期刊
NATURE CATALYSIS
卷 1, 期 2, 页码 120-126出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/s41929-017-0023-z
关键词
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资金
- NoNoMeCat Marie Sklodowska-Curie training network - European Union under the Horizon Programme [675020-MSCA-ITN-2015-ETN]
Amines are a quintessential moiety in bioactive molecules, pharmaceuticals and organic materials. Transition-metal-catalysed C-N coupling of aryl electrophiles has been established as a powerful and reliable method for amine synthesis. However, the analogous C-N coupling of alkyl electrophiles is largely under-developed due to the decomposition of metal alkyl intermediates by beta-hydrogen elimination and difficulty in C(sp(3))-N reductive elimination. Here, we provide a general strategy for amination of alkyl electrophiles by merging photoredox and copper catalysis. Photoredox catalysis allows the use of alkyl redox-active esters, recently established as a superior class of alkyl electrophiles, whereas copper catalysis enables C(sp(3))-N cross-coupling. Decarboxylative amination can be used for the synthesis of a diverse set of alkyl anilines with high chemoselectivity and functional-group compatibility. Rapid functionalization of amino acids, natural products and drugs is demonstrated.
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