PROCESS FOR PREPARATION OF .alpha.-ALKYL AMINO ACIDS

摘要

A process for preparing .alpha.-alkyl amino acids by enantioretentive .alpha.-alkylation of .alpha.-amino acids is described. The process comprises the steps of converting an optically active acyclic .alpha.-amino acid to a 2-aryloxazolidinone compound in which the non-hydrogen substituent at the 4-position and the aryl group are in a cis relationship, stereospecifically alkylating the 2-aryloxazolidinone by first forming an alkali metal enolate by reacting the oxazolidinone compound with a strong base at greatly reduced temperatures followed by reacting the enolate with an alkylating agent, and generating the .alpha.-alkyl-.alpha.-amino acid from the alkylated 2-aryloxazolidinone by alkaline hydrolysis to open the ring followed by hydrolytic or reductive removal of the protecting group. The products are bioactive compounds including some useful as therapeutic agents.