摘要

An efficient asymmetric domino reaction of amino aldehyde to beta,gamma-unsaturated alpha-keto esters was achieved by using trans-perhydroindolic acid 1d as a chiral organocatalyst with excellent asymmetric behavior. Under the optimal reaction conditions, products with more than 99% de and up to 93% ee were obtained in high chemical yield (up to 98%) for a series of beta,gamma-unsaturated a-keto esters. The methodology provided an efficient route to dihydropyran derivatives containing many substituent groups (including amino groups).