N-Tosyl-(Sa)-binam-L-prolinamide as highly efficient bifunctional organocatalyst for the general enantioselective solvent-free aldol reaction.

[摘要]：N-Tosyl-(Sa)-binam-L-prolinamide (5 mol%; binam = 1,1'-binaphthyl-2,2'-diamine) and benzoate (1 mol%) were used as catalysts in the enantioselective direct aldol reaction between ketones and aldehydes under solvent-free conditions in the presence or absence of water. Under these reaction conditions, it was possible to reduce the amt. of required ketone to 2 equiv. to give the corresponding aldol products with high yields and regio-, diastereo-, and enantioselectivities. The aldol reaction between aldehydes or the intramol. aldol reaction can be also performed with excellent results.

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