Regio- and Stereoselective Synthesis of Polysubstituted γ-Lactams Enabled by Photocatalyzed Sequential Radical Aminoalkylation of MBH Acetates

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Abstract
A visible-light photocatalytic method is reported for the regio- and stereoselective synthesis of polysubstituted γ-lactams from N-arylglycines and Morita-Baylis-Hillman (MBH) acetates. The reaction proceeds through sequential radical aminoalkylation of the dual electrophilic MBH acetate by photogenerated α-aminoalkyl radicals, forming a key γ,γ'-diaminobutyl ester intermediate that undergoes regioselective lactamization. This strategy provides a mild and efficient route to privileged γ-lactam scaffolds, demonstrating the rational integration of two versatile synthons in cascade reactions.
Funding Information
  • Southwest University (SWU-XDZD22011)
  • National Natural Science Foundation of China (22378334)
  • National Natural Science Foundation of China (22477103)

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