Direct α-C(sp

The chemistry of site-selective C-H heteroarylation of aliphatic aldehydes is highly valuable, yet it remains inadequately explored. Hence, we demonstrated that aliphatic aldehydes undergo highly selective α-C(sp3)-H heteroarylation reactions under electrochemical oxygenation conditions. This transformation took place under environmentally friendly and external oxidant-free conditions, offering a broad and sustainable route to various aldehyde-functionalized pyrazinones. It provides a novel strategy for the efficient synthesis of heterocyclic compounds bearing aldehyde functionalities, utilizing readily available aliphatic aldehydes.