Process for preparing benzothiazepine derivatives

Details Process for preparing benzothiazepine derivatives Process for preparing benzothiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/238.6

C07D 417/04 (2006.01) C07D 281/10 (2006.01)

Patent

CA 1284321

ABSTRACT OF THE DISCLOSURE Diltiazem and acid addition salts thereof are prepared by a process in which, in a first step, a 5-unsubstituted, 2- alkoxyphenylbenzothiazepine lactam of the general formula Image where R is, for example, methoxy, is reacted with a 2-haloethyl- N,N-dimethylamine in the presence of a strong organic base such as benzyltrimethylammonium hydroxide, to effect 5-N-substitution thereof. The resulting 5-N substituted lactam can then be acetylated, e.g. with acetic anhydride, to form diltiazem.

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