ECSP003862A - NEW PROCESS AND INTERMEDIARIES - Google Patents
NEW PROCESS AND INTERMEDIARIESInfo
- Publication number
- ECSP003862A ECSP003862A ECSP003862A ECSP003862A EC SP003862 A ECSP003862 A EC SP003862A EC SP003862 A ECSP003862 A EC SP003862A EC SP003862 A ECSP003862 A EC SP003862A
- Authority
- EC
- Ecuador
- Prior art keywords
- compound
- formula
- enantiomerically enriched
- converting
- defined above
- Prior art date
Links
Landscapes
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Un proceso para la preparación de enantioselectiva de tolterodina y análogos y sales de la misma que comprende pasos de: reducir enantioselectivamente la función carbonilo en un compuesto de fórmula (II): donde R1, R2 y R3 son independientemente entre sí, hidrógeno, metilo, metoxi, hidroxi, hidroximetilo, carbamoílo, sulfamoílo o halógeno, para formar un compuesto enriquecido enantioméricamente de fórmula (IIIa) o (IIIb) donde R1, R2 y R3 tienen la valores definidos anteriormente; someter al compuesto de fórmula (IIIa) o (IIIb) a un reordenamiento sigmatrópico para formar el correspondiente compuesto enriquecido enantioméricamente de fórmula (IVa) o ( IVb): donde R1, R2 y R3 tienen la valores definidos anteriormente; c) someter al compuesto de fórmula (IVa) o ( IVb) a una oxidación de Baeyer-Villiger para formar el correspondiente compuesto enriquecido enantioméricamente de fórmula general (Va) o ( Vb): donde R1, R2 y R3 tienen los valores definidos anteriormente; d) convertir elcompuesto de fórmula (Va) o ( Vb) para formar el correspondiente compuesto enriquecido enantioméricamente de tolterodina o análogos; y e) optativamente, convertir el compuesto obtenido en su forma básica en una sal del mismo o convertir la forma salina en la base libre. La invención también se relaciona con nuevos materiales iniciales e intermediarios usados en el proceso.A process for the preparation of tolterodine enantioselective and analogs and salts thereof comprising steps of: reducing enantioselectively the carbonyl function in a compound of formula (II): where R1, R2 and R3 are independently from each other, hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulfamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb) where R1, R2 and R3 have the values defined above; subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropic rearrangement to form the corresponding enantiomerically enriched compound of formula (IVa) or (IVb): where R1, R2 and R3 have the values defined above; c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form the corresponding enantiomerically enriched compound of general formula (Va) or (Vb): where R1, R2 and R3 have the values defined above ; d) converting the compound of formula (Va) or (Vb) to form the corresponding enantiomerically enriched compound of tolterodine or the like; and e) optionally, converting the compound obtained in its basic form into a salt thereof or converting the salt form into the free base. The invention also relates to new initial and intermediate materials used in the process.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ECSP003862 ECSP003862A (en) | 2000-12-29 | 2000-12-29 | NEW PROCESS AND INTERMEDIARIES |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ECSP003862 ECSP003862A (en) | 2000-12-29 | 2000-12-29 | NEW PROCESS AND INTERMEDIARIES |
Publications (1)
Publication Number | Publication Date |
---|---|
ECSP003862A true ECSP003862A (en) | 2001-07-27 |
Family
ID=42041409
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ECSP003862 ECSP003862A (en) | 2000-12-29 | 2000-12-29 | NEW PROCESS AND INTERMEDIARIES |
Country Status (1)
Country | Link |
---|---|
EC (1) | ECSP003862A (en) |
-
2000
- 2000-12-29 EC ECSP003862 patent/ECSP003862A/en unknown
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