发明名称 PRODUCTION OF CYANOGUANIDINE DERIVATIVE
摘要 PURPOSE:To obtain the titled compound which is a histamine H2-receptor antagonistic agent in high purity and satisfactory yield in a simple step, by using 1-trityl-4-hydroxymethyl-5-carboalkoxyimidazole as a raw material. CONSTITUTION:A compound of formula I (R is lower alkyl) is reacted with a halogenating agent, perferably thionyl chloride, to give a compound of formula II (X is halogen), which is then reacted with N-cyano-N'-methyl-N''-(2-mercaptoethyl)guanidine under basic conditions under cooling or at room temperature to afford a compound of formula III. The resultant compound of formula IIIis then reduced with LiAlH4 or LiBH4 or NaBH4 in a solvent at 10 deg.C or below to give N-cyano-N'-methyl-N''-[2-{(4-hydroxymethyl-5-imidazolyl)methylthio}ethyl] guanidine of formula IV as crystals.
申请公布号 JPS59190973(A) 申请公布日期 1984.10.29
申请号 JP19830064289 申请日期 1983.04.12
申请人 FUJIMOTO SEIYAKU KK 发明人 FUJIMOTO DOUTAROU;SAKAI TAKESHI;TAKAMATSU SHIYUUHEI
分类号 C07D233/64;A61K31/415;A61P43/00 主分类号 C07D233/64
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