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氰基胍(4)是抗溃疡药西咪替丁(1)和抗高血压药吡那地尔(2)的重要组成部分,通常由相应的硫脲/脲制备,但多数要求分离碳化二亚胺或S-烷基异硫脲鎓盐中间体。本文报道应用水溶性的碳化二亚胺(WSC)由氰基硫脲(3)一步合成4的简便方法。 3和伯或仲胺于DMF中室温下加入1-(3-二甲氨基丙基)-3-乙基碳化二亚胺盐酸盐(WSC)(加料顺序对反应收率影响很大),搅拌反应30分钟,得相应4,7例收率60～85%。该法优于DCC法,而且3也并不都须分离,如异硫氰酸苯酯与氰氨基钠反应得3
Cyanoguanidine (4) is an important component of the antiulcer drug cimetidine (1) and the antihypertensive drug pinacidil (2), usually prepared from the corresponding thiourea / urea but most require the isolation of bis Imine or S-alkyl isothiuronium salt intermediate. This paper reports a simple and convenient method to synthesize 4 from cyano thiourea (3) using water-soluble carbodiimide (WSC). 3 and primary or secondary amines in DMF were added 1- (3-dimethylaminopropyl) -3-ethylcarbodiimide hydrochloride (WSC) at room temperature (the order of addition had a great effect on the reaction yield) The reaction was stirred for 30 minutes to give the corresponding 4,7 yield of 60 ~ 85%. This method is superior to the DCC method, and 3 are not all must be separated, such as phenyl isothiocyanate and sodium cyanide reaction 3