The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprising 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); 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); c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form a corresponding enantiomerically enriched compound of formula (Va) or (Vb); d) converting the compound of formula (Va) or (Vb) to form the corresponding enantiomerically enriched compound of tolterodine or analogue thereof; and e) optionally converting a compound obtained in base form to a salt thereof, or converting a salt form to the free base. Formulas (IIIa), (IIIb), (IVa), (IVb), (Va) and (Vb) are specified in the application. The invention also relates to novel starting materials and intermediates used in the process.