An Efficient Synthetic Process for Scale-Up Production of 4,5-Diamino-2-(trifluoromethyl)benzonitrile and 5-Bromo-3-(trifluoromethyl)benzene-1,2-diamine

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• 作者：Xun Li ; Raymond A. Ng ; Yongzheng Zhang ; Ronald K. Russell ; Zhihua Sui
• 刊名：Organic Process Research & Development
• 出版年：2009
• 出版时间：May 15, 2009
• 年：2009
• 卷：13
• 期：3
• 页码：652-655
• 全文大小：108K
• 年卷期：v.13,no.3(May 15, 2009)
• ISSN：1520-586X

文摘

Starting from 4-amino-2-(trifluoromethyl)benzonitrile (6), an efficient and nonchromatographic process was developed for multihundred gram production of 4,5-diamino-2-(trifluoromethyl)benzonitrile (1) in 73% yield and 98 HPLC area% purity over four synthetic steps. The same synthetic strategy was applied to 4-bromo-2-(trifluoromethyl)aniline (7) that afforded 5-bromo-3-(trifluoromethyl)benzene-1,2-diamine (5) in 81% overall yield and 99% HPLC area% purity.