【摘要】 以2-氯-6-甲基苯胺为起始原料,在吡啶的催化下,以99%的转化率得到酰化产物(E)-N-(2-氯-6-甲基苯基)-3-乙氧基丙烯酰胺(Ⅲ);Ⅲ在以水为主的溶剂中与N-溴代丁二酰亚胺(NBS)、硫脲经"一锅法"连续反应得化合物2-氨基-N-(2-氯-6-甲基苯基)-5-噻唑甲酰胺(Ⅴ);Ⅴ经纯化后与4,6-二氯-2-甲基嘧啶反应得化合物2-(6-氯-2-甲基嘧啶-4-氨基)-N-(2-氯-6-甲基苯基)-5-噻唑甲酰胺(Ⅵ);Ⅵ与1-(2-羟乙基)哌嗪缩合得达沙替尼(Ⅶ),总收率为71%。该合成方法条件温和、反应步骤少、收率高。更多还原

【Abstract】 Catalyzed by pyridine,compound Ⅲ was synthesized by using 2-chloro-6-methyl aniline as raw material with a yield of 99%.CompoundⅤ was synthesized from compoundⅢand NBS,thiourea in "one-pot" by using water as main solvent.CompoundⅥ was obtained by compoundⅤand 4,6-dichloride-2-methyl pyrimidine.And then dasatinib was synthesized from condensation reaction of compoundⅥ and 1-(2-hydroxyethyl)piperazine with total yield of 71%.This synthetic method has advantages such as moderate conditions,less reaction step,high yield.更多还原