Preparation of n-aminoalkyl-1,5-benzothiazepine derivative

Abstract

Abstract PURPOSE:To obtain the titled compound for coronary vasodilators, etc. safely, by cyclizing an alpha-2-acyloxy-3-(substituted phenyl)-3-(2-aminophenylthio)-propionic acid derivative, and dialkylaminoalkylating the nitrogen atom at the 5-position of the resultant compound. CONSTITUTION:An alpha-2-acyloxy-3-(substituted phenyl)-3-(2-amino-phenylthio)- propinoic acid derivative of formulaI(X1 and X2 are H, halogen, alkyl or alkoxyl; R is alkyl) is reacted with a 1-substituted-2-halopyridinium salt of formula II (X3 is halogen; A<-> is ion of haogen, BF4, p-toluenesulfonic acid, methylsulfuric acid or perchloric acid respectively; Z is alkyl) in the presence of a tertiary amine to give a compound of formula III, which is then reacted with a compound of formula IV (X is halogen; Y is alkylene; R1 and R2 are alkyl) in the presence of a phase transfer catalyst and a base to afford the titled compound of formula V in high yield. USE:Psychotropic and nerve agents.

Inventors

• 👤 Yasumasa Nakamoto
• 👤 中本　泰正
• 👤 Naoyasu Ishizuka
• 👤 石塚　「い」康
• 👤 Osamu Futsukaichi
• 👤 二日市　修
• 👤 Yoshio Miyamura
• 👤 宮村　佳男

Bibliographic Details