Novel primary–tertiary diamine organocatalysts derived from l-serine were utilized to promote enantioselective aldol reaction of acetone with α-ketoesters. The desired products were obtained in high yields and with good to excellent enantioselectivities (up to 95% ee).A novel primary–tertiary diamine organocatalyst-promoted enantioselective aldol reaction of acetone with α-ketoesters is described.
