Process for the preparation of benzothiazepine derivatives

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

1985-04-01

1986-01-28

Bond, Robert T.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07D28102

Patent

active

045669953

ABSTRACT:
The present invention relates to a process for the preparation of benzothiazepine derivatives of general formula I ##STR1## wherein R stands for hydrogen and acetyl or of acid addition salts thereof in which a corresponding compound of general formula II ##STR2## 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 hydrocarbon solvent in the presence of calcium hydroxide or of barium hydroxide. The process is advantageously performed at a temperature between 15.degree. and the refluxing temperature of the aliphatic polychlorinated hydrocarbon solvent. The process is optionally performed in the presence of a suitable 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.

REFERENCES:
patent: 3562257 (1971-02-01), Kugita et al.
patent: 4416819 (1983-11-01), Nagao et al.
patent: 4438035 (1984-03-01), Gaino et al.
patent: 4521430 (1985-06-01), Oh-Ishi et al.

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