Process for preparing imidazopyridine derivatives

Details Process for preparing imidazopyridine derivatives Process for preparing imidazopyridine derivatives

1994-09-19

1995-08-29

Dentz, Bernard

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D47104

Patent

active

054461600

ABSTRACT:
A new process for preparing imidazopyridines of the general formula: ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl or aralkyl group or is a heterocyclic radical, R.sub.2 and R.sub.4 are identical or different and are hydrogen, a hydroxy, a cyano, alkyl, cycloalkyl, aryl or aralkyl group or are an alkanoyl or an alkoxy-carbonyl group, and R.sub.3 is hydrogen, an alkyl, aryl or aralkyl group or a halogen atom. In the key step of the process, an imidate of the formula: ##STR2## is cyclized with aminoacetonitrile and a 1,3-dicarbonyl compound of the general formula: ##STR3## The imidazopyridines are valuable intermediates for the preparation of angiotensin II antagonists.

REFERENCES:
patent: 5066654 (1991-11-01), Taylor, Jr. et al.
patent: 5240938 (1993-08-01), Greenlee et al.
Katritsky and Rees, Comprehensive Heterocyclic Chem., Pergamon Press, vol. 5-part 4A, pp. 373, 374, 438, 439, 607 & 635-639 (1984).
J. Med. Chem., (1991), 34, pp. 2919-2922.
Brooker et al., J. Am., Chem. Soc., (1935), 57, pp. 2480-2488.
WO 93/23399 International Published Application, Nov. 1993.

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