PURPOSE: To obtain the titled compound useful as a vasodilator for coronary blood vassel through a novel substance, by acetylating a 2-(4-hydroxyphenyl)-3- hydroxy-benzothiazepine derivative corresponding to the desired compound, followed by alkylation.
CONSTITUTION: A compound shown by the formual II is acetylated with acetic anhydride, glacial acetic acid, or acetl hydride in the absence of a solvent or in a basic solvent such as pyridine, trialkylamine, etc., to give a novel substance shown by the formula II. It is reacted with a dialkyl sulfate in the presence of an alkali to give a compound shown by the formulaI(R is alkyl, preferably 1W6C, especially methyl or ethyl) in high yield, having vasodilating action on coronary blood vessel and neurotropic action, useful as a remedy for angina of effort, breast pang in old myocardial infarction, etc. This method can be carried out by simple operations, and the alkylating agent is obtainable easily and inexpensively, so it is industrially advantageous.
UNEDA TAKASHI
SASAO YASUTAKA
TAKATANI MASAHIRO
| JP46016988A |