塞卡替尼的合成

Synthesis of saracatinib

目的:合成Src蛋白酪氨酸激酶抑制剂塞卡替尼,并对其工艺改进。方法:以2,4,6-三氟苯腈为原料,经氨解、水解、环合、取代得到塞卡替尼。结果:合成了塞卡替尼,目标产物结构经1H-NMR,MS确证,总收率为24.54%。结论:本方法具有可行性,适合工业化生产。

Objective： To synthesize the Src kinase inhibitor saracatinib, and optimize the synthetic process. Medthods： Saraeatinib was synthesized from 2,4 16-trifluorobenzonitrile through procedures of ammonolysis, hydrolysis, eyclization, and substitution. Results and Conclusion： Saraeatinib was synthesized with a total yield of 24.54% , and was verified by ^1H-NMR and MS. This synthetic method was suitable for large-scale production.