阿帕鲁胺合成路线图解

Graphical Synthetic Routes of Apalutamide

本文概述了阿帕鲁胺的合成方法。主要包括:阿帕鲁胺(1)的合成路线综述、关键中间体N-甲基-2-氟-4-(1-氰基环丁胺基)苯甲酰胺(2)、2-氰基-3-三氟甲基-5-氨基吡啶(3)合成方法的综述,得出结论:2(3)法制备阿帕鲁胺、1.1(2)法制备中间体2、1.2(3)法制备中间体3,这几类方法收率高、反应条件温和、成本较低,具备工业化潜力。

This article gives a comprehensive description of the synthetic routes of apalutamide (1), as well as the key intermediate4-((1-cyanocyclobutyl)amino)-2-fluoro-N-methylbenzamide (2) and 5-amino-3-(trifluoromethyl)picolinonitrile (3). In conclusion method2.3 for preparation of apalutamide, method1.1.2 for preparation of the intermediate2 and method1.2.3 for preparation of the intermediate3, which have high yield, mild reaction conditions, low cost and industrial potential.