193
II-30	2-pyridyl	CN	B7	A35	200.5-202.5*
II-31	2-pyridyl	CN	H	A36	viscous oil
II-32	2-pyridyl	CN	B7	A36	viscous oil
II-33	c-Hex	CN	H	A2	126.5-128.1
II-34	c-Hex	CN	H	2,6-F2—Ph	110.9-112.7
II-35	c-Hex	CN	B7	2,6-F2—Ph	111.2-117.4*
II-36	c-Hex	CN	B7	A2	viscous oil*
II-37	2,6-F2—Ph	CN	H	A2	176.8-178.2
II-38	2,6-F2—Ph	CN	B7	A2	95.9-98.0*
II-39	2-Cl—Ph	CN	H	A2	172.9-175.2
II-40	t-Bu	CN	B35	A2	vitreous state
II-41	t-Bu	CN	B35	A2	vitreous state#4
II-42	t-Bu	CN	B36	A2	vitreous state
II-43	t-Bu	CN	H	A13	168-173
II-44	t-Bu	CN	B28	A2	vitreous state
II-45	t-Bu	CN	B30	A2	vitreous state
II-46	t-Bu	CN	B30	A2	vitreous state#5
II-47	t-Bu	CN	CO(2-Me—Ph)	A2	vitreous state
II-48	t-Bu	CN	B38	A2	vitreous state
II-49	t-Bu	CN	B37	A2	vitreous state
II-50	t-Bu	CN	nicotinoyl	A2	vitreous state
II-51	t-Bu	CN	B40	A2	vitreous state
II-52	t-Bu	CN	CO2iBu	A2	viscous oil
II-53	t-Bu	CN	CO2Ph	A2	viscous oil
II-54	t-Bu	CN	B41	A2	viscous oil
II-55	t-Bu	CN	CO2nHex	A2	viscous oil
II-56	t-Bu	CN	H	3-Cl—Ph	89.7-91.1
II-57	t-Bu	CN	H	3-F—Ph	63.7-64.4
II-58	t-Bu	CN	H	2-Br—Ph	86-87
II-59	t-Bu	CN	H	2-I—Ph	vitreous state
II-60	t-Bu	CN	H	2-Cl-6-F—Ph	109.6-110.6
II-61	t-Bu	CN	CO(2-MeS—Ph)	A2	vitreous state
II-62	t-Bu	CN	H	2-MeS—Ph	120.6-122.1
II-63	t-Bu	CN	H	A22	113-118
II-64	t-Bu	CN	B7	A22	98-99.5*
II-65	t-Bu	CN	B15	A22	viscous oil
II-66	t-Bu	CN	B38	A13	viscous oil
II-67	t-Bu	CN	B39	A2	vitreous state
II-68	t-Bu	CN	CO(4-Cl—Ph)	A2	vitreous state
II-69	t-Bu	CN	CO(3-Cl—Ph)	A2	vitreous state
II-70	t-Bu	CN	B7	2,6-F2—Ph	viscous oil
II-71	t-Bu	CN	B8	2,6-F2—Ph	viscous oil
II-72	t-Bu	CN	B6	2,6-F2—Ph	150.2-151.3
II-73	t-Bu	CN	CO2nPr	A2	viscous oil
II-74	t-Bu	CN	CO2nBu	A2	viscous oil
II-75	t-Bu	CN	B6	A13	viscous oil
II-76	t-Bu	CN	CO2CH2CCl3	A2	viscous oil
II-77	t-Bu	CN	CO(2-Cl—Ph)	A2	vitreous state
II-78	t-Bu	CN	CO(3-CF3—Ph)	A2	vitreous state
II-79	t-Bu	CN	CO(4-CF3—Ph)	A2	vitreous state
II-80	t-Bu	CN	CO(3-NO2—Ph)	A2	vitreous state
II-81	t-Bu	CN	CO(2-Cl-6-F—Ph)	A2	vitreous state
II-82	t-Bu	CN	CO2cPen	2,6-F2—Ph	vitreous state
II-83	t-Bu	CN	3-Cl-pivaloyl	A2	viscous oil*
II-84	t-Bu	CN	CO2iPr	A2	viscous oil
II-85	t-Bu	CN	CO2CH2CH2Cl	A2	viscous oil
II-86	t-Bu	CN	CO2CHClCH3	A2	viscous oil
II-87	t-Bu	CN	COiPr	A2	viscous oil
II-88	t-Bu	CN	isonicotinoyl	A2	viscous oil
II-89	t-Bu	CN	picolinoyl	A2	viscous oil
II-90	t-Bu	CN	CO(4-Me—Ph)	A2	viscous oil
II-91	t-Bu	CN	CO(4-NO2—Ph)	A2	viscous oil
II-92	t-Bu	CN	methacryloyl	A2	viscous oil
II-93	t-Bu	CN	B15	A2	vitreous state
II-94	t-Bu	CN	PhCH2	A2	viscous oil
II-95	t-Bu	CN	Me	A2	136.5-138
II-96	t-Bu	CN	CBrF2	A2	84-86.5
II-97	t-Bu	CN	COnPr	A2	viscous oil
II-98	t-Bu	CN	COiBu	A2	viscous oil
II-99	t-Bu	CN	B43	A2	vitreous state
II-100	t-Bu	CN	PhCOCH2	A2	148-152*
II-101	t-Bu	CN	B42	A2	128-129.5*
II-102	t-Bu	CN	H	A14	98-99
II-103	t-Bu	CN	H	A16	viscous oil
II-104	t-Bu	CN	B7	A16	viscous oil*
II-105	t-Bu	CN	cinnamoyl	A2	vitreous state
II-106	t-Bu	CN	H	A23	109-112
II-107	t-Bu	CN	B7	A23	120-122.5
II-108	t-Bu	CN	B7	A14	viscous oil
II-109	t-Bu	CN	B7	A14	viscous oil#6
II-110	t-Bu	CN	COnC17H35	A14	viscous oil
II-111	t-Bu	CN	PhCH2CO	A2	viscous oil
II-112	t-Bu	CN	B7	A17	viscous oil
II-113	t-Bu	CN	H	A17	140-143
II-114	t-Bu	CN	H	A24	115-117
II-115	t-Bu	CN	CO2iBu	A24	vitreous state
II-116	t-Bu	CN	B7	A2	69.5-73.5#7
II-117	t-Bu	CN	H	A25	107-109
II-118	t-Bu	CN	B7	A25	viscous oil
II-119	t-Bu	CN	H	A31	116-117
II-120	t-Bu	CN	CO2(4-Me—Ph)	A31	92-93
II-121	t-Bu	CN	H	A26	133.2-135.4
II-122	t-Bu	CN	B7	A26	133.9-145
II-123	t-Bu	CN	H	A27	46-47
II-124	t-Bu	CN	H	A28	168-169
II-125	t-Bu	CN	H	A29	94.7-95.4
II-126	t-Bu	CN	B8	A29	viscous oil
II-127	t-Bu	CN	B8	A29	viscous oil#8
II-128	t-Bu	CN	H	A32	133.9-134.4
II-129	t-Bu	CN	H	A33	220-230
II-130	2,6-F2—Ph	CN	H	2,6-F2—Ph	138-143
II-131	2-pyridyl	CN	B7	A18	115-145
II-132	2-pyridyl	CN	H	A18	176-178
II-133	2-pyridyl	CN	H	A9	191.5-195
II-134	2-pyridyl	CN	B7	A9	101-103
II-135	2-pyridyl	CN	H	A8	211-216
II-136	2-pyridyl	CN	H	A10	189-193
II-137	2-pyridyl	CN	CO2(4-F—Ph)	A10	137-142
II-138	2-pyridyl	CN	H	A24	188-191.5
II-139	2-pyridyl	CN	B7	A24	160-163.5
II-140	2-pyridyl	CN	B7	A30	123-125
II-141	2-pyridyl	CN	H	A30	165-166
II-142	2-pyridyl	CN	H	A13	149.5-151
II-143	NMePh	CN	H	A7	161.5-164
II-144	NMePh	CN	B7	A7	120-123
II-145	NMePh	CN	H	A2	vitreous state
II-146	NMePh	CN	B7	A2	vitreous state
II-147	1-piperidyl	CN	B3	A2	165.5-169
II-148	1-piperidyl	CN	H	A2	151-153
II-149	1-piperidyl	CN	H	A7	187-190
II-150	1-piperidyl	CN	B8	A7	viscous oil
II-151	1-piperidyl	CN	B8	A2	120-121.5
II-152	1-piperidyl	CN	B6	A2	viscous oil
II-153	1-naphthyl	CN	H	A2	161-163
II-154	1-naphthyl	CN	B7	A2	vitreous state
II-155	t-Bu	CO2Me	H	A2	viscous oil
II-156	1-Me-1-cHex	PO(OEt)2	H	A1	vitreous state
II-157	t-Bu	CO2Et	H	A1	viscous oil
II-158	t-Bu	CO2Et	B7	A1	viscous oil
II-159	1-Me-1-cHex	CN	H	A2	vitreous state
II-160	n-Pen	CN	H	A2	73-75
II-161	t-Bu	CN	B8	A32	108-112
II-162	t-Bu	CN	H	A1	viscous oil
II-163	t-Bu	CO2Me	H	A1	89-92
II-164	t-Bu	SO2Ph	H	A1	145-148
II-165	t-Bu	SO2Ph	B7	A1	122-123
II-166	t-Bu	SO2Ph	B7	A1	152-153#14
II-167	t-Bu	CO2Me	B7	A1	viscous oil
II-168	t-Bu	CO2Me	B7	A2	76-78
II-169	t-Bu	CO2CH2CH═CH2	H	A2	viscous oil
II-170	t-Bu	CO2CH2CH═CH2	B7	A2	viscous oil
II-171	1-Me-1-cHex	CN	B7	A2	vitreous state
II-172	n-Pen	CN	B7	A2	vitreous state
II-173	1-Me-1-cHex	CN	CH2O(CH2)2OCH3	A2	97-98*
II-174	t-Bu	5-Me-1,3,4-oxadiazol-2-yl	H	A1	vitreous state
II-175	t-Bu	5-Me-1,3,4-oxadiazol-2-yl	H	A1	vitreous state
II-176	t-Bu	Bu	H	A2	viscous oil
II-177	t-Bu	CN	B6	A13	104-107*
II-178	t-Bu	5-Me-1,3,4-oxadiazol-2-yl	B7	A1	134-137
II-179	t-Bu	5-Me-1,3,4-oxadiazol-2-yl	B7	A1	114-116#15
II-180	t-Bu	5-Me-1,3,4-oxadiazol-2-yl	B7	A1	86-90*
*E-form or Z-form
#4geometric isomer of II-40
#5geometric isomer of II-45
#6geometric isomer of II-108
#7geometric isomer of II-5
#8geometric isomer of II-126
#14geometric isomer of II-165
#15geometric isomer of II-178

