胺化
亲电胺化
芳基
化学
钴
苯甲酸酯
电泳剂
产量(工程)
羟胺
催化作用
有机化学
药物化学
组合化学
烷基
材料科学
冶金
作者
Yi‐Hung Chen,Simon Graßl,Paul Knochel
标识
DOI:10.1002/anie.201710931
摘要
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.
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