Asymmetric Mannich Reactions of β-Keto Esters with Acyl Imines Catalyzed by Cinchona Alkaloids

Abstract
Cinchona alkaloids catalyze the enantioselective Mannich reaction of β-keto esters with acyl aryl imines. The reaction requires 10 mol % of cinchonine or cinchonidine. The reaction products are obtained in good yields (81−99%), high enantioselectivities (80−96% ee), and in diastereoselectivities that range from 1:1 to >95:5. The cinchonine-catalyzed reaction provides access to highly functionalized building blocks used in the asymmetric synthesis of a dihydropyrimidone and β-amino alcohol.

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