FremgangsmÕte ved fremstilling av cykloheptimidazolderivater og synteseintermediat dertil

摘要

Disclosed is a method in which a compound of general formula (1) is reacted with a compound of general formula (2), followed by deprotection of protective group Z to give the cycloheptimidazole derivative (4) wherein R1 is hydrogen or isopropyl; R2 is a lower alkyl; A and A1 are each a substituent at the 4- or 8-position, A1 is hydrogen or hydroxyl when A is a hydrogen or A and A1 together form an oxo group or =CHCOOR3 (R3 represents a lower alkyl); the dotted line means two double bonds or saturated single bonds; X is halogen atom or trifluoromethanesulfonate group; Y is B (OH) 2 or -Sn (R5) 3 (R5 represents a lower alkyl group). The cycloheptimidazole derivative (4) is useful as antihypertensive agent. ( 1 ) (2) (4)