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.

中文翻译：

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大规模生产4,5-二氨基-2-（三氟甲基）苄腈和5-溴-3-（三氟甲基）苯-1,2-二胺的高效合成工艺

从4-氨基-2-（三氟甲基）苄腈（6）开始，开发了一种高效且无色谱的方法，用于以73％的收率和98 HPLC制备数克的4,5-二氨基-2-（三氟甲基）苄腈（1）。在四个合成步骤中的纯净面积百分比纯度。将相同的合成策略应用于4-溴-2-（三氟甲基）苯胺（7），以81％的总收率和99％HPLC获得5-溴-3-（三氟甲基）苯-1,2-二胺（5）面积％纯度。