Synthesis of Diverse Oxetane Amino Acids via Visible‐Light‐Induced Photocatalytic Decarboxylative Giese‐Type Reaction

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.