尼鲁米特类化合物的合成  

Synthesis of Nilutamide and Its Analogue

作　　者：李倩[1] 吴为忠 孙婧[1] 吕伟[1] 蔡俊超[1] 

机构地区：[1]中国科学院上海药物研究所,上海201203 [2]苏州第一制药厂,江苏苏州215008

出　　处：《中国医药工业杂志》2004年第8期455-456,共2页Chinese Journal of Pharmaceuticals

摘　　要：用4-硝(氰)基-3-三氟甲基苯胺在硫酸中进行重氮碘代反应制得相应的碘苯化合物,在氧化亚铜催化下与5,5-二甲基乙内酰脲在DMF中反应制得抗雄激素类药物尼鲁米特及5,5-二甲基-3-[4-氰基-3-(三氟甲基)苯基]-2,4-咪唑烷二酮,总收率分别为68.9%和64.8%。Nilutamide and its analogue 5,5-dimethyl-3-[4-cyano-3-(trifluoromethyl)phenyl]imidazolidin-2,4-dionewere synthesized from 4-nitro- or 4-cyano-3-trifluoromethylaniline by diazotization and replacement with NaI to give corre-sponding iodo compounds, which subjected to nucleophilic substitution with 5,5-dimethylglycolylurea in the presence ofCu2O in DMF with an overall yield of 68.9% and 64.8%, respectively.

关 键 词：尼鲁米特 5 5-二甲基-3-[4-氰基-3-(三氟甲基)苯基]-2 4-咪唑烷二酮 抗雄激素 合成 

分 类 号：R979.9[医药卫生—药品]