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Cobalt‐Catalyzed Electrophilic Amination of Aryl‐ and Heteroarylzinc Pivalates with N‐Hydroxylamine Benzoates
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2017-12-28 , DOI: 10.1002/anie.201710931
Yi-Hung Chen 1 , Simon Graßl 1 , Paul Knochel 1
Affiliation  

Aryl‐ and heteroarylzinc pivalates can be aminated with O‐benzoylhydroxylamines at 25 °C within 2–4 h in the presence of 2.5–5.0 % CoCl2⋅2 LiCl to furnish the corresponding tertiary arylated or heteroarylated amines in good yields. This electrophilic amination also provides access to diarylamines and aryl(heteroaryl)amines. A new tuberculosis drug candidate (Q203) was prepared in six steps and 56 % overall yield by using this cobalt‐catalyzed amination as the key step.

中文翻译:

N-羟胺苯甲酸酯的钴催化新戊酸芳基和杂芳基锌的亲电胺化反应

芳基-和三甲基乙酸盐heteroarylzinc可胺化以Ó在存在-benzoylhydroxylamines在25℃下2-4小时内2.5-5.0%氯化钴2 ⋅2的LiCl以提供相应的以良好的收率叔芳基化或heteroarylated胺。这种亲电胺化作用还提供了二芳基胺和芳基(杂芳基)胺的通道。使用该钴催化的胺化反应作为关键步骤,可以分六个步骤制备新的候选结核病药物(Q203),使总收率达到56%。
更新日期:2017-12-28
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