TABLE 17
					m.p.
No.	R	E	B	A	(° C.)
III-1	Ph	CN	B4	A1	viscous oil*
III-2	Ph	CN	B5	A1	40-41*
III-3	t-Bu	CN	B1	A1	151-152*
III-4	t-Bu	CN	B4	A1	77-79*
III-5	t-Bu	CN	B6	A2	55-61*
III-6	t-Bu	CN	B7	A2	viscous oil*
III-7	2-pentyl	CN	B1	A1	viscous oil
III-8	4-tBu-Ph	CN	B1	A5	viscous oil
III-9	t-Bu	CN	Na	A2	165-174
III-10	t-Bu	CN	B9	A2	viscous oil
III-11	t-Bu	CN	B10	A2	185-186*
III-12	t-Bu	CN	B11	A2	viscous oil
III-13	2-NO2—Ph	CN	B9	A1	168-171*
III-14	1-naphthyl	CN	B9	A7	136-138*
III-15	t-Bu	CN	B7	A2	viscous oil#9
III-16	Ph	CN	B4	A1	solid#10
III-17	t-Bu	CN	B4	A1	viscous
					oil#11
III-18	2-Cl-6-F—Ph	CN	B7	A2	152-153
III-19	2,6-F2—Ph	CN	B7	A2	vitreous state*
III-20	Ph	CN	B5	A1	105-107#12
III-21	Ph	CN	B7	A2	viscous oil
*E-form or Z-form,
#9geometric isomer of III-6,
#10geometric isomer of III-1,
#11geometric isomer of III-4,
#12geometric isomer of III-2

TABLE 18
					m.p.
No.	G	E	B	A	(° C.)
IV-1	2-CF3	CN	H	A1	viscous oil
IV-2	3-CF3	CN	H	A1	159-163
IV-3	3-CF3	CN	B1	A1	174-175
IV-4	4-CF3	CN	H	A1	176-179
IV-5	4-CF3	CN	B1	A1	viscous oil
IV-6	2-CF3	CN	CSNMe2	A1	viscous oil
IV-7	3(1-CN-1-Me)-Et	CN	H	A1	viscous oil
IV-8	3(1-CN-1-Me)-Et	CN	B1	A1	148-155
IV-9	3-OPh	CN	H	A1	103-110
IV-10	3-OPh	CN	B7	A1	viscous oil
IV-11	4-OPh	CN	H	A1	148-150
IV-12	4-OPh	CN	B7	A1	viscous oil
IV-13	4-Et	CN	H	A1	148-149
IV-14	4-Et	CN	B7	A1	81-82
IV-15	4-Et	CN	B5	A1	viscous oil
IV-16	4-i-Pr	CN	H	A1	126-127
IV-17	4-i-Pr	CN	B7	A1	105-106
IV-18	4-t-Bu	CN	H	A1	117-118
IV-19	4-t-Bu	CN	B1	A1	viscous oil
IV-20	4-OCF3	CN	H	A1	128-129
IV-21	4-OCF3	CN	B7	A1	96-99
IV-22	3,4-methylene-dioxy	CN	H	A1	129-131
IV-23	3,4-methylene-dioxy	CN	B7	A1	viscous oil
IV-24	4-t-Bu	CN	B7	A2	viscous oil
IV-25	4-t-Bu	CN	B15	A2	viscous oil
IV-26	4-t-Bu	CN	H	A2	139-140
IV-27	4-t-Bu	CN	B7	A13	87-88
IV-28	4-t-Bu	CN	H	A13	141-142
IV-29	4-t-Bu	CN	B8	A2	vitreous state
IV-30	4-t-Bu	CN	H	A19	169.5-173
IV-31	4-t-Bu	CN	H	A20	vitreous state
IV-32	4-t-Bu	CN	B7	A20	146-148
IV-33	4-t-Bu	CN	B15	A14	viscous oil
IV-34	4-t-Bu	CN	B7	A19	vitreous state
IV-35	4-t-Bu	CN	B7	A1	viscous oil*
IV-36	4-t-Bu	CN	B8	A1	viscous oil
IV-37	4-t-Bu	CN	H	A24	vitreous state
IV-38	4-t-Bu	CN	B8	A24	vitreous state
IV-39	4-t-Bu	CN	CO2Et	A1	viscous oil
IV-40	4-t-Bu	CN	CO2iBu	A1	viscous oil
IV-41	4-t-Bu	CN	COCO2CH3	A1	viscous oil
IV-42	4-s-Bu	CN	H	A2	107-108
IV-43	4-s-Bu	CN	B15	A2	77-85
IV-44	4-i-Pr	CN	B15	A1	100-101
IV-45	4-i-Pr	CN	B15	A2	viscous oil
IV-46	4-i-Pr	CN	H	A2	98-99
IV-47	4-i-Pr	CN	B8	A2	viscous oil
IV-48	4-i-Pr	CN	CO(4-NO2—Ph)	A2	vitreous state
IV-49	4-Et	CN	B15	A1	viscous oil
IV-50	4-Ph	CN	H	A1	vitreous state
IV-51	4-Ph	CN	H	A2	vitreous state
IV-52	4-Ph	CN	H	A12	vitreous state
IV-53	4-Ph	CN	H	A13	167-169
IV-54	3,4-Cl2	CN	H	A1	vitreous state
IV-55	4-Cl	CN	H	A1	vitreous state
IV-56	2-F-4-CF3	CN	H	A2	vitreous state
IV-57	2-F-4-CF3	CN	B7	A2	vitreous state
IV-58	2-F-4-CF3	CN	B15	A2	vitreous state
IV-59	4-NO2	CN	H	A1	186-188
IV-60	4-MeO	CN	H	A1	108-110
IV-61	4-MeO	CN	B15	A1	viscous oil*
IV-62	4-i-PrO	CN	H	A1	127-131
IV-63	4-i-PrO	CN	H	A2	141.4-148.3
IV-64	4-i-PrO	CN	B15	A1	viscous oil
IV-65	4-i-PrO	CN	B15	A2	viscous oil
IV-66	4-i-PrO	CN	B6	A2	viscous oil
IV-67	4-n-BuO	CN	H	A1	101-104
IV-68	4-n-BuO	CN	B15	A1	75-70
IV-69	4-n-BuO	CN	H	A2	104.6-105.4
IV-70	4-n-BuO	CN	B8	A1	77.1-80.7
IV-71	4-n-BuO	CN	B15	A2	viscous oil
IV-72	4-t-amyl	CN	B15	A2	viscous oil
IV-73	4-allyloxy	CN	H	A1	vitreous state
IV-74	4-allyloxy	CN	B15	A1	vitreous state
IV-75	4-(Cl2C═CHCH2O)	CN	H	A1	vitreous state
IV-76	4-(Cl2C═CHCH2O)	CN	B15	A1	vitreous state
IV-77	4-(ClCCCH2O)	CN	H	A1	vitreous state
IV-78	4-PhCH2O	CN	H	A1	152.9-154.7
IV-79	4-PhCH2O	CN	H	A2	189-190.5
IV-80	4-PhCH2O	CN	B15	A2	123-129
IV-81	4-MeOCH2O	CN	H	A1	130.4-131.7
IV-82	4-CF3CH2O	CN	H	A1	100-103
IV-83	4-pivaloyl	CN	B15	A2	vitreous state
IV-84	4-pivaloyl	CN	H	A2	vitreous state
IV-85	4-Me2NCO2	CN	H	A2	vitreous state
IV-86	4-Me2NCO2	CN	B15	A2	vitreous state
IV-87	4-Me2NCO2	CN	B7	A2	vitreous state
IV-88	4-t-Bu	PO(OEt)2	H	A1	87-88
IV-89	4-t-Bu	PO(OEt)2	B1	A1	121-124
IV-90	H	Br	H	A1	74.5-75.5
IV-91	H	CO2Et	H	A1	viscous oil
IV-92	H	Br	B7	A1	viscous oil
IV-93	4-t-Bu	PO(OEt)2	H	A2	viscous oil
IV-94	4-t-Bu	CN	COCO2Et	A1	viscous oil
IV-95	4-t-Bu	CN	CO2iBu	A2	viscous oil
IV-96	4-t-Bu	CN	CO2iBu	A13	104-105
IV-97	4-t-Bu	SO2Ph	H	A1	143-145
IV-98	H	CO2Et	B7	A1	viscous oil
IV-99	4-t-Bu	CN	B3	A1	viscous oil
IV-100	4-t-Bu	CN	B19	A1	vitreous state
IV-101	4-t-Bu	CN	CO(4-CO2Me—Ph)	A2	vitreous state
IV-102	4-t-Bu	CN	CO(4-CO2Me—Ph)	A13	vitreous state
IV-103	4-t-Bu	CO2Me	H	A2	88-89
IV-104	4-t-Bu	CO2Me	H	A1	123-124
IV-105	4-t-Bu	CO2Me	B7	A1	77-78
IV-106	4-t-Bu	CO2Me	B7	A2	viscous oil
IV-107	4-t-Bu	SO2Ph	B7	A1	98-99
IV-108	4-t-Bu	SO2Ph	B7	A1	130-131#13
IV-109	4-t-Bu	CN	B3	A2	71-72*
IV-110	4-CHF2O	CN	H	A2	vitreous state
IV-111	4-CHF2O	CN	B15	A2	vitreous state
IV-112	4-CHF2O	CN	B7	A2	vitreous state
IV-113	4-CH3CONH	CN	H	A2	247.9-251.9
IV-114	4-CH3CONH	CN	B7	A2	82.1-84.3
IV-115	4-CO2Me	CN	H	A2	151-152
IV-116	4-CO2Me	CN	B7	A2	viscous oil*
IV-117	4-vinyl	CN	H	A2	vitreous state
IV-118	4-t-Bu	CN	B15	A1	78-82
IV-119	4-t-Bu	CN	methacryloyl	A1	viscous oil*
IV-120	4-t-Bu	CN	COCH═(CH3)2	A1	viscous oil
IV-121	4-t-Bu	CN	B33	A1	viscous oil
IV-122	4-t-Bu	CN	CH2OCH2Ph	A1	viscous oil
IV-123	4-t-Bu	CN	B24	A1	viscous oil
IV-124	H	Cl	H	A1	48-49
IV-125	4-t-Bu	5-Me-1,3,4-oxadiazol-2-yl	H	A1	149-151
IV-126	4-SMe	CN	H	A2	154-156
IV-127	4-SMe	CN	B7	A2	viscous oil*
IV-128	4-SOMe	CN	H	A2	vitreous state
IV-129	4-t-Bu	CN	B33	A2	viscous oil
IV-130	4-t-Bu	CN	B3	A13	111-112*
IV-131	4-t-Bu	CN	B7	A3	viscous oil
IV-132	4-t-Bu	CN	B3	A3	viscous oil
IV-133	4-t-Bu	CN	COCH2(4-OMe—Ph)	A1	117-121
IV-134	4-SO2Me	CN	B7	A2	vitreous state*
IV-135	4-SOMe	CN	B7	A2	vitreous state*
IV-136	4-OCH2Ph-3-Cl	CN	H	A2	vitreous state
IV-137	4-OPri-3-Cl	CN	H	A2	vitreous state
IV-138	4-OBui-3-Cl	CN	H	A2	vitreous state
IV-139	4-t-Bu	CN	B8	A3	viscous oil
IV-140	4-t-Bu	CN	B7	2-Cl-4-CF3-thiazol-5-yl	90-91
*E-form or Z-form
#13geometric isomer of IV-107

