Process for the preparation of benzothiazepine derivatives

Details Process for the preparation of benzothiazepine derivatives Process for the preparation of benzothiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/238.6

C07D 281/10 (2006.01)

Patent

CA 1223585

ABSTRACT The present invention relates to a process for the preparation of benzothiazepine derivatives of general formula I Image wherein R stands for hydrogen and acetyl or of acid addi- tion salts thereof in which a corresponding compound of general formula II Image in which R has the same meaning as above is reacted with 2-(dimethylamino)-ethyl chloride in a biphasic system of water and a non-combustible aliphatic polychlorinated hydro- carbon solvent in the presence of calcium hydroxide or of barium hydroxide. The process is advantageously performed at a temperature between 15° and the refluxing temperature of the aliphatic polychlorinated hydrocarbon solvent. The process is optionally performed in the presence of a suit- able quaternary ammonium halide. In the process the amount of calcium hydroxide or barium hydroxide is advantageously 1-3 moles per 1 mole of the compound of general formula II, the amount of aliphatic polychlorinated hydrocarbon solvent is advantageously 15-40 ml and that of water 3-10 ml per g of the compound of general formula II and the ratio aliphatic chlorinated hydrocarbon solvent:water is advantageously 2:1 to 10:1.

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