Method of manufacturing the cycloheptimidazole derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 403/10 (2006.01) C07D 235/02 (2006.01) C07F 5/02 (2006.01) C07F 7/22 (2006.01)

Patent

CA 2156121

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, Al 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.

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