恩杂鲁胺的合成

Synthesis of Enzalutamide

目的:通过创新优化合成工艺、催化剂等使恩杂鲁胺的合成工艺适合工业化规模生产。方法:以4-溴-2-氟苯甲酸和4-氨基-2-三氟甲基苯甲腈为起始原料,经酰胺化、胺烷基化、甲基化及成环等一系列反应合成恩杂鲁胺。结果:优化后工艺路线的总收率53.4%,产物的结构经IR、~1HNMR、^(13)CNMR、MS得到确证。结论:优化后的合成工艺适合工业化规模生产。

Objective： Developing the enzalutamide＇s industrial synthesis process by an innovative approach to optimize the operation process, the catalyst and etc. Methods： Enzalutamide was synthesized from 4-bromo-2-fluorobenzoic acid and 4-Amino-2-trifluoromethyl-benzonitrile through a series of reactions including amidation, amine alkylation, methylation, cyclization and etc. Results： The product yield was 53.4 %. The structure of products was characterized by IR, 1HNMR, 13 CNMR and MS. Conclusion： The optimized synthetic process is suitable for industrial production.