PREPARATION OF OPTICALLY PURE BETA-AMINO ACIDS HAVING AFFINITY FOR THE ALPHA-2-DELTA PROTEIN

摘要

Disclosed are materials and methods for preparing optically active beta-amino acids, which bind to the alpha-2-delta subunit of a calcium channel and are useful for treating pain, fibromyalgia, and a variety of psychiatric and sleep disorders. The method includes reacting a chiral allyl amine with a 2-alkynoate in the presence of a Lewis acid and a base to give a chiral tertiary enamine, which after reaction with ammonia, is hydrogenated to give optically active beta-amino acids.