Department of Chemistry, Room 18-490, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA.
Angew Chem Int Ed Engl. 2018 May 28;57(22):6672-6675. doi: 10.1002/anie.201802797. Epub 2018 Apr 30.
A CuH-catalyzed enantioselective hydroamidation reaction of vinylarenes has been developed using readily accessible 1,4,2-dioxazol-5-ones as electrophilic amidating reagents. This method provides a straightforward and efficient approach to synthesize chiral amides in good yields with high levels of enantiopurity under mild conditions. Moreover, this transformation tolerates substrates bearing a broad range of functional groups.
发展了一种使用易得的 1,4,2-二恶唑-5-酮作为亲电酰胺化试剂的 CuH 催化的对映选择性乙烯基芳基的氢酰胺化反应。该方法在温和条件下以良好的收率和高对映选择性提供了一种直接有效的合成手性酰胺的方法。此外,这种转化可以容忍具有广泛官能团的底物。