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以1,1,3,3-四甲氧基丙烷为原料,经溴化铜溴代后,与硫脲缩合环化合成2-氨基噻唑-5-甲醛,再与2-氯-6-甲基苯胺在溴化亚铜和叔丁基过氧化氢(t-Bu OOH)作用下直接发生氧化酰胺化反应得到抗肿瘤药达沙替尼的重要中间体2-氨基-N-(2-氯-6-甲基苯基)噻唑-5-甲酰胺,总收率为81.3%。该方法合成路线短,原料价廉易得,反应收率高,生产成本低,避免使用易挥发的溴素以及会产生HCl的酰氯。
1,1,1,3,3-tetramethoxypropane as raw material, the bromination of copper bromide, with thiourea condensation cyclization of 2-aminothiazole-5-carboxaldehyde, and then 2-chloro-6-methyl Aniline was oxidized directly by cuprous bromide and tert-butyl hydroperoxide (t-Bu OOH) to obtain 2-amino-N- (2-chloro-2- -6-methylphenyl) thiazole-5-carboxamide was obtained in a total yield of 81.3%. The method has the advantages of short synthesis route, cheap raw materials, high reaction yield, low production cost, avoidance of volatile bromine and acid chloride which can generate HCl.