School of Chemistry and Chemical Engineering, South China University of Technology, No. 381, Wushan Road, Tianhe District, Guangzhou, PR China 510641.
Org Lett. 2011 Sep 16;13(18):4914-7. doi: 10.1021/ol2019955. Epub 2011 Aug 23.
C-Acylimines 1 undergo intermolecular amidation with amides 2 to produce monoacyl gem-diamino acid derivatives 3 upon treatment with Cu(OTf)(2) (20 mol%)/ PPh(3) (20 mol%) under mild conditions. This method provides an efficient access to gem-diamino acid equivalents with good to excellent yields.
C-酰亚胺 1 在温和条件下经 Cu(OTf)2(20 mol%)/PPh3(20 mol%)作用,与酰胺 2 发生分子间酰胺化反应,得到单酰基双氨 酸衍生物 3,产率良好至优秀。该方法为得到双氨 酸等价物提供了一种有效且温和的途径。