| 摘要 |
PCT No. PCT/GB96/03103 Sec. 371 Date Jun. 19, 1998 Sec. 102(e) Date Jun. 19, 1998 PCT Filed Dec. 16, 1996 PCT Pub. No. WO97/22578 PCT Pub. Date Jun. 26, 1997A process for the optical resolution of racemic 3-(p-chlorophenyl)glutaramide (GAM) into its R isomer R-COOH and its S isomer S-COOH, which process includes the steps of either: (1) reacting racemic 3-(p-chlorophenyl)-glutaramide dissolved in a suitable solvent with S-(-)- alpha -methylbenzylamine of the formula H2N-S'(2) precipitating out of the solution of step (1) R-CO2-.H3+N-S'; (3) dissolving the precipitate of step (2) in water, with the addition of a suitable acid; and (4) precipitating out of the solution of step (3) R-COOH; or (5) reacting racemic -3-(p-chlorophenyl)-glutaramide dissolved in a suitable solvent with R-(+)- alpha -methylbenzylamine of the formula H2N-R'; (6) precipitating out of the solution of step (5) S-CO2-.H3+N-R'; (7) dissolving the precipitate of step (6) in water, with the addition of a suitable acid, and (8) precipitating out of the solution of step (7) S-COOH. The R isomer of GAM may be used for the production of R-baclofen and the S isomer of GAM may be used for the production of S-baclofen. |
