Substituted benzimidazoles as angiotensin ii antagonist
1990
NEW MATERIAL: Compounds of formula 4 [R 1 is -CO 2 R 4 (wherein R 4 is H, a 1-6C alkyl, etc.), etc.; R 2a and R 2b are H, a halo, etc.; R 3a is H, a halo, etc.; R 3b is H, NO 2 , etc.; R 6 is an aryl, etc.; R 7a and R 7b are each H, a 1-6C alkyl, etc.; R 8a and R 8b are each H, an aryl-1-4C alkyl, etc.; and r is 1 or 2]. EXAMPLE: 2-Propyl-1-(2'-carboxypiphene-4-yl)methylbenzimidazole. USE: Antihypertensives, diuretics, angiotensinase inhibitors, and calcium channel blocking agents. PROCESS: An alkali metal of benzimidazole of formula 1 is directly alkylated by using a properly protected benzyl halide, a tosylate or a mesylate of formula 2 (Q is I, Br, etc.,) to obtain a compd. of formula 3. COPYRIGHT: (C)1991,JPO
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