A process for the preparation of N-sulfamyl-propionamidine derivatives
N-sulfamyl-propionamidine derivatives are prepared by the reaction of 3-substituted-propionitriles with an oxonium hydrochloride, preferably of 1,4-dioxane, in the presence of sulfamide in a close system at pressures between 0.5 kg/cm and 4.0 kg/cm. These compounds are useful in the preparation of famotidine, an anti-ulcer agent.
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(2008/06/13)
Process for the preparation of N-sulfamyl-3-(2-guanidino-thiazol-4-methylthio)-propionamidine
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.
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(2008/06/13)
N-sulfamyl-3-halopropionamidines
The invention relates to new propionamidine derivatives of formula (I) STR1 wherein X is halogen, and to a process for their preparation. According to the invention compounds of the formula (I) are prepared by reacting a 3-halopropionitrile of the formula (III) STR2 wherein X is as defined above, with sulfamide of the formula (II) STR3 in the presence of a hydrogen halide. Compounds of the formula (I) are useful intermediates in the preparation of famotidine.
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(2008/06/13)
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