Herein, we describe the dual C­(sp3)–H bond functionalization of a tertiary amine through hydride-transfer-induced dehydrogenation, followed by cycloaddition, using an easily preparable diazoester as a new type hydride-acceptor precursor under mild, redox-neutral conditions. With carbene as a hydrogen acceptor, this method was demonstrated by the preparation of a broad range of functionalized isoxazoldines in moderate to good yields.

Herein, we report a blue visible-light-promoted approach for preparing a variety of α-substituted γ-ketoester derivatives through carbene insertion and the decarbonylation of enaminones and diazoesters. These reactions use readily available starting materials and transition-metal-free, eco-friendly procedures that are amenable to gram-scale synthesis and wide functional group tolerance. This methodology may be useful for constructing polysubstituted heterocycles with potential biological activity.

A catalyst-free method for the highly regioselective hydrated ring-opening and formylation of quinazolinones was developed.