TABLE 19
No.	Q	R	E	B	A	m.p. (° C.)
V-1	Q9	1-Ph	CN	H	A1	148.7-151.3
V-2	Q9	1-Ph	CN	H	A2	156-157
V-3	Q9	5-Me-1-iPr	CN	H	A2	78-80
V-4	Q9	5-Me-1-iBu	CN	B7	A2	84-89*
V-5	Q9	5-Me-1-sBu	CN	B7	A2	99-105
V-6	Q9	5-Me-1-iBu	CN	H	A2	113-114
V-7	Q9	5-Me-1-sBu	CN	H	A2	75-80
V-8	Q9	1-t-Bu	CN	B7	A2	vitreous state*
V-9	Q9	1-t-Bu	CN	H	2,6-F2—Ph	111-113
V-10	Q9	1-t-Bu	CN	H	A2	127-129
V-11	Q9	1-pyridin-2-yl	CN	H	A2	156.4-158.1
V-12	Q9	1-pyridin-2-yl	CN	B15	A2	vitreous state*
V-13	Q9	1-pyridin-2-yl	CN	B7	A2	vitreous state*
V-14	Q10	1-Ph	CN	B7	A2	130-131
V-15	Q10	1-Ph	CN	H	A2	207-208
V-16	Q10	1-t-Bu	CN	B7	A2	viscous oil
V-17	Q10	1-t-Bu	CN	H	A2	viscous oil
V-18	Q11	1-Me-3-tBu	CN	H	A2	vitreous state
V-19	Q11	1-Me-3-tBu	CN	B7	A2	119-124
V-20	Q12	Ph	CN	H	A2	247-253
V-21	Q12	Ph	CN	B7	A2	147.5-148.5*
V-22	Q12	Ph	CN	SO2(4-tBu—Ph)	A2	174-176.5
V-23	2-naphthyl	—	CN	B1	A1	viscous oil
V-24	2-naphthyl	—	CN	H	A1	140.1-141.1
V-25	2-naphthyl	—	CN	B7	A1	viscous oil
V-26	Q13	—	CN	H	A2	121-122
V-27	Q1	5-Cl	CN	H	A2	160 (decomposition)
V-28	Q1	5-Cl	CN	B7	A2	79.5-81
V-29	Q2	4-Ph	CN	H	A1	231-232
V-30	Q2	4-t-Bu	CN	H	A1	218-219
V-31	Q3	3-Ph	CN	H	A1	243-245
V-32	Q4	Ph	CN	H	A1	255.8-256.8
V-33	Q4	Ph	CN	B1	A1	187-190
V-34	Q5	t-Bu	CN	H	A2	158-160
V-35	Q6	t-Bu	CN	H	A2	215-216
V-36	Q7	5-CF3	CN	H	A1	184-185
V-37	Q7	5-CF3	CN	H	A2	211-212
V-38	Q7	5-PhCH2O	CN	H	A1	220-221
V-39	Q8	4,6-(MeO)2	CN	H	A1	149-155
V-40	Q14	t-Bu	CN	H	A1	137.9-143.7
V-41	Q14	t-Bu	CN	B7	A1	vitreous state
V-42	Q14	t-Bu	CN	H	A2	127.5-128.9
V-43	Q14	t-Bu	CN	B7	A2	vitreous state
V-44	Q14	t-Bu	CN	B33	A2	vitreous state
V-45	Q14	t-Bu	CN	H	2,6-F2—Ph	105.6-108.1
V-46	Q14	t-Bu	CN	B7	2,6-F2—Ph	viscous oil
V-47	Q14	Ph	CN	H	A2	113.0-114.9
V-48	Q14	Ph	CN	B7	A2	vitreous state
V-49	Q14	Ph	CN	B15	A2	vitreous state
V-50	Q14	2-Cl—Ph	CN	H	A1	125.5-127.5
V-51	Q14	2-Cl—Ph	CN	B7	A1	104.0-107.5
V-52	Q14	2-Cl—Ph	CN	H	A2	142.4-143.6
V-53	Q14	2-Cl—Ph	CN	B15	A2	vitreous state
V-54	Q14	2-Cl—Ph	CN	B7	A2	vitreous state
V-55	Q14	2,6-F2—Ph	CN	H	A2	136.3-164.7
V-56	Q14	2,6-F2—Ph	CN	B15	A2	vitreous state
V-57	Q14	2,6-F2—Ph	CN	B7	A2	vitreous state
V-58	Q14	PhCH2	CN	H	A2	113.2-114.3
V-59	Q14	PhCH2	CN	B15	A2	vitreous state
V-60	Q14	PhCH2	CN	B7	A2	vitreous state
V-61	Q14	2-Cl—Ph	CN	H	2-MeO—Ph	131.4-132.8
V-62	Q14	2-Cl—Ph	CN	CO2-2-Oct	2-MeO—Ph	viscous oil
V-63	Q14	2-Cl—Ph	CN	B44	2-MeO—Ph	vitreous state
V-64	Q14	2-Cl—Ph	CN	H	2,6-F2—Ph	155.1-157.9
V-65	Q14	2-Cl—Ph	CN	B45	2,6-F2—Ph	159.3-160.3
V-66	Q14	2-Cl—Ph	CN	H	A7	150-152
V-67	Q14	2-Cl—Ph	CN	SO2(3-Cl—Ph)	A7	132-133
V-68	Q14	PhMe2C	CN	H	A2	vitreous state
V-69	Q14	PhMe2C	CN	B7	A2	vitreous state
V-70	Q14	PhMe2C	CN	COCH2OMe	A2	vitreous state
V-71	Q15	Ph	CN	H	A1	151-153
V-72	Q16	3-CN—Ph	CN	H	A1	174-175
V-73	Q17	5-CO2Et	CN	B7	A2	viscous oil
V-74	Q18	3-pyridin-2-yl	CN	H	A2	219 (decomposition)
V-75	Q19	5-Me-2-Ph	CN	H	A2	181-182
V-76	Q19	5-Me-2-Ph	CN	B7	A2	viscous oil
V-77	Q18	3-pyridin-2-yl	CN	B7	A2	vitreous state
V-78	Q18	3-pyridin-2-yl	CN	B46	A2	vitreous state
V-79	Q18	t-Bu	CN	H	A2	110.4-110.8
V-80	Q20	6-I	CN	H	A2	205-208
V-81	Q20	6-I	CN	B7	A2	137-142
V-82	4-Ph-oxazol-2-yl	—	CN	H	A2	165.9-166.7
V-83	4-Ph-oxazol-2-yl	—	CN	B15	A2	vitreous state
V-84	4-Ph-oxazol-2-yl	—	CN	B7	A2	vitreous state
V-85	Q19	5-Me-2-Ph	CN	H	A7	117-118
V-86	3-(2-Cl—Ph)-imidazolidin-2-on-1-yl	—	CN	H	A2	155-156
*E-form or Z-form

