Abstract
Abstract A stereoselective synthesis of α-hydroxy phosphonates, a new class of transition state analog inhibitors is described. Methods of incorporating neutral and basic amino acid residues at the N-terminus of α-hydroxy-β-amino dimethyl phosphonate 8 are discussed. Incorporation of this novel functionality in a tripeptidic framework suitable for the aspartyl protease renin has led to the development of potent inhibitors of this enzyme.
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