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Copper Mediated C–H Amination with Oximes: En Route to Primary Anilines

Abstract

Here we report an efficient Cu(I)-mediated C−H amination reaction with oximes as amino donor to introduce NH2 group directly. Various strongly coordinating heterocycles including quinoline, pyrimidine, pyrazine, pyrazole and triazole were well tolerated. The potential utility was further demonstrated in a late-stage modification of Telmisartan (an antagonist for the angiotensin II receptor).

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Publication details

The article was received on 17 Mar 2018, accepted on 12 May 2018 and first published on 14 May 2018


Article type: Edge Article
DOI: 10.1039/C8SC01256C
Citation: Chem. Sci., 2018, Accepted Manuscript
  • Open access: Creative Commons BY-NC license
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    Copper Mediated C–H Amination with Oximes: En Route to Primary Anilines

    H. Dai, L. Xu, X. Wang, B. Ma, M. Yin, H. Lin and J. Yu, Chem. Sci., 2018, Accepted Manuscript , DOI: 10.1039/C8SC01256C

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