TABLE 20
No.	G	B	Y1	Y2	melting point (° C.)
VI-4	tBu	B33	H	Me	93.7-96.6
VI-5	tBu	Et	Me	H	resinous
VI-6	tBu	B33	Me	H	resinous
VI-7	tBu	Me	Me	Me	resinous
VI-8	tBu	Et	Me	Me	resinous
VI-9	tBu	B3	Me	Me	resinous
VI-10	tBu	B3	Me	Me	resinous
					(Isomer of VI-9)
VI-11	tBu	CH2OCH2Ph	Me	Me	resinous
VI-12	tBu	CH2OCH2Ph	Me	Me	resinous
					(isomer of VI-11)
VI-13	tBu	B24	Me	Me	resinous
VI-14	tBu	B32	Me	Me	resinous
VI-15	tBu	B32	Me	Me	resinous
					(Isomer of VI-14)
VI-16	tBu	B33	Cl	Me	66.5-67.45
VI-17	tBu	B33	Me	Br	94.0-95.0
VI-18	tBu	Et	H	Me	133.0-135.5
VI-19	tBu	B33	Me	Me	resinous (Z-form)
VI-20	tBu	B33	Me	Me	resinous
VI-21	tBu	H	Me	H	resinous
VI-22	tBu	H	H	Me	resinous
VI-23	tBu	H	Me	Me	resinous
VI-24	tBu	H	Cl	Me	68.0-69.0
VI-25	tBu	H	Me	Br	resinous
VI-26	sBu	H	Me	Me	resinous
VI-27	EtMe2C	H	Me	Me	resinous
VI-28	EtMe2C	H	Cl	Me	resinous
VI-29	tBu	B7	Me	Me	102.2-103.8
VI-30	tBu	B6	Me	Me	resinous
VI-31	tBu	CO(2-MeO—Ph)	Me	Me	resinous
VI-32	tBu	B26	Me	Me	resinous
VI-33	tBu	B7	Cl	Me	resinous
VI-34	tBu	COOiBu	Me	Me	resinous
VI-35	EtMe2C	B7	Me	Me	resinous
VI-36	sBu	B7	Me	Me	resinous
VI-37	tBu	CO(2-MeO—Ph)	Cl	Me	181.5-182.5
VI-38	tBu	B7	—(CH2)3—	105.3-106.8
VI-39	tBu	B7	MeO	Me	68.1-70.6
VI-40	tBu	B7	Me	H	resinous
VI-41	tBu	CO(2-Me—Ph)	Cl	Me	128.0-130.0
VI-42	tBu	CO(3-pyridyl)	Me	Me	resinous
VI-43	tBu	CO(2-Cl—Ph)	Me	Me	133.0-134.0
VI-44	tBu	CO(2-Cl—Ph)	Me	Me	150.0-151.0
					(Isomer of I-43)
VI-45	tBu	B7	Me	Br	118.0-119.0
VI-46	tBu	CO(3-Cl—Ph)	Me	Me	143.0-145.0
VI-47	tBu	CO(4-Cl—Ph)	Me	Me	169.0-170.0
VI-48	tBu	B5	Me	Me	resinous
VI-49	tBu	B2	Me	Me	110.6-111.8
VI-50	tBu	CO(2-Me—Ph)	Me	Me	127.0-128.0
VI-51	tBu	CO(3-Me—Ph)	Me	Me	111.0-112.0
VI-52	tBu	CO(4-Me—Ph)	Me	Me	134.5-136.0

TABLE 21
				melting point ° C.
No.	B	Y1	Y2	(ratio of isomer)
VII-1	H	H	H	pale brown solid
VII-2	H	H	Me	>200 (hydrochloride)
VII-3	H	Me	H	86.2-88.1
VII-4	H	Cl	Me	resinous
VII-5	H	H	Cl	resinous
VII-6	H	Cl	Et	resinous
VII-7	H	Me	Me	207-210
VII-8	H	—(CH2)3—	resinous
VII-9	Me	Me	Me	resinous
VII-10	CH2Ph	Me	Me	resinous
VII-11	B7	Me	Me	133.7-134.5
VII-12	B7	Me	Me	resinous (E-form)
VII-13	B7	H	Me	resinous (3/2)
VII-14	B7	H	Cl	resinous (20/1)
VII-15	B7	Me	H	resinous
VII-16	B7	Cl	Me	resinous (20/1)
VII-17	B7	Cl	Et	resinous (10/1)
VII-18	B6	Cl	Me	resinous (=3/1)
VII-19	B36	Cl	Me	resinous (5/1)
VII-20	B7	—(CH2)3—	resinous (5/1)
VII-21	B15	Me	Me	resinous (10/1)
VII-22	CO-cPen	Me	Me	resinous (10/1)
VII-23	B8	Me	Me	resinous (10/1)
VII-24	B6	Me	Me	resinous (10/1)
VII-25	CO(4-Me—Ph)	Me	Me	resinous (10/1)
VII-26	B40	Me	Me	resinous (10/1)
VII-27	CO(2-MeO—Ph)	Me	Me	resinous (10/1)
VII-29	B38	Me	Me	resinous (10/1)
VII-30	B36	Me	Me	resinous (10/1)
VII-31	B35	Me	Me	resinous (10/1)
VII-32	B37	Me	Me	resinous (10/1)
VII-33	B5	Me	Me	resinous (10/1)
VII-34	SO2Ph	Me	Me	resinous (10/1)
VII-35	SO2(4-Me—Ph)	Me	Me	resinous (10/1)
VII-36	SO2(4-CF3—Ph)	Me	Me	resinous (10/1)
VII-37	SO2(2,4,6-Me3—Ph)	Me	Me	resinous (10/1)
VII-38	B23	Me	Me	resinous (10/1)
VII-39	Et	Me	Me	resinous (7/1)
VII-40	B7	H	CF3	resinous
VII-41	B7	H	H	resinous (2/1)
VII-42	H	Cl	MeO	149.6-151.2
VII-43	B7	Cl	MeO	resinous
VII-44	H	MeO	Me	resinous
VII-45	H	MeO	Me	resinous

