| 摘要 |
The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprises the steps of:a) enantioselectively reducing the carbonyl function in a compound of formula (II):wherein R1, R2 and R3 independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb):wherein R1, R2 and R3 are as defined above;b) subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb):wherein R1, R2 and R3 are as defined above;c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form a corresponding enantiomerically enriched compound of the general formula (Va) or (Vb).wherein R1, R2 and R3 are as defined above;d) converting the compound of formula (Va) or (Vb) to form the corresponding enantiometrically enriched compound of tolterodine or analogue, ande) optionally converting a compound obtained in base form to a salt thereof, or converting a salt form to the free base.The invention also relates to novel starting materials and intermediates used in the process.
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