Aqua-organocatalyzed direct asymmetric aldol reaction with acyclic amino acids and organic bases with control of diastereo- and enantioselectivity

An effective aqua-organocatalytic direct aldol reaction is described. Aromatic amino acids can be a bifunctional catalyst system, which demonstrate excellent reactivity, diastereoselectivity, and enantioselectivity (up to 96% ee) in water without the addition of organic solvents. Furthermore, the present study demonstrates that both diastereo- and enantioselectivity can be easily modulated by the appropriate combination of an organocatalyst together with an organic base as a co-catalyst.

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