尼鲁米特类化合物的合成 |
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引用本文: | 李倩,吴为忠,孙婧,吕伟,蔡俊超.尼鲁米特类化合物的合成[J].中国医药工业杂志,2004,35(8):455-456. |
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作者姓名: | 李倩 吴为忠 孙婧 吕伟 蔡俊超 |
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作者单位: | 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 |
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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%。
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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 |
文章编号: | 1001-8255(2004)08-0455-02 |
Synthesis of Nilutamide and Its Analogue |
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Abstract: | 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. |
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Keywords: | nilutamide 5 5-dimethyl-3-[4-cyano-3-(trifluoromethyl)phenyl]imidazolidin-2 4-dione antiandrogenagent synthesis |
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