Claims
- 1. A process for the preparation of a compound represented by the formula: whereinG1 is a bond, CO or SO2, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, R4 is a hydrogen atom, a hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, an alkoxy group optionally having substituents, an aryloxy group optionally having substituents or an amino group optionally having substituents, and R5 is a cyclic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, which comprises:reacting a compound represented by the formula: wherein X1 is a halogen atom and X2 is a leaving group, with a compound represented by the formula: R2NH2 (VII) wherein R2 is as defined above, or a salt thereof, to give a compound represented by the formula: wherein R2 and X1 are as defined above, or a salt thereof; reacting the compound represented by the formula (IV) or a salt thereof with a trialkyl phosphite represented by the formula: (R3O)3P (V) wherein R3 is a lower alkyl group; thereafter reacting with a compound represented by the formula: wherein R1 is a hydrogen atom or an amino-protecting group, or a salt thereof, to give a compound represented by the formula: wherein R1 and R2 are as defined above, or a salt thereof; reducing and thereafter where necessary deprotecting the compound represented by the formula (III) or a salt thereof to give a compound represented by the formula: wherein R2 is as defined above, or a salt thereof; and reacting the compound represented by the formula (VIII′) or a salt thereof with a compound represented by the formula: wherein X3 is a leaving group and G1, R4 and R5 are as defined above, or a salt thereof.
- 2. The process of claim 1, wherein the compound represented by the formula (IV) or a salt thereof is reacted with the compound represented by the formula (V) in the presence of alkali metal iodide.
- 3. The process of claim 1, wherein the compound represented by the formula (II) or a salt thereof is reacted in the presence of a base.
- 4. A process for the preparation of a compound represented by the formula: whereinG1 is a bond, CO or SO2, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, R4 is a hydrogen atom, a hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, an alkoxy group optionally having substituents, an aryloxy group optionally having substituents or an amino group optionally having substituents, and R5 is a cyclic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, or a salt thereof, which comprises reacting a compound represented by the formula: wherein X3 is a leaving group and R5 is as defined above, or a salt thereof, with a compound represented by the formula: wherein G1 and R4 are as defined above, or a salt thereof, to give a compound represented by the formula: wherein G1, X3, R4 and R5 are as defined above, or a salt thereof, and reacting the compound represented by the formula (IX) or a salt thereof with a compound represented by the formula: wherein R2 is as defined above, or a salt thereof.
- 5. The process of claim 4, wherein R2 is a hydrogen atom, R4 is a methyl group, R5 is a phenyl group having 1 or 2 substituents selected from the group consisting of a halogen atom and a methyl group, G1 is a carbonyl, and X3 is a chlorine atom.
Priority Claims (1)
Number |
Date |
Country |
Kind |
2001-010354 |
Jan 2001 |
JP |
|
Parent Case Info
This application is the National Phase filing of International Patent Application No. PCT/JP02/00304, filed 18 Jan. 2002.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
PCT/JP02/00304 |
|
WO |
00 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO02/05723 |
7/25/2002 |
WO |
A |
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4690931 |
Wick et al. |
Sep 1987 |
A |
Foreign Referenced Citations (1)
Number |
Date |
Country |
04-312572 |
Nov 1992 |
JP |
Non-Patent Literature Citations (1)
Entry |
Zhou, et al, “A Practical Synthesis of 4-(Substituted-benzyl)piperidines and (±)-3-(Substituted-benzyl)pyrrolidines via a Wittig Reaction” J. Org. Chem 64(10): 3763-3766 (1999). |