PREPARATION OF BETA-AMINO ACID PRECURSORS VIA INDIUM (III) MEDIATED MARKOVNIKOV ADDITION AND KNOEVENAGEL CONDENSATION

摘要

Disclosed are materials and methods for preparing precursors of optically active ß-amino acids, which bind to the alpha-2-delta (a2d) 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 malonate derivative with a terminal alkyne in the presence of an In(III) catalyst.