TABLE 22
No.	Q	R	B	A	melting point ° C.
VIII-1	Q21	Ph	H	A2	165.9-166.7
VIII-2	Q21	Ph	B15	A2	resinous
VIII-3	4-tBu—Ph	—	CH2O(4-Cl—Ph)	A1	resinous
VIII-4	Q19	5-Me-2-Ph	H	A7	117.0-118.0
VIII-5	A7	5-CF3	H	A38	74.0-77.0
VIII-6	4-tBu—Ph	—	B7	A48	145.0-146.0
VIII-7	Q19	5-Me-2-Ph	B3	A7	117.0-122.0
VIII-8	Q23	cHex	H	A13	resinous
VIII-9	Q23	tBu	SO2(3-Cl—Ph)	A13	resinous
VIII-10	Q23	1-naphtyl	H	A13	145.0-146.0
VIII-11	Q8	4-Cl—Ph	H	A2	212.0-214.0
VIII-12	Q24	2-pyridyl	B7	A2	182.0-183.0
VIII-13	3-Cl-4-CHF2O—Ph	—	B7	A2	resinous
VIII-14	Q22	tBu	CONMe2	A13	98.0-100.0
VIII-15	Q24	tBu	B7	A2	80.0-92.0
VIII-16	A22	2-pyridyl	B7	A2	133.0-134.0
VIII-17	Q19	5-Me-2-Ph	B7	A7	85.0-102.0
VIII-18	Q10	5-Me-1-(2-pyridyl)	H	A2	139.0-142.0
VIII-19	Q22	1-Me-cHex	H	A13	98.0-99.0
VIII-20	Q14	PhMe2C	B6	A13	resinous
VIII-21	Q22	tBu	B2	A13	resinous
VIII-22	Q22	nPen	H	A13	resinous
VIII-23	Q25	4-I	H	A13	177.5-178.2
VIII-24	Q25	4-I	B7	A2	resinous
VIII-25	Q22	tBu	B7	A39	resinous
VIII-26	Q22	nNon	H	A13	resinous
VIII-27	Q22	C17H35	H	A13	resinous
VIII-28	Q22	cPr	H	A13	88.8-89.7
VIII-29	Q22	cPen	B6	A13	resinous
VIII-30	Q22	PhMeCH	H	A13	resinous
VIII-31	Q22	nPrMe2C	H	A13	resinous
VIII-32	Q25	2-pyridyl	H	A41	261.0-262.0
VIII-33	Q25	4-COOMe	B7	A2	97.0-98.0
VIII-34	Q22	CH2═CHCH2CHMe	H	A13	resinous
VIII-35	Q22	3-Me-cHex	H	A13	resinous
VIII-36	Q22	4-Me—CHex	H	A13	resinous
VIII-37	Q22	2-Me-cPr	H	A13	resinous
VIII-38	Q22	sBu	H	A13	resinous
VIII-39	Q26	tBu	H	A13	134.3-135.7
VIII-40	Q22	Et2CH	H	A13	74.0-75.0
VIII-41	Q22	nPr2CH	H	A13	resinous
VIII-42	Q22	2-Me-cHex	B6	A13	resinous
VIII-43	Q22	cHep	H	A13	resinous
VIII-44	Q25	2-pyridyl	H	A42	270.0-272.0
VIII-45	Q22	2,3-(MeO)2—Ph	B7	A13	resinous
VIII-46	Q22	2-EtO—Ph	B7	A13	131.3-132.6
VIII-47	Q25	3-(2-pyridyl)	H	A21	resinous
VIII-48	Q25	3-(2-pyridyl)	B7	A14	84.0-85.0
VIII-49	Q25	3-(2-pyridyl)	H	A43	186.9-188.3
VIII-50	Q25	3-COOEt	B7	A2	resinous
VIII-51	Q22	2,4-Cl2—Ph	H	A13	137.5-138.5
VIII-52	Q22	2-Ph—Ph	H	A13	112.0-113.0
VIII-53	Q19	2-Ph	H	A10	232.5-235.6
VIII-54	Q19	2-Ph	B7	A10	resinous
VIII-55	Q25	5-(2-pyridyl)	B7	A10	resinous
VIII-56	Q25	3-COOiPr	H	A2	130.0-131.0
VIII-57	Q25	3-(2-pyridyl)	H	4-NH2-2-F—Ph HCl	114.3-117.5
VIII-58	Q25	3-(2-pyridyl)	B7	A22	resinous
VIII-59	Q25	3-(2-pyridyl)	B7	A44	resinous
VIII-60	Q25	3-(2-pyridyl)	H	A18	resinous
VIII-61	Q25	3-(2-pyridyl)	B7	A7	resinous
VIII-62	Q25	3-CN	B7	A45	resinous
VIII-63	Q25	3-(2-pyridyl)	B7	A49	resinous
VIII-64	Q25	3-(2-pyridyl)	H	A50	143.2-147.6
VIII-65	Q25	3-(2-pyridyl)	B7	A30	116.0-117.0
VIII-66	Q25	3-COOiPr	B7	A45	resinous
VIII-67	Q25	3-(4-pyridyl)	H	A45	resinous
VIII-68	Q25	3-(2-pyridyl)	B7	A46	140.7-144.5
VIII-69	4-tBu—Ph	—	B7	A42	resinous
VIII-70	Q25	3-(2-thienyl)	H	A47	resinous
VIII-71	Q22	cHep	H	A47	resinous
VIII-72	Q22	cHeP	B7	A47	resinous
VIII-73	4-tBu—Ph	—	B6	A42	resinous
VIII-74	4-tBu—Ph	—	B33	A42	62.0-63.0
VIII-75	Q22	tBu	B33	A47	resinous
VIII-76	Q27	2-pyridyl	B7	A45	144.0-145.0
VIII-77	Q27	2-pyridyl	H	A45	170.0-171.0
VIII-78	Q27	2-pyridyl	B7	A42	180.0-181.0
VIII-79	Q28	2-pyridyl	H	A45	resinous
VIII-80	Q28	2-pyridyl	B7	A45	resinous
VIII-81	Q19	5-Me-2-Ph	H	A47	resinous
VIII-82	Q19	5-Me-2-Ph	B7	A47	139.2-141.6
VIII-83	Q25	3-tBu-4-COOMe	B7	A47	115.0-116.0
VIII-84	Q22	EtMe2C	B7	A47	resinous
VIII-85	Q27	2-pyridyl	H	A3	139.0-140.0
VIII-86	4-tBu—Ph	—	B7	A49	93.6-95.2
VIII-87	Q9	1-(2-pyridyl)	H	A47	resinous
VIII-88	Q9	5-MeO-1-(2-pyridyl)	H	A47	resinous
VIII-89	4-tBu—Ph	—	H	A21	123.0-124.0
VIII-90	Q29	tBu	B7	A47	resinous
VIII-91	Q22	iBu	B7	A2	73.0-74.0
VIII-92	Q22	iBu	H	A2	62.0-63.0
VIII-93	4-tBu—Ph	—	B7	A14	98.0-99.0
VIII-94	Q22	tBu	B33	A52	92.0-93.0

Formulation Examples

Now, Formulation Examples of pesticides comprising the compounds of the present invention as the active ingredient are shown below, which, however, are not intended to restrict the scope of the invention. In the following Formulation Examples, “part” or “parts” are by weight.

Compound No. I-1 of the invention 50 parts
Zeeklite PFP (trade name, kaolin-type clay 43 parts
manufactured by Zeeklite Mining Industries,
Co., Ltd.)
Solpol 5050 (trade name, anionic surfactant 2 parts
manufactured by Toho Chemical Co., Ltd.)
Runox 1000C (trade name, anionic surfactant 3 parts
manufactured by Toho Chemical Co., Ltd.)
Carplex #80 (anti-caking agent, trade name, 2 parts
white carbon manufactured by Shionogi
Pharmaceutical Co., Ltd.)

The above-mentioned components were homogeneously mixed and ground to form a wettable powder.

Compound No. I-1 of the invention 3 parts
Methylnaphthalene                76 parts
Isophorone                       15 parts
Solpol 3005X (trade name, mixture of 6 parts
nonionic surfactant and anionic surfactant
manufactured by Toho Chemical Co., Ltd.)

The above-mentioned components were homogeneously mixed to form an emulsion.

Compound No. I-1 of the invention 35 parts
Agrisol S-711 (trade name, nonionic surfactant 8 parts
manufactured by Kao Corp.)
Runox 1000C (trade name, anionic surfactant 0.5 part
manufactured by Toho Chemical Co., Ltd.)
Aqueous solution of 1% Rhodopol (trade name, 20 parts
thickener manufactured by Rhone-Poulenc)
Ethylene glycol (freezing inhibitor) 8 parts
Water                            28.5 parts

The above-mentioned components were homogeneously mixed to prepare a flowable.

Compound No. I-1 of the invention 75 parts
Isoban No. 1 (trade name, anionic surfactant 10 parts
manufactured by Kuraray Isoprene Chemical
Co., Ltd.)
Vanilex N (trade name, anionic surfactant 5 parts
manufactured by Sanyo Kokusaku Pulp
Co., Ltd.)
Carplex #80 (trade name, white carbon 10 parts
manufactured by Shionogi Pharmaceutical
Co., Ltd.)

The above-mentioned components were homogeneously mixed and finely ground to form a dry flowable.

Compound No. I-1 of the invention 0.1 part
Bentonite                        55.0 parts
Talc                             44.9 parts

The above-mentioned components were homogeneously mixed and ground, to which was added a small amount of water, stirred, mixed and kneaded. The resulting mixture was granulated and dried into granules, using an extrusion granulator.

Compound No. I-1 of the invention 3.0 parts
Carplex #80 (trade name, white carbon 0.5 part
manufactured by Shionogi Pharmaceutical
Co., Ltd.)
Clay                             95 parts
Diisopropyl phosphate            1.5 parts

The above-mentioned components were homogeneously mixed and ground to form a dust.

Upon use, the wettable powder, emulsion, flowable and dry flowable are diluted from 50 to 20000 times with water, and applied in an amount of from 0.005 to 50 kg/ha in terms of the active ingredient.

Now, Formulation Examples of agents for preventing the attachment of aquatic organisms of the present invention are shown below, which, however, are not intended to restrict the scope of the invention.

Compound No. II-2 of the invention 8 parts
VYHH (vinyl-type synthetic resin 7 parts
manufactured by UCC Co., Ltd.)
Rosin                            7 parts
Tricresyl phosphate              3 parts
Talc                             20 parts
Barium sulfate                   15 parts
Red iron oxide                   10 parts
Xylene                           20 parts
Methyl isobutyl ketone           10 parts

The above-mentioned components were homogeneously mixed to form an agent for preventing the attachment of aquatic organisms of the invention. This agent can be used as a coating paint.

Compound No. II-2 of the invention 5 parts
CR-10 (chlorine rubber resin manufactured 13 parts
by Asahi Denka KK)
Zinc flower                      20 parts
Talc                             20 parts
Plasticizer                      2 parts
Red iron oxide                   10 parts
Xylene                           30 parts

The above-mentioned components were homogeneously mixed to form an agent for preventing the attachment of aquatic organisms of the invention. This agent can be used as a coating paint.

Compound No. II-2 of the invention 8 parts
VYHH (vinyl-type synthetic resin manufactured 7 parts
by UCC Co., Ltd.)
Rosin                            7 parts
Tricresyl phosphate              3 parts
Talc                             20 parts
Barium sulfate                   15 parts
Red iron oxide                   10 parts
Xylene                           20 parts
Methyl isobutyl ketone           10 parts

The above-mentioned components were homogeneously mixed to form an agent for preventing the attachment of aquatic organisms the invention. This agent can be used as a coating paint.

Compound No. II-2 of the invention 5 parts
CR-10 (chlorine rubber resin manufactured 13 parts
by Asahi Denka KK)
Zinc flower                      20 parts
Talc                             20 parts
Plasticizer                      2 parts
Red iron oxide                   10 parts
Xylene                           30 parts

The above-mentioned components were homogeneously mixed to form an agent for preventing the attachment of aquatic organisms of the invention. This agent can be used as a coating paint.

Test Examples

Now, the following Test Examples are to demonstrate the usefulness of the compounds of the present invention as pesticides.

Test Example 1

Insecticidal Test for Brown Rice Planthopper (Nilaparvata lugens Stal)

A 5% emulsion (or 25% wettable powder) of a compound of the present invention was diluted with water containing a spreading agent to give a 500 ppm solution of the compound.

The stems and leaves of rice-plants in 1/20,000 are pot were sufficiently applied with the resulting solution. After the thus-applied chemical solution was dried in air, each pot was covered with a cylindrical cover. Ten (10) second instar nymphae of brown rice planthoppers (Nilaparvata lugens) were released in each pot. After having been thus covered, the pots were stored in a thermostatic chamber. After 6 days passed, the insects in each pot were observed, and the mortality thereof was determined according to the following equation. Each compound was tested in that manner for two groups of pots.Mortality (%)=([number of insect killed/(number of insect killed+number of living insect)]×100

In this test, the following compounds exhibited mortality of 80% or more.

Compounds of the invention: Nos. I-2, I-18, I-19, I-23, I-30, I-31, I-32, I-35, I-39, I-42, I-44, I-58, I-59, I-62, I-63, I-70, I-72, I-80, I-106, I-114, I-123, I-137, II-1, II-2, II-3, II-5, II-6, II-12, II-15, II-23, II-25, II-26, II-28, II-33, II-34, II-36, II-37, II-38, II-39, II-43, II-44, II-46, II-53, II-54, II-55, II-61, II-66, II-73, II-74, II-75, II-76, II-80, II-83, II-84, II-85, II-86, II-87, II-88, II-89, II-91, II-92, II-93, II-97, II-98, II-111, II-114, II-116, II-134, II-136, II-137, II-154, II-155, II-159, III-1, III-2, III-4, III-6, III-15, III-16, III-17, III-18, III-19, III-21, IV-48, IV-58, V-2, V-12, V-13, V-28, V-48, V-49, V-51, V-53, V-54, V-55, V-56, V-57, V-59, V-60

Test Example 2

Insecticidal Test for Green Rice Leafhoppers (Nephotettix cincticeps Uhler)

The stems and leaves of plants was dipped in a 500 ppm emulsion of a compound of the invention for about 10 seconds. The thus-treated stems and leaves were put into glass cylinders, into which were released adults of green rice leafhoppers (Nephotettix cincticeps) that were resistant to organic phosphorous insecticides. Each glass cylinder was covered with a perforated cover, and stored in a thermostatic chamber at 25° C. After 6 days passed, the insects in each cylinder were observed, and the mortality of the insects was determined according to the same equation as in Test Example 1. Each compound was tested in that manner for two groups of cylinders. In this test, the following compounds exhibited morality of 80% or more.

Compounds of the invention: Nos. I-1, I-2, I-4, I-5, I-8, I-9, I-10, I-19, I-24, I-29, I-30, I-31, I-32, I-33, I-34, I-35, I-36, I-39, I-40, I-41, I-42, I-43, I-44, I-47, I-53, I-54, I-55, I-56, I-57, I-58, I-59, I-62, I-63, I-69, I-70, I-71, I-72, I-74, I-79, I-80, I-81, I-115, I-121, I-125, I-127, I-137, II-1, II-2, II-3, II-5, II-6, II-7, II-9, II-10, II-11, II-12, II-13, II-15, II-23, II-26, II-28, II-33, II-34, II-36, II-38, II-37, II-43, II-46, II-49, II-52, II-54, II-55, II-63, II-64, II-65, II-66, II-67, II-68, II-69, II-73, II-74, II-75, II-76, II-77, II-78, II-79, II-80, II-81, II-83, II-84, II-85, II-86, II-87, II-88, II-89, II-91, II-92, II-93, II-97, II-98, II-99, II-107, II-111, II-116, II-117, II-130, II-131, II-132, II-134, II-136, II-137, II-142, II-145, II-153, II-154, III-1, III-2, III-3, III-4, III-5, III-6, III-13, III-15, III-16, III-17, III-18, III-19, III-20, III-21, IV-32, IV-58, V-2, V-12, V-13, V-14, V-38, V-41, V-43, V-48, V-49, V-51, V-53, V-54, V-55, V-56, V-57, V-59, V-60, V-75

Test Example 3

Insecticidal Test for Green Peach Aphids (Myzus persicae Sulzer)

Moistured filter paper was placed in each laboratory glass dish having an inner diameter of 3 cm, and a leaf cabbage having the same diameter as that of the dish was put on the filter paper. Four female, apterous adults of green peach aphids (Myzus persicae) were put on the cabbage leaf. Fllowing day, a chemical sample (2.5 mg/cm²) was sprayed over the dishes, using a rotary sprinkler. The chemical solution herein was prepared by diluting a 5% emulsion (or 25% wetttable powder) of a compound of the invention to 500 ppm with water containing a spreading agent. After 6 days passed, the insects in each cylinder were observed, and mortality of the insects (larvae and adults) was determined according to the following equation. Each compound was tested in that manner for two groups of dishes.Mortality (%)=[number of insect killed/(number of insect killed+number of living insect)]×100

In this test, the following compounds exhibited mortality of 80% or more.

Compounds of the invention: Nos. I-1, I-2, I-3, I-4, I-5, I-7, I-8, I-9, I-10, I-11, I-12, I-13, I-14, I-16, I-17, I-18, I-19, I-21, I-22, I-23, I-24, I-25, I-26, I-27, I-28, I-29, I-30, I-31 I-32, I-33, I-34, I-35, I-36, I-37, I-38, I-40, I-41, I-42, I-43, I-44, I-45, I-46, I-47, I-48, I-51, I-52, I-53, I-54, I-55, I-56, I-57, I-58, I-59, I-62, I-63, I-69, I-70, I-71, I-72, I-73, I-74, I-76, I-77, I-78, I-79, I-80, I-81, I-84, I-85, I-86, I-89, I-90, I-92, I-96, I-97, I-104, I-108, I-125, I-136, I-137, I-138, II-2, II-3, II-5, II-6, II-7, II-8, II-9, II-10, II-11, II-12, II-15, II-16, II-17, II-23, II-24, II-25, II-26, II-27, II-28, II-33, II-34, II-35, II-36, II-37, II-38, II-39, II-43, II-44, II-50, II-52, II-53, II-54, II-55, II-58, II-60, II-63, II-64, II-65, II-66, II-68, II-69, II-70, II-71, II-73, II-74, II-75, II-76, II-78, II-79, II-83, II-84, II-85, II-86, II-87, II-88, II-89, II-90, II-91, II-92, II-93, II-97, II-98, II-99, II-101, II-102, II-105, II-107, II-111, II-116, II-117, II-118, II-121, II-130, II-131, II-132, II-133, II-134, II-136, II-137, II-138, II-140, II-141, II-142, II-151, II-153, II-154, II-159, II-160, III-1, III-2, III-3, III-4, III-5, III-6, III-15, III-16, III-17, III-18, III-19, III-20, III-21, IV-10, IV-11, IV-21, IV-23, IV-45, V-1, V-2, V-10, V-11, V-12, V-13, V-14, V-28, V-31, V-32, V-41, V-45, V-48, V-49, V-50, V-51, V-52, V-53, V-54, V-55, V-56, V-57, V-59, V-60, V-73, V-75, VII-1, VII-2, VII-3, VII-4, VII-5, VII-6, VII-7, VII-8, VII-9, VII-10, VII-11, VII-12, VII-13, VII-14, VII-15, VII-16, VII-17, VII-18, VII-19, VII-20, VII-21, VII-22, VII-23, VII-24, VII-25, VII-26, VII-27, VII-28, VII-29, VII-30, VII-31, VII-32, VII-33, VII-34, VII-35, VII-36, VII-37, VII-38, VII-39, VII-40, VII-41, VII-42, VII-43, VII-44, VII-45, VIII-12, VIII-32, VIII-42, VIII-47, VIII-49, VIII-55, VIII-57, VIII-58, VIII-61, VIII-64, VIII-65, VIII-67, VIII-85.

Test Example 4

Insecticidal Test for Diamond Back Moth (Plutella xylostella Linné)

The leaves of cabbage were dipped in a 500 ppm aqueous emulsion of a compound of the invention for about 10 seconds. After having been dried in air, the thus-treated leaves were put into laboratory dishes. Ten (10) second larvae of diamond back moth (Plutella xylostella) were released in each dish. Each dish was covered with a perforated cover, and stored in a thermostatic chamber at 25° C. After 6 days passed, the insects in each dish were observed, and mortality of the insects was obtained according to the same equation as in Test Example 1. Each compound was tested in that manner for two groups of dishes. In this test, the following compounds exhibited mortality of 80% or more.

Compounds of the invention: Nos. I-1, I-2, I-4 I-5, I-6, I-8, I-9, I-10, I-13, I-18, I-19, I-29, I-30, I-31, I-33, I-34, I-35, I-36, I-38, I-39, I-40, I-41, I-43, I-44, I-45, I-46, I-47, I-51, I-52, I-53, I-56, I-57, I-58, I-59, I-62, I-63, I-70, I-71, I-72, I-73, I-74, I-76, I-77, I-78, I-79, I-80, I-81, I-84, I-86, I-89, I-96, I-97, I-99, I-104, I-106, I-114, I-125, I-137, II-1, II-2, II-5, II-6, II-7, II-8, II-9, II-10, II-11, II-12, II-13, II-15, II-17, II-23, II-24, II-25, II-26, II-27, II-28, II-33, II-34, II-35, II-36, II-37, II-38, II-39, II-40, II-41, II-42, II-43, II-54, II-55, II-58, II-60, II-61, II-62, II-63, II-64, II-65, II-66, II-67, II-68, II-69, II-70, II-71, II-72, II-73, II-74, II-75, II-76, II-77, II-78, II-79, II-80, II-81, II-83, II-84, II-85, II-86, II-87, II-88, II-89, II-90, II-91, II-92, II-93, II-94, II-97, II-98, II-99, II-100, II-101, II-105, II-106, II-107, II-108, II-109, II-110, II-111, II-116, II-117, II-118, II-121, II-122, II-155, II-159, II-161, III-1, III-2, III-3, III-4, III-5, III-6, III-7, II-1-9, III-10, III-11, III-13, III-14, III-15, III-16, III-17, III-18, III-19, III-20, III-21, IV-7, IV-8, IV-29, IV-47, IV-53, IV-58, V-1, V-2, V-11, V-12, V-13, V-29, V-37, V-41, V-43, V-46, V-48, V-50, V-51, V-52, V-53, V-54, V-55, V-56, V-57, V-58, V-59, V-60, V-64, V-75

Test Example 5

Insecticidal Test for Cucurbit Leaf Beetles (Aulacophora femoralis Motschulsky)

A 5% emulsion (or 25% wettable powder) of a compound of the present invention was diluted with water containing a spreading agent to give a 500 ppm solution of the compound. The leaves of cucumbers were dipped in this chemical solution for about 10 seconds, dried in air, and put into a laboratory dish. Ten (10) second instar nymphae of cucurbit leaf beetles (Aulacophora femoralis) were released in each dish. Each dish was covered with a cover, and stored in a thermostatic chamber at 25° C. After 6 days passed, the insects in each dish were observed, and mortality of the insects was determined according to the same equation as in Test Example 1. Each compound was tested in that manner for two groups of dishes.

In this test, the following compounds exhibited mortality of 100%.

Compounds of the invention: Nos. I-1, I-2, I-4, I-6, I-8, I-9, I-10, I-11, I-12, I-13, I-29, I-30, I-31, I-32, I-33, I-34, I-35, I-39, I-40, I-41, I-43, I-44, I-46, I-53, I-54, I-55, I-56, I-57, I-58, I-59, I-61, I-62, I-63, I-69, I-70, I-71, I-72, I-74, I-76, I-77, I-78, I-79, I-80, I-81, I-82, I-83, I-92, I-101, I-103, I-104, I-108, I-109, I-124, I-127, I-128, II-1, II-6, II-7, II-8, II-9, II-10, II-11, II-12, II-13, II-14, II-15, II-16, II-17, II-23, II-24, II-25, II-26, II-27, II-28, II-33, II-34, II-35, II-36, II-37, II-38, II-39, II-41, II-42, II-43, II-47, II-50, II-53, II-54, II-55, II-57, II-58, II-61, II-62, II-63, II-65, II-66, II-99, II-101, II-102, II-104, II-105, II-106, II-107, II-108, II-109, II-110, II-114, II-122, II-124, II-125, II-131, II-132, II-133, II-134, II-136, II-137, II-139, II-140, II-141, II-142, II-153, II-154, III-1, III-2, III-3, III-4, III-5, III-6, III-9, III-10, III-11, III-12, III-14, III-15, III-16, III-17, III-20, IV-6, IV-13, IV-33, IV-39, IV-56, IV-60, IV-61, IV-72, IV-82, V-1, V-2, V-11, V-12, V-13, V-17, V-22, V-26, V-27, V-29, V-37, V-40, V-42, V-48, V-49, V-50, V-51, V-52, V-54, V-55, V-57, V-59, V-60, V-61, V-64, V-75

Test Example 6

Acaricidal Test for Two-Spotted Spider Mites (Tetranychus urticae Koch)

The leaves of kidney bean plants were punched into 3 cm-diameter discs, using a leaf punch, and put onto moistured filter paper in a 7 cm-diameter styrol cup. Ten (10) larvae of two-spotted spider mites (Tetranychus urticae) were put to each leaf. A 5% emulsion (or 25% wettable powder) of a compound of the invention was diluted with water containing a spreading agent to give a 500 ppm solution of the compound. The solution was sprayed over each cup in an amount of 2 ml/cup, using a rotary sprinkler, and the cups were stored in a thermostatic chamber at 25° C. After 96 hours passed, the mites in each cup were observed, and mortality of the mites was determined according to the same equation as in Test Example 1. Each compound was tested in that manner for two groups of cups.

In this test, the following compounds exhibited the mites at a percentage of 80% or more.

