Patent ID: 8703996
Filing Date: 2014-04-22
Classification: A61P,C07B,C07C

Abstract:
1. A process of preparing fesoterodine or a salt thereof, comprising the steps of: (a) reacting N,N-diisopropyl-3-phenylprop-2-en-1-amine with hydroxyphenylglycine or a derivative thereof denoted by formula A′ in which * denotes chiral C atom, R is hydrogen, C (b) optionally removing R and Y, if other than H (c) followed by oxidative decarboxylation in the presence of an oxidizing reagent to obtain 3-(5-formyl-2-hydroxyphenyl)-N,N-diisopropyl-3-phenylpropylamine; (d) reducing the formed 3-(5-formyl-2-hydroxyphenyl)-N,N-diisopropyl-3-phenylpropylamine to obtain hydroxytolterