达沙替尼的合成工艺优化研究  

Optimization of Synthesis Technology of Dastinib

作　　者：谭桂林[1] 黄本东[1] TAN Gui-lin HUANG Ben-dong(School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China)

机构地区：[1]湖南中医药大学药学院,湖南长沙410208

出　　处：《精细化工中间体》2016年第5期18-21,24,共5页Fine Chemical Intermediates

摘　　要：以2-氨基噻唑-5-甲酸乙酯为原料,经过氨基保护、水解、经酰氯成酰胺、脱保护和两步亲核取代反应,合成了达沙替尼,反应总收率达53.4%。目标化合物经质谱、核磁共振氢谱确证结构。该合成工艺优化了反应条件,降低了生产成本,具有工业化生产前景。Dasatinb was synthesized from ethyl 2-aminothiazole-5-carboxylate through a series reactions including N-Boc protection, hydrolysis, chlorination, amidation, deprotection and two steps of nucleophilic substitution in an overall yield of 53.4%. MS and1 H NMR were used for structure identification. This technology provided a prospect for industrial production by optimizing the reaction conditions and reducing the production cost.

关 键 词：络氨酸激酶抑制剂 达沙替尼 2-氨基噻唑-5-甲酸乙酯 

分 类 号：TQ464.51[化学工程—制药化工]