Organocatalytic Asymmetric Synthesis of 1,2,4-Trisubstituted Azetidines by Reductive Cyclization of Aza-Michael Adducts of Enones

[摘要]：An efficient and highly enantioselective organocatalytic aza-Michael addition of N-substituted phosphoramidates to enones generates aza-Michael adducts which undergo intramolecular reductive cyclization with (R)-alpine borane to afford 1,2,4-trisubstituted azetidines in a one-pot procedure. These optically active products are obtained in good to high yields (67-93%) with excellent stereocontrol (78-96% ee) from a vast variety of enones.

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