Magic Blue Initiated S N 2–Type Ring Opening of Azetidines with Electron‐Rich Arenes/Heteroarenes: Formal Synthesis of Nonracemic Tolterodine

A simple and atom‐economical protocol to access racemic and nonracemic γ , γ ‐diaryl/heteroaryl‐substituted propylamines in excellent yields (up to 98%) and with moderate enantiomeric excess (up to 62%) starting from azetidines and electron rich arenes/heteroarenes is described. The reaction involves Magic Blue‐initiated and incipient SbCl 5 ‐catalyzed S N 2‐type nucleophilic ring‐opening of activated azetidines with electron rich arenes/heteroarene under mild reaction conditions. The methodology has been efficiently used for the formal synthesis of optically active Tolterodine, an antimuscarinic drug.