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Title:
NOVEL ISOTHIOUREA DERIVATIVE AND ITS PREPARATION
Document Type and Number:
Japanese Patent JPS579760
Kind Code:
A
Abstract:

NEW MATERIAL:An isothiourea derivative of formula I (R is hydroxy group or chlorine).

EXAMPLE: N-Cyano-N'-(2-chloroethyl)-S-methyl isothiourea.

USE: Useful as an intermediate for the preparation of cimetidine which blocks histamine H2-receptor and has the remedying activity to gastric ulcer, duodenal ulcer, etc. The compound can be prepared from aminoethanol and chloroethylamine which are easily available in the market, and accordingly it has excellent industrial value.

PROCESS: The compound of formula I is prepared by reacting an ethylamine derivative of formula II with dimethylcyanoimide dithiocarbonate of formula III in a polar solvent at a temperature between room temperature and 110°C for 0.5W5 hours. The polar solvent is selected from those which do not directly concern with the reaction, e.g. alcohols.


Inventors:
FUJIMOTO DOUTAROU
FUNAZUKURI GIICHI
SHIGEARI TOSHIMITSU
SEKI KOUICHI
Application Number:
JP8553180A
Publication Date:
January 19, 1982
Filing Date:
June 23, 1980
Export Citation:
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Assignee:
FUJIMOTO SEIYAKU KK
International Classes:
C07C335/38; C07C67/00; C07C325/00; (IPC1-7): C07C157/14