题目：Brook-Oxidation Reaction of Acylsilanes: General Access to α-Ketoamides and α-Ketothioamides

作者：Dan-Ni Yang（杨丹妮、2022级研究生）, Ya-Nan Du, Peng Wang*（汪鹏）, and Man-Yi Han*（韩满意）

单位：Key Laboratory of Green and Precise Synthetic Chemistry and Application, Ministry of Education, Anhui Provincial Key Laboratory of Synthetic Chemistry and Applications, College of Chemistry and Materials Science, Huaibei Normal University, Huaibei, Anhui 235000, P. R. China

摘要：A novel chemoselective Brook-oxidation reaction of acylsilanes initiated by the carbamoyl anion has been successfully developed for the first time. This method enables the synthesis of diverse α-ketoamides and α-ketothioamides under transition metal-free and strong oxidant-free conditions with high yields and high chemoselectivity. It also demonstrates tolerance toward a wide range of functional groups. The synthetic utility of this process is underscored by its successful application in the synthesis of an orexin receptor antagonist from acylsilane, highlighting its potential for the development of novel therapeutic agents and further exploration in synthetic chemistry.

影响因子：4.9

分区情况：一区

链接：https://pubs.acs.org/doi/10.1021/acs.orglett.4c03889

（文：汪鹏 / 审核：韩满意 / 审校：曹静 / 终审：杨振兴）