Login| Sign Up| Help| Contact|

Patent Searching and Data


Title:
PRODUCTION OF 1,5-BENZOTHIAZEPINE DERIVATIVE
Document Type and Number:
Japanese Patent JPS60146884
Kind Code:
A
Abstract:

PURPOSE: To obtain the titled compound useful as pharmaceuticals, by condensing a specific thiophenol derivative with a propionic acid derivative, reacting with acetic anhydride after hydrolysis, and cyclizing the resultant threo-type propionic acid derivative with DCC.

CONSTITUTION: The objective compound of formula V, i.e. cis-2-(4'-methoxy- phenyl )-3-acetoxy-5-( N,N-dimethylaminoethyl )-2, 3-dihydro-1, 5-benzothiazepin-4- 5(H)one, is produced by (1) condensing the 2-(N,N-dimethylaminoethyl)aminothiophenol alkali metal salt of formula I (M is Na or K) with the erythro-type 3-(4- methoxy-phenyl)-3-chloro-2-hydroxypropionic acid methyl ester of formula II, (2) hydrolyzing the resultant threo-type propionic acid derivative with an alkali, (3) reacting with acetic anhydride in the presence of a base to obtain the compound of formula IV, and (4) carrying out the intramolecular cyclization reaction of the threo-type propionic acid derivative of formula IV with DCC (N,N'-dicyclohexylcarbodiimide).


Inventors:
MATSUMURA YOSHIO
Application Number:
JP170284A
Publication Date:
August 02, 1985
Filing Date:
January 09, 1984
Export Citation:
Click for automatic bibliography generation   Help
Assignee:
NIHON CHEMICAL KK
International Classes:
C07D281/10; (IPC1-7): C07D281/10
Attorney, Agent or Firm:
Kiyoshi Minoura