Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India.
Molecular and Structural Biology, CSIR-Central Drug Research Institute, Lucknow, 226031, India.
Chem Asian J. 2020 Dec 14;15(24):4297-4301. doi: 10.1002/asia.202001160. Epub 2020 Nov 24.
The use of unsymmetric diaryliodonium salts as a versatile class of arylating agents has been demonstrated by developing a novel strategy to quickly access α-arylated α-fluoroacetoacetamides. The protocol provides a convenient metal-free method for the α-arylation of a diverse class of fluorinated acetoacetamides, and the products are obtained in good yields. The strategy, upon use of electron-deficient diaryliodonium salts as an arylating agent, provides α-fluoroacetamides through a spontaneous arylation/deacylation cascade.
使用不对称二芳基碘鎓盐作为一类多功能的芳基化试剂已经得到了证明，我们开发了一种新策略，能够快速获得α-芳基-α-氟代乙酰乙酸酰胺。该方案为各种氟化乙酰乙酸酰胺的α-芳基化提供了一种方便的无金属方法，并且以良好的产率得到了产物。该策略使用缺电子的二芳基碘鎓盐作为芳基化试剂，通过自发的芳基化/去酰化级联反应提供α-氟代乙酰乙酸酰胺。
