biostudies-literatureUnknown9(13)Xie DA convenient method for the synthesis of 2-oxo-acetamidines from methyl ketones using aromatic amines and DMF as nitrogen sources is reported <i>via</i> copper-catalyzed C(sp³)-H amidination. Various methyl ketones react readily with aromatic amines and DMF, producing 2-oxo-acetamidines in yields of 47 to 92%. This protocol features the simultaneous formation of C-N and C[double bond, length as m-dash]N bonds using DMF and aromatic amines as two different nitrogen sources. It thus provides an efficient approach to construct acyclic amidines <i>via</i> three C(sp³)-H bond amidination. Based on the preliminary experiments, a plausible mechanism of this transformation is disclosed.RSC advances7203-7209https://www.ebi.ac.uk/biostudies/studies/S-EPMC9061129biostudies-literatureDirect synthesis of 2-oxo-acetamidines from methyl ketones, aromatic amines and DMF <i>via</i> copper-catalyzed C(sp³)-H amidination.PMC9061129Xie DGuo YHe WXiao JLiu QGuo CWu YfalseDirect synthesis of 2-oxo-acetamidines from methyl ketones, aromatic amines and DMF <i>via</i> copper-catalyzed C(sp³)-H amidination.A convenient method for the synthesis of 2-oxo-acetamidines from methyl ketones using aromatic amines and DMF as nitrogen sources is reported <i>via</i> copper-catalyzed C(sp³)-H amidination. Various methyl ketones react readily with aromatic amines and DMF, producing 2-oxo-acetamidines in yields of 47 to 92%. This protocol features the simultaneous formation of C-N and C[double bond, length as m-dash]N bonds using DMF and aromatic amines as two different nitrogen sources. It thus provides an efficient approach to construct acyclic amidines <i>via</i> three C(sp³)-H bond amidination. Based on the preliminary experiments, a plausible mechanism of this transformation is disclosed.2019-01-01T00:00:00Z2019 Mar2025-04-04T07:43:05.941Z2024-11-06T23:38:54.982ZS-EPMC90611293551995110.1039/c9ra00616h