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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 donors to introduce NH₂ groups directly. Various strongly coordinating heterocycles including quinoline, pyrimidine, pyrazine, pyrazole and triazole were tolerated well. The potential utility was further demonstrated in a late-stage modification of telmisartan (an antagonist for the angiotensin II receptor).

SUBMITTER: Xu LL

PROVIDER: S-EPMC6001278 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature

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Copper mediated C-H amination with oximes: en route to primary anilines.

Xu Lin-Lin LL Wang Xing X Ma Biao B Yin Ming-Xing MX Lin Hai-Xia HX Dai Hui-Xiong HX Yu Jin-Quan JQ

Chemical science 20180514 23

Here we report an efficient Cu(i)-mediated C-H amination reaction with oximes as amino donors to introduce NH<sub>2</sub> groups directly. Various strongly coordinating heterocycles including quinoline, pyrimidine, pyrazine, pyrazole and triazole were tolerated well. The potential utility was further demonstrated in a late-stage modification of telmisartan (an antagonist for the angiotensin II receptor). ...[more]

PMID: 29997868

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