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.
|