Title:
PRODUCTION OF 1,5-BENZOTHIAZEPINE DERIVATIVE
Document Type and Number:
Japanese Patent JPS63307866
Kind Code:
A
Abstract:
PURPOSE: To introduce dimethylaminoethyl group into d-cis-3-OH-2,3-dihydro-2-(4- methoxyphenyl)-1,5-benzothiazepin-4(5H)-one, by reacting the compound with 2-Cl-N,N-dimethylethylamine.
CONSTITUTION: The objective compound of formula II can be produced in one step at a stroke in high purity and yield, by reacting the compound of formula I with the compound of formula II in an aprotic solvent in the presence of KF-Al2O3 at 20W30°C. The amount of KF-Al2O3 is 2W5 times equivalent (in terms of KF) based on the compound of formula I and the content of KF in KF-Al2O3 is usually 40wt.%. The compound of formula III is useful e.g. as a synthetic intermediate for diltiazem hydrochloride which is a drug having coronary vasodilating action.
Inventors:
NAKAMOTO YASUMASA
ISHIZUKA YORIYASU
FUTSUKAICHI OSAMU
OHIRA YUTAKA
ISHIZUKA YORIYASU
FUTSUKAICHI OSAMU
OHIRA YUTAKA
Application Number:
JP14239087A
Publication Date:
December 15, 1988
Filing Date:
June 09, 1987
Export Citation:
Assignee:
NIHON IYAKUHIN KOGYO CO LTD
International Classes:
C07D281/10; B01J27/12; C07B61/00; (IPC1-7): B01J27/12; C07D281/10
Attorney, Agent or Firm:
Heiyoshi Odashima