Process for the preparation of benzothiazepine derivatives
US4566995A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Apr 1, 1985 |
| Grant date | Jan 28, 1986 |
| Priority date | — |
| Expiry date | Apr 1, 2005 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D281/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.