2-氟-3-三氟甲基苯胺的合成研究  

Synthesis of 2-Fluoro-3-(trifluoromethyl)aniline

作　　者：杨东 刘辉 何立 YANG Dong;LIU Hui;HE Li(Shanghai Chemspec Corporation,Shanghai 200331,China)

机构地区：[1]上海康鹏科技股份有限公司,上海200331

出　　处：《有机氟工业》2022年第3期17-21,共5页Organo-Fluorine Industry

摘　　要：2-氟-3-三氟甲基苯胺是重要的合成普克鲁胺(Proxalutamide)——新一代雄激素受体拮抗剂的前体化合物。研究了以邻氟三氟甲苯为原料,先在-70~-60℃与正丁基锂和对甲苯磺酰叠氮依次反应合成2-氟-3-三氟甲基苯基叠氮中间体,再经氢化还原合成2-氟-3-三氟甲基苯胺。对各步反应条件进行了优化,合成总收率为91.7%。2-Fluoro-3-(trifluoromethyl) aniline is an important precursor compound for the synthesis of Proxalutamide,a new generation of androgen receptor antagonists.The intermediate 2-fluoro-3-(trifluoromethyl)phenyl azide was synthesized from 2-fluorobenzotrifluoride by reaction with n-butyllithium and p-toluenesulfonyl azide in turn at low temperature,followed by reduction with Hto give 2-fluoro-3-(trifluoromethyl)anilin.After the optimized reaction conditions of each step,the total synthesis yield was 91.7%.

关 键 词：邻氟三氟甲苯 2-氟-3-三氟甲基苯胺 对甲苯磺酰叠氮 合成 

分 类 号：TQ460.1[化学工程—制药化工]