| 摘要 |
PURPOSE:To obtain cimetidine, by condensing 4-methyl-5-chloromethylimidazole with N-cyano-N', S-ethyleneisothiourea in the presence of a base, reacting the condensation product with methylamine, making the reaction product into an alkali metal salt, heating the salt. CONSTITUTION:4-Methyl-5-chloromethylimidazole or its hydrochloride is reacted with N-cyano-N', S-ethyleneisothiourea in the presence of a base to give a compound shown by the formula III, this compound is reacted with methylamine to give a compound shown by the formula IV, which is made into an alkali metal salt and heated at about 80-150 deg.C to give a guanidine derivative, especially N-cyano-N'-methyl-N'' [(4-methyl-5-imidazolymethylthio)ethyl]guanidine(namely, cimetidine). USE:A remedy for gastric ulcer and duodenal ulcer, having H2-acceptor antagonism.
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