Journal
CHEMISTRYSELECT
Volume 4, Issue 15, Pages 4647-4651Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201900226
Keywords
amidination; C(sp(3))-H activation; Copper; Oxidative Methyl ketones; alpha-oxo-acetamidines
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Funding
- National Natural Science Foundation of China [21372068, 21572049]
- Science and Technology Program of Hunan Province, China [2014GK3115]
- Science and Technology Program of Changsha, China [K1508004-11]
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A convenient synthetic approach for the synthesis of alpha-oxo-acetamidines via copper-catalyzed C(sp(3))-H amidination has been developed. This approach allows the direct amidination of three C(sp(3))-H bonds without cyclization.Methyl ketones and primary and secondary amines are tolerant and afford the corresponding products in moderate to good yields. Furthermore, this protocol is also applicable to the synthesis of unsymmetrical alpha-oxo-acetamidines via one-pot, multicomponent reactions (MCRs).
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