The development of a direct catalytic asymmetric Mannich reaction is shown and its potential demonstrated by the synthesis of optically active lactones via 4-hydroxyglutamic acid ester derivatives. The catalytic asymmetric Mannich reaction of carbonyl compounds with α-imino esters [Eq. (1); Ts = p-toluenesulfonyl] gives good yields and diastereoselectivities, as well as excellent enantioselectivities.

The catalytic asymmetric Mannich reaction of carbonyl compounds with -imino esters provides good yields, diastereoselectivity, and excellent enantioselectivity for the synthesis of optically active lactones.

Paper

Catalytic Asymmetric Direct Mannich Reactions of Carbonyl Compounds with α-Imino Esters.

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