Process for the preparation of a benzothiazepine
AssigneeDsm N.V.
InventorsMarcus J. M. Plaum, Wilhelmus H. J. Boesten
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AssigneeDsm N.V.
InventorsMarcus J. M. Plaum, Wilhelmus H. J. Boesten
Estimating the term…
Process for the preparation of a 1,5-benzothiazepine derivative, or a salt thereof, of formula 1 ##STR1## where R1 represents H, an alkyl group or an alkoxy group and R.sub.2 represents H or a halogen, in which process a propanoic acid derivative of formula 2 ##STR2## where R.sub.1 and R.sub.2 are as defined above and R.sub.3 represents H or an alkyl group is subjected to an intramolecular cyclisation reaction in a non-halogenated solvent in the presence of a carboxylic acid. Preferably, R.sub.2 is H and R.sub.1 is OCH.sub.3. Trichloroacetic acid is preferably used as .alpha.-chlorinated acid. The benzothiazepine obtained on cyclisation can be subjected to an alkylation reaction and/or an acylation reaction to obtain known pharmaceutical products, in particular diltiazem.
A process for the preparation of a 1,5-benzothiazepine derivative, or a salt thereof, represented by the formula 1 ##STR7## where R.sub.1 represents H, an alkyl group or an alkoxy group and R.sub.2 represents H or a halogen, in which process a propanoic acid derivative represented by the formula 2 ##STR8## where R.sub.1 and R.sub.2 are defined above and R.sub.3 represents H or an alkyl group is subjected to an intramolecular cyclisation reaction in a non-halogenated solvent in the presence of a carboxylic acid, wherein the carboxylic acid comprises an .sub..alpha. -chlorinated carboxylic acid.
Dependencies are inferred from the claim text.