Asymmetric Synthesis and Molecular Design of Peptidic Renin Inhibitors

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1.Development of Novel Chiral Synthons for Unusual Amino AcidsIntramolecular radical cyclizations of 2,2-dichloroacyl groups to the olefinic moiety of 2-oxazolone followed by dechlorination with (Me_3) _3SiH furnished an excellent route for the stereoselective preparation of 2-aminoalcohol chiral synthons with three ajacent asymmetric centers.2.Chiral Synthesis of Hydroxyamino Acids of Biological SignificanceDiastereoselective aldol reactions between alpha-amino aldehydes and N-acetyl derivatives of the chiral 2-oxazolidinones previously developed as chiral auxiliaries resultedin stereoselective formation of gamma-amino-beta-hydroxy acids which served as the compornents essential for the renin inhibitory peptides.3.Higly Efficient Catalytic Reductions of KetonesAsymmetric reduction of ketones with BH_3 proceeded with catalytic amount of the 2-aminoalcohol derived from the newly developed 2-oxazolidinone, HMCOx, to give the enantiomerically pure secondary alcohols.