Pd-Catalyzed C-S Activation/Isocyanide Insertion/Hydrogenation Enables a Selective Aerobic Oxidation/Cyclization

Org Lett. 2016 Aug 19;18(16):3984-7. doi: 10.1021/acs.orglett.6b01780. Epub 2016 Aug 8.

Abstract

Unique imidoylation of thioorganics with isocyanides endows an unprecedented aerobic oxidation process. Catalyzed by Pd(Ph3P)2Cl2 in the presence of Ph3SiH under N2 then upon exposure to air, a wide range of α-acyl ketene dithioacetals react with isocyanides to afford 5-hydroxy-α,β-unsaturated γ-lactams via a C-S bond activation, isocyanide migratory insertion, hydrogenation, selective aerobic oxidation, and intramolecular nucleophilic addition sequence.

Publication types

  • Research Support, Non-U.S. Gov't