A facile route for highly enantioenriched six‐membered 1,4‐N,N‐ and N,O‐heterocycles from L‐serinate‐derived α‐bromoacetates

Abstract

Preparation of highly enantioenriched six‐membered 1,4‐N,N‐ and N,O‐heterocycles has been developed through [4 + 2] heteroannulation of α‐bromoacetates with 1,4‐binucleophiles. Two consecutive substitutions of highly diastereoenriched L‐serinate‐derived α‐bromoacetates provide convenient access to a wide range of C‐aryl/aliphatic substituted 1,4‐N,N‐ and N,O‐heterocycles with up to 99:1 er.