Process for preparing enantiomerically enriched amino-alcohols

Abstract

A process for preparing an enantiomerically enriched amino alcohol or derivatives thereof having the structure: wherein C* is a chiral carbon atom and R1 and R2 are independently selected from hydrogen, alkyl, alkoxy, aryl and a peptide chain, wherein said process includes the steps of: (a) providing an amino acid having the structure of Formula I: (b) protecting the amino group of the Formula I amino acid with a carbobenzoxy(Cbz) N-protecting group by reacting the amino acid with benzyl chloroformate in the presence of a base; (c) forming a carboxylic acid alkyl ester of the Cbz N-protected Formula I amino acid by reacting the amino acid with a C1-12 alcohol; and (d) reducing the Cbz N-protected amino acid ester with a borohydride reducing agent in an organic solvent or mixture of organic solvents to form a Cbz N-protected amino-alcohol

Dependencies are inferred from the claim text.