Patent Number: 6,310,248

Title: Process and intermediates

Abstract: The invention relates to a process for the enantioselective preparation oftolterodine and analogues and salts thereof comprises the steps of:a) enantioselectively reducing the carbonyl function in a compound offormula (II):##STR1##wherein R.sub.1, R.sub.2 and R.sub.3 independently of each other arehydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoylor halogen, to form an enantiomerically enriched compound of formula(IIIa) or (IIIb):##STR2##wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above;b) subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropicrearrangement to form a corresponding enantiomerically enriched compoundof formula (IVa) or (IVb):##STR3##wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above;c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Virligeroxidation to form a corresponding enantiomerically enriched compound ofthe general formula (Va) or (Vb):##STR4##wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above;d) converting the compound of formula (IVa) or (IVb) to form thecoresponding enantiometrically enriched compound of tolterodine oranalogue, ande) optionally converting a compound obtained in base form to a saltthereof, or converting a salt form to the free base.The invention also relates to novel starting materials and intermediatesuse in the process.

Inventors: Andersson; Pher G. (Uppsala, SE), Hedberg; Christian (Uppsala, SE)

Assignee:

International Classification:

Expiration Date: 10/32013