Synthesis of Axially Chiral CF3‐Substituted 2‐Arylpyrroles by Sequential Phosphine‐Catalyzed Asymmetric [3+2] Annulation and Oxidative Central‐to‐Axial Chirality Transfer

Abstract

AbstractA sequential phosphine‐catalyzed asymmetric [3+2] annulation of aldimines with allenoates and oxidative central‐to‐axial chirality transfer strategy has been developed. This approach is operationally simple, allowing for rapid access to a range of axially chiral CF3‐containing 2‐arylpyrroles with high enantiomeric excess. Furthermore, an atroposelective synthesis of esaxerenone is presented, illustrating the practical potential of the reported method.