Claims
- 1. A process for the preparation of a compound of the following Formula I: ##STR22## wherein A is N or CH;
- B is N or CR.sub.3 ;
- D is N or CR.sub.2 ;
- R, R.sub.1, are the same or independently hydrogen, hydroxy, loweralkyl, lower alkoxy, phenyloxy, R.sub.6 S(O).sub.n -, W-ALK-Q-, ##STR23## R.sub.2 is hydrogen, lower alkyl, phenyl which may be substituted by up to three methoxy groups, lower alkyl substituted by phenyl which may be substituted by up to three methoxy groups, -lower alkyl -N(R.sub.8).sub.2, ##STR24## pyridinyl or R.sub.3 is hydrogen, lower alkyl, phenyl, lower alkylphenyl, pyridinyl or loweralkyl pyridinyl;
- R.sub.4, R.sub.5 are the same or independently hydrogen or lower alkyl;
- R.sub.6 is lower alkyl, phenyl, lower alkylphenyl or pyridinyl;
- R.sub.7 are the same or independently hydrogen, loweralkyl, phenyl, pyridinyl, ##STR25## R.sub.8 are the same or independently lower alkyl, phenyl or pyridinyl; Q is ##STR26## W is hydroxy, loweralkoxy, phenoxy, -N(R.sub.10).sub.2, ##STR27## ALK is a C.sub.1 -C.sub.4 straight or branched chain alkyl; R.sub.9 is hydrogen, lower alkyl or phenyl;
- R.sub.10 are the same or independently hydrogen, loweralkyl or phenyl;
- R.sub.11 are the same or independently hydrogen or lower alkyl;
- X is CH.sub.2, O, S(O).sub.n, -NR.sub.10 ;
- n is the integer 0, 1 or 2 and
- p is the integer 0 or 1;
- with the provisos that:
- a) one and only one of B or D must be N;
- b) when A is CH, when D is N, when B is CR.sub.3 where R.sub.3 is H, when R.sub.2 is hydrogen, lower alkyl or phenyl then R and/or R.sub.1 must be ##STR28## or W-ALK-Q-; which comprises reacting a compound of the following Formula II: ##STR29## wherein R, R.sub.1, & R.sub.3 have the same meaning as above and wherein R.sub.2a & R.sub.2b have the same meaning as R.sub.2 and where one of R.sub.2a or R.sub.2b must be hydrogen; with a 1 to 4 equivalent excess of a doubly activated carbonic acid derivative in an inert aprotic solvent at a temperature of from about 150.degree. C. to about 200.degree. C. for about 30 min. to 6 h.
- 2. A process of claim 1 wherein said doubly activated carbonic acid derivative is carbonyldiimidazole, said inert aprotic solvent is 1,2-dichlorobenzene, said temperature range 175.degree.-180.degree. C. and said duration of the reaction about 1 h.
Cross Reference to Related Applications
This application is a division of U.S. Ser. No. 359,182 filed May 31, 1989 now U.S. Pat. No. 5,055,465.
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Name |
Date |
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4333394 |
Barnes et al. |
Jun 1982 |
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4440929 |
Lee et al. |
Mar 1984 |
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Non-Patent Literature Citations (1)
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Synthesis and Oral Antiallergic Activity of Carboxylic Acids Derived from Imidazo-etc.-Alger, et al. J. Med. Chem., 1988 31, 1098-1115. |
Divisions (1)
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Number |
Date |
Country |
Parent |
359182 |
May 1989 |
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