Design of organocatalysts for asymmetric direct syn-aldol reactions

Org Lett. 2007 Oct 11;9(21):4247-9. doi: 10.1021/ol701798x.

Abstract

Two new organocatalysts 3a and 3b, derived from L-leucine and (S)-beta-amino alcohols that were prepared from L-valine, were designed and afforded the direct syn-aldol reactions of a wide scope of aldehydes with various ketones with an excellent diastereomeric ratio of up to >20/1 and enantioselectivities of up to 99% ee.