达沙替尼的合成工艺优化研究

Optimization of Synthesis Technology of Dastinib

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.