| 摘要 |
PURPOSE:To obtain a non-peptidic new compound for oral administration having angiotensin II antagonism and vasodepressor action, useful as a therapeutic agent for circulatory system such as hypertension. CONSTITUTION:A compound of formula I [R<1> is (halo) lower alkyl, lower cycloalkyl, etc.; R<2> and R<3> are H, halogen, CmF2m+1 (m is 1-6), (CH2)nR<9> (R<9> is OH or alkoxyl; n is 1-4)], etc.; R<4> is H, halogen, lower alkyl, etc.; R<5> is H, halogen, COOH, etc.; R<6> is COOH, COOR<14> (R<14> is lower alkyl, etc.), etc.; R<7> and R<8> are H, halogen, lower alkyl, etc.], e.g. 2-{6-[(2-butyl-4-chloro-5-formyl-1H- imidazol-1-yl)methyl]quinolin-2-yl}benzoic acid methyl ester. The compound of formula I is obtained by reacting a compound of formula II (L is eliminable group; R<24> to R<28> are same as R<4> to R<8>) with imidazoles of formula III (R<21> to R<23> are same as R<1> to R<3>) in the presence of a base in aprotic solvent. |
