| 摘要 |
<p>This invention concerns a process of preparing optically active alpha -arylalkanoic acids useful as pharmaceutical (e.g., anti-inflammatory) agents, and their precursors. These alpha -arylalkanoic acids, esters, amides, nitriles, oxazolines and metal salts are stereoselectively prepared by forming the metal or metal halide of the corresponding acid, ester, amide, oxazoline, nitrile, or metal salt and treating the compound so prepared with an aryl halide in the presence of a chiral (optically active) transition metal catalyst, optionally in the presence of a dipolar aprotic solvent or mixtures thereof, for a time sufficient to form the corresponding optically active alpha -arylalkanoic acid, ester, amide, nitrile, oxazoline or metal salt, and optionally concomitantly or sequentially hydrolyzing any ester, amide, nitrile, oxazoline or metal salt formed to the corresponding optically active alpha -arylalkanoic acid. The process optionally further includes removal of halogen atom from the aromatic portion or methylation of the aryl hydroxyl portion of the alpha -arylalkanoic acid, as well as subsequent formation of the pharmaceutically acceptable salts and esters of the optically active alpha -arylalkanoic acid.</p> |
