Subtle Strain-Release-Driven Aroylation of Four-Membered Rings via Decarboxylative Giese-Type Reactions

Four-membered rings are common in pharmaceuticals and
bioactive
natural products due to their ability to improve both potency and
metabolic stability. Herein, we report a subtle strain-release-driven
aroylation of four-membered Michael acceptors via decarboxylative
Giese reactions that occur under visible-light photoredox catalysis.
Our methodology leverages α-oxo acids as acylating agents and
uses strain release to overcome steric challenges that traditionally
hinder addition to β,β-disubstituted Michael acceptors.
The nature of strain release radical addition to strained rings further
offers a unique framework for the synthesis of complex molecules with
potential applications in drug discovery and medicinal chemistry.