Difluorocarbene-enabled access to 1,3-oxazin-6-ones from enamides

Abstract

1,3-Oxazin-6-ones as important structural scaffolds widely exist in many bioactive or therapeutic agents. The development of straightforward synthetic approaches to access 1,3-oxazin-6-ones is highly desirable for studying their fundamental properties and applications. Herein, we report an efficient and general strategy for the construction of 1,3-oxazin-6-ones with high efficiency and chemoselectivity. Instead of using CO as a C1 source, difluorocarbene was introduced as a carbonyl provider. This method features readily available starting materials and valuable products, good functional group tolerance, and simple operation.