PURPOSE: To obtain the subject novel compounds which inhibit the effects of angiotensin II as a vasopressor and a stimulator of aldosterone secretion and used for antihypertensives, anti-arteriosclerotics by reacting a sulfonylbenzyl with a nitrobenzoic acid ester and reducing the product.
CONSTITUTION: There are provided benzimidazoles of formula I [wherein R1 is a (substituted) 1-8C alkyl, a 3-8C cycloalkyl or the like; R2 is H, a halogen, a (substituted) 1-8C alkyl, an alkenyl, a 3-8C cycloalkyl or the like; R3 is a group of the formula: COR6 (wherein R6 is OH, a halogen, an alkoxyl or the like), a group of the formula: SO3H, a group of formula II (wherein R7 is H, a 1-6C alkyl, phenyl or the like) or the like; R4 is H, a halogen, a 1-8C alkyl or the like; and A is a three- to eight-membered saturated heterocyclic ring having up to two additional hetero atoms such as S, N or O bonded to A through the N atom] and salts thereof. These compounds can be obtained by reacting a sulfonylbenzyl compound of formula III (wherein L is a halogen) with a nitrobenzoic acid ester of formula IV in the presence of a base in an inert solvent and cyclizing the product in the presence of an iron powder and an acid.
TOOMASU KUREMAA
YURUGEN DORETSUSERU
PEETAA FUAI
BARUTAA HIYUPUSHIYU
URURIHI MIYURAA
MATEIASU MIYURAA GURIIMAN
MARUTEIN BOIKU
SUTANISURAFU KATSUDA
ANDOREASU KUNORU
YOHANESUUPEETAA SHIYUTASHIYU
SHIYUTEFUAN BOORUFUAIRU
KURAUDEIA HIRUTOODEIITORIHI
