Cumyl: A Better N-Protecting Group of α-Diazo Acetamides for Intramolecular CH Insertion Reaction and its Application in the Synthesis of Pregabalin and 3- …
Abstract Via intramolecular CH insertion of N-cumyl α-diazo acetamides, γ-lactams were efficiently synthesized with excellent regioselectivity. A concise route for the preparation of pregabalin (79% overall yield) and 3-benzyloxy pyrrolidine (21% overall yield) were reported.