Sodium Methoxide‐Catalyzed Direct Amidation of Esters

Abstract The severe epimerization reaction is rectified by the addition of the rather acidic alcohol 4‐trifluorophenol. Under the optimized conditions using 4‐trifluorophenol, a catalytic ester‐amide exchange reaction of various N‐Boc protected chiral α‐amino esters with benzylamine proceeds in high yield without epimerization.