The divergent synthesis of versatile 3,3’-disubstituted oxetane amino acids by utilizing visible-light-induced photocatalytic decarboxylative Giese-type reaction has been demonstrated.

Comprehensive Summary

The divergent synthesis of versatile 3,3′-disubstituted oxetane amino acids by utilizing visible-light-induced photocatalytic decarboxylative Giese-type reaction has been demonstrated. 3-Methyleneoxetane-derived substrates are readily available in a single-step and highly reactive as radical acceptors, allowing the production of versatile oxetane γ- and α-amino acids in high yields. A distinct ring strain release-driven radical addition mechanism was preliminarily revealed. The preparative power was further highlighted by the application in the synthesis of oxetane-containing dipeptides and azetidine amino acids, as well as the transformation of the product into novel oxetane-containing spiro-heterocycle pharmacophore.