Compounds of the invention: Nos. I-1, I-2, I-3, I-4, I-5, I-7, I-8, I-9, I-10, I-12, I-13, I-19, I-24, I-25, I-26, I-27, I-28, I-29, I-30, I-31, I-32, I-33, I-34, I-35, I-36, I-38, I-40, I-41, I-42, I-43, I-44, I-45, I-46, I-47, I-48, I-50, I-51, I-52, I-55, I-56, I-57, I-58, I-59, I-60, I-61, I-62, I-63, I-70, I-71, I-72, I-74, I-76, I-80, I-94, I-95, I-96, I-97, I-99, I-101, I-102, I-103, I-104, I-105, I-106, I-108, I-109, I-110, I-111, I-112, I-113, I-114, I-115, I-117, I-118, I-119, I-122, I-123, I-124, I-125, I-126, I-127, I-128, I-137, II-2, II-3, II-5, II-6, II-7, II-8, II-9, II-10, II-11, II-12, II-13, II-15, II-16, II-17, II-23, II-25, II-26, II-27, II-28, II-33, II-34, II-35, II-36, II-37, II-38, II-39, II-40, II-41, II-42, II-43, II-45, II-46, II-47, II-48, II-50, II-52, II-53, II-54, II-55, II-58, II-59, II-60, II-61, II-63, II-64, II-65, II-66, II-67, II-68, II-69, II-70, II-71, II-72, II-73, II-74, II-75, II-76, II-77, II-78, II-79, II-80, II-81, II-83, II-84, II-85, II-86, II-87, II-88, II-89, II-90, II-91, II-92, II-93, II-95, II-97, II-98, II-99, II-101, II-102, II-103, II-105, II-106, II-107, II-108, II-109, I-110, II-111, II-116, II-117, II-118, II-133, II-134, II-136, II-137, II-151, II-153, II-154, II-155, II-159, II-160, II-161, II-173, III-3, III-4, III-5, III-6, III-7, III-9, III-10, III-11, III-12, III-15, III-17, III-18, III-19, III-21, IV-1, IV-2, IV-3, IV-4, IV-5, IV-7, IV-10, IV-11, IV-12, IV-13, IV-14, IV-16, IV-17, IV-18, IV-19, IV-20, IV-21, IV-22, IV-24, IV-25, IV-26, IV-28, IV-29, IV-33, IV-35, IV-36, IV-39, IV-40, IV-41, IV-42, IV-43, IV-44, IV-45, IV-46, IV-47, IV-48, IV-49, IV-50, IV-51, IV-54, IV-55, IV-56, IV-58, IV-59, IV-60, IV-61, IV-62, IV-63, IV-64, IV-65, IV-66, IV-67, IV-68, IV-69, IV-70, IV-71, IV-72, IV-74, IV-75, IV-76, IV-79, IV-80, IV-82, IV-94, IV-95, IV-96, IV-99, IV-100, IV-101, IV-102, IV-109, IV-110, IV-111, IV-112, V-1, V-2, V-3, V-4, V-5, V-6, V-7, V-8, V-10, V-11, V-12, V-13, V-14, V-15, V-16, V-17, V-19, V-23, V-24, V-25, V-26, V-28, V-31, V-36, V-37, V-38, V-40, V-41, V-42, V-43, V-44, V-46, V-47, V-48, V-49, V-50, V-51, V-52, V-53, V-54, V-55, V-56, V-57, V-58, V-59, V-60, V-73, V-75, VI-1, VI-2, VI-3, VI-4, VI-5, VI-6, VI-7, VI-8, VI-9, VI-10, VI-11, VI-12, VI-13, VI-14, VI-15, VI-16, VI-17, VI-18, VI-19, VI-20, VI-21, VI-22, VI-23, VI-24, VI-25, VI-29, VI-30, VI-31, VI-32, VI-33, VI-34, VI-35, VI-36, VI-37, VI-38, VI-39, VI-40, VI-41, VI-42, VI-43, VI-44, VI-45, VI-46, VI-47, VI-48, VI-49, VI-50, VI-51, VI-52, VIII-1, VIII-2, VIII-4, VIII-6, VIII-7, VIII-8, VIII-9, VIII-10, VIII-13, VIII-14, VIII-15, VIII-16, VIII-17, VIII-18, VIII-19, VIII-20, VIII-21, VIII-22, VIII-23, VIII-24, VIII-26, VIII-27, VIII-28, VIII-29, VIII-30, VIII-31, VIII-33, VIII-34, VIII-35, VIII-36, VIII-37, VIII-38, VIII-39, VIII-40, VIII-41, VIII-43, VIII-44, VIII-45, VIII-46, VIII-48, VIII-50, VIII-51, VIII-52, VIII-53, VIII-54, VIII-56, VIII-59, VIII-60, VIII-63, VIII-66, VIII-69, VIII-70, VIII-71, VIII-72, VIII-73, VIII-74, VIII-75, VIII-76, VIII-77, VIII-78, VIII-81, VIII-82, VIII-83, VIII-84, VIII-86, VIII-87, VIII-89, VIII-90, VIII-91, VIII-92, VIII-93.

Test Example 7

Test for Preventing Leaf Rust, Brown Rust (Puccinia recondita ex Desmaziére)

A chemical solution obtained by diluting an emulsion of a compound of the invention to 500 ppm with water was sprayed on wheat plants (Norin No. 61) grown to 1.5- to 2.0-leaf in a pot having a diameter of 5.5 cm-diameter at a dose of 20 ml/pot using a spraygun.

The following day, a spore suspension (2×10⁵ spore/ml) of leaft rust (brown rust) (Puccinia recondita) was sprayed over the plant-pots were placed overnight in an inoculation box having a temperature of 25° C. and a humidity of 95% or more. Then, the pots were put in a green house. After 7 days of the inoculation, a ratio of an infected and spored area formed to the leaf inoculated was measured, and a preventive vlaue was calculated according to the following equation.Preventive value=[1−(infected and spotted area ratio in treated region/infected and spotted area ratio in untreated region)]×100

In this test, the following compounds had an protective value of from 70 to 100.

Compounds of the invention: Nos. I-9, I-108, I-127, I-128, II-14, II-15, IV-2, IV-7, V-15, V-10.

With the long-term use of insecticides and microbicides, recently, some pests have become resistant to chemicals and are often difficult to exterminate with conventional insecticides and microbicides. In addition, some insecticides are highly toxic and are prone to remain long, without being decomposed, to destroy the ecosystem. Accordingly, the present invention provides novel, non-toxic and non-persistent insecticides and fungicides, and provides agents for preventing the attachment of aquatic organisms having few influences on the ecosystem and causing little secondary pollution.

Claims

1. Ethylene derivatives of a formula (I):

2. Ethylene derivatives as claimed in claim 1, wherein Q is a heterocyclic group optionally substituted by R, (said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,4,5-tetrazinyl, pyrazolinyl, imidazolinyl, imidazolinone or imidazolidinedione group; A is a phenyl group optionally substituted by W, or a heterocyclic group optionally substituted by Y, said heterocyclic group being a thienyl, furyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2,3,4-tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, pyrazolinyl or imidazolinyl group;B is H, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C2-C4 alkoxyalkyl group, CH3OC2H4OCH2, a C1-C4 alkylsulfonyl group, a phenylsulfonyl group optionally substituted by a halogen or a C1-C4 alkyl group, —SO2CF3, a C2-C8 dialkylaminosulfonyl group, a C2-C9 dialkylaminothiocarbonyl group, a C3-C9 alkoxycarbonylalkyl group, —C(═O)T1, —P(═O)T2T3, —P(═S)T2T3, an alkali metal atom, an alkaline earth metal atom, or NHT4T5T6; andT1 is a C1-C20 alkyl group, a C2-C6 alkenyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy-C1-C4 alkyl group, a C1-C4 alkyl group substituted by a phenyl group optionally substituted by a halogen or a C1-C4 alkyl group, a C3-C6 halocycloalkyl group, a C3-C6 cycloalkyl group optionally substituted by a C1-C3 alkyl group, a cycloalkyl group substituted by a phenyl group optionally substituted by a halogen or a C1-C4 alkyl group, a cyclopropyl group substituted by both a phenyl optionally substituted by a halogen or a C1-C4 alkyl group, and a C1-C4 alkyl group, a C3-C4 cycloalkyl group substituted by both a phenyl group optionally substituted by a halogen or a C1-C4 alkoxy group and a halogen, a cyclopropyl group substituted by both a C2-C4 alkenyl group optionally substituted by a halogen and a C1-C4 alkyl group, a C2-C4 alkenyl group substituted by a phenyl group optionally substituted by a halogen or a C1-C4 alkyl group, a C1-C12 alkoxy group, a C1-C4 haloalkoxy group, a C2-C5 alkenyloxy group, a C3-C6 cycloalkoxy group optionally substituted by a C1-C3 alkyl group, a benzyloxy group, a C2-C5 alkoxycarbonyl group, a phenyl group optionally substituted by Z, a phenoxy group optionally substituted by Z, a phenylthio group, a naphthyl group, or a heterocyclic group optionally substituted by Z, said heterocyclic group being selected from thienyl, furyl, oxazolyl, thiazolyl, pyrazolyl and pyridinyl groups.

3. Ethylene derivatives as claimed in claim 2, wherein Q is a heterocyclic group optionally substituted by R, said heterocyclic group being

4. Ethylene derivatives as claimed in claim 2 , wherein Q is an oxazolyl group optionally substituted by R, a pyrazolyl group optionally substituted by R, a pyridinyl group optionally substituted by R, or a pyrimidinyl group optionally substituted by R.

5. Ethylene derivatives as claimed in claim 4, wherein Q is an oxazolyl group optionally substituted by R.

6. Ethylene derivatives as claimed in claim 4, wherein Q is a pyrazolyl group optionally substituted by R.

7. Ethylene derivatives as claimed in claim 3, wherein Q is Q-9, Q-10, Q-11, Q-25, Q-26, Q-27, Q-28, Q-29, Q-30, Q-52, Q-53, Q-54, Q-55, Q-56 or Q-57.

8. Ethylene derivatives as claimed in claim 7, wherein Q is Q-10.

9. Ethylene derivatives as claimed in claim 7, wherein Q is Q-25, Q-26, Q-27, Q-28, Q-29 or Q-30.

10. Ethylene derivatives as claimed in claim 2, wherein A is a phenyl group optionally substituted by W, a thiazolyl group optionally substituted by Y, a pyrazolyl group optionally substituted by Y, a pyridinyl group optionally substituted by Y, or a pyrimidinyl group optionally substituted by Y.

11. Ethylene derivatives as claimed in claim 3 wherein Q is Q-31, Q-32, Q-33, Q-34, Q-35, Q-36, Q-37, Q-49,

12. Ethylene derivatives as claimed in claim 1, wherein the derivatives are selected from the following:

13. An agricultural composition containing, as an active ingredient, one or more ethylene derivatives of the claim 1.

14. A composition for preventing the attachment of aquatic organisms to fishing nets, the bottoms of ships, marine equipment, marine constructions, circulating water systems in thermal and atomic power plants, inlet channels for heat exchanger cooling water in chemical industry, underwater constructions, or reservoirs, the composition containing, as an active ingredient, one or more ethylene derivatives of the claim 1.