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Cu-Catalyzed intermolecular [3 + 3] annulation involving oxidative activation of an unreactive C(sp3)–H bond: access to pyrimidine derivatives from amidines and ketones

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Abstract

A facile and efficient approach for the synthesis of various pyrimidine derivatives from amidines and ketones via a Cu-catalyzed intermolecular oxidative coupling process using TEMPO/O2 as a co-oxidant has been developed. This novel protocol features unreactive C(sp3)–H bond amination, a wide range of substrates, good functional group tolerance and mild reaction conditions.

Graphical abstract: Cu-Catalyzed intermolecular [3 + 3] annulation involving oxidative activation of an unreactive C(sp3)–H bond: access to pyrimidine derivatives from amidines and ketones

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Publication details

The article was received on 22 Dec 2016, accepted on 21 Feb 2017 and first published on 27 Feb 2017


Article type: Research Article
DOI: 10.1039/C6QO00842A
Citation: Org. Chem. Front., 2017, Advance Article
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    Cu-Catalyzed intermolecular [3 + 3] annulation involving oxidative activation of an unreactive C(sp3)–H bond: access to pyrimidine derivatives from amidines and ketones

    W. Guo, D. Liu, J. Liao, F. Ji, W. Wu and H. Jiang, Org. Chem. Front., 2017, Advance Article , DOI: 10.1039/C6QO00842A

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