Organocatalytic Regio‐ and Enantioselective N‐Alkylation of Isoxazol‐5‐ones

Abstract A chiral phosphoric acid catalyzed regio‐ and enantioselective reaction between 1‐acylamino‐3‐arylprop‐2‐yn‐1‐ols and isoxazol‐5‐ones has been developed for the first time. With the established protocol, N ‐alkylation of isoxazol‐5‐ones was achieved, affording enantioenriched N , N ‐acetals in 74–99 % yield with 72–88 % ee.