A Highly Stereoselective Synthesis of (3S,4S)-Statine and (3S,4S)-Cyclohexylstatine.

Abstract
The title compounds, which are synthetic intermediates of renin inhibitors, could be prepared from (S)-leucine and (S)-phenylalanine, respectively, by employing highly stereoselective aldol reactions of O-methyl-O-trimethylsilyl ketene acetal with an (S)-α-amino aldehyde in the presence of titanium(IV) chloride as a key step. Maximum diastereoselectivity of the aldol reaction was found to be more than 95 : 5.

This publication has 0 references indexed in Scilit: