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Process for preparing the d-threo isomer of methylphenidate hydrochloride - US Patent 6162919 (Site not responding. Last check: 2007-10-17) |
 | | 2,957,880 discloses a rather tedious sequence involving the resolution of the amide derivative of the corresponding erythro isomer, conversion to the threo isomer, followed by the hydrolysis of the amide to the corresponding acid, and esterification of the resulting acid with methanol. |
 | | In WO 97/27176, the d-threo enantiomer is prepared by resolving racemic threo methylphenidate employing a di-aroyltartaric acid, preferably a ditoluoyltartaric acid, whereas in WO 97/32851, the d-threo enantiomer is prepared by resolving racemic threo methylphenidate employing (-)-menthoxyacetic acid. |
 | | A resolution of the free base form of racemic threo methylphenidate with the recovered material yielded the desired phosphate salt enriched with the d-threo isomer of methylphenidate. |
| www.patentstorm.us /patents/6162919.html (3651 words) |