ABSTRACT A general and modular catalytic enantioselective route to 5‐substituted chiral oxazolines has been developed via palladium‐catalyzed intramolecular asymmetric allylic amidation. This strategy employs readily available racemic 2‐substituted‐5‐styryl oxazolidinones as substrates. Key to the success is the identification of a sterically hindered biphenol‐derived phosphoramidite ligand, which, in combination with Pd 2 (dba) 3 , promotes the cyclization with high efficiency and enantiocontrol. The reaction demonstrates broad substrate scope and excellent functional group tolerance, accommodating a wide range of sterically diverse 2‐substituents and electronically varied aryl allylic units, delivering the desired 5‐vinyl oxazolines in good yields with high enantioselectivity (up to 99% ee).
Su et al. (Sat,) studied this question.