Process for the preparation of N-sulfamyl-3-(2-guanidino-thiazol

Details Process for the preparation of N-sulfamyl-3-(2-guanidino-thiazol Process for the preparation of N-sulfamyl-3-(2-guanidino-thiazol

1987-07-23

1989-05-30

Gerstl, Robert

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D27742

Patent

active

048352810

ABSTRACT:
The invention relates to a new process for the preparation of N-sulfamyl-3-(2-guanidinothiazol-4-yl-methylthio)-propionitrile (famotidine) of the formula (I) ##STR1## by S-alkylation of 2-guanidino-thiazol-4-yl-methanethiol obtained from S-(2-guanidino-thiazol-4-yl-methyl)-isothiourea dihydrochloride of the formula (III) ##STR2## by in situ treatment with a base, which comprises carrying out S-alkylation with a N-sulfamyl-3-halopropionamidine of the formula (II) ##STR3## wherein X stands for halogen.

REFERENCES:
patent: 4283408 (1981-08-01), Hirata
patent: 4496737 (1985-01-01), Hoffman
patent: 4731479 (1988-03-01), Bod et al.

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