PURPOSE: To obtain the titled compound useful for improving the stenocardiac pain advantageously in four steps, by passing through two novel substances from 2-(4-benzyloxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one.
CONSTITUTION: A compound of formula II is reacted with a dimethylaminoethyl halide, preferably chloride or hydrochloride, in the presence of an alkali metallic compound in a suitable solvent at room temperature W under heating to give a novel compound of formula III, which is then acetylated by the well-known method to afford a novel compound of formula IV. The resultant compound of formula IV is debenzylated in a solution of hydrogen bromide in acetic acid of an adequate concentration to give a compound of formula V, which is alkylated to afford a compound of formulaI(R is alkyl) useful for improving the stenocardiac parin in the angina of effort, etc. from an easily available raw material in high yield. The compound of formula IV or V is also useful for a coronary vasodilator.
UNEDA TAKASHI
SHINOO YASUTAKA
TAKATANI MASAHIRO
