达沙替尼的合成工艺改进

Process Improvement on Synthesis of Dasatinib

以3-乙氧基丙烯酰氯为起始原料,经酰化、环合及亲核取代反应合成靶向药物达沙替尼,总收率60.1%,纯度99.5%,其结构经~1H NMR确证。对合成工艺进行了优化,总收率由50.2%提高至60.1%。

The targeted antitumor drug,dasatinib,was synthesized by amidation,cyclization and nucleophilic substitution using（E）-3-ethoxyacryloyl chloride as the starting material. The total yield and purity were 60. 1% and 99. 5%,respectively. The structure was confirmed by^1H NMR. The synthetic method was optimized and the total yield increased from 50. 2% to 60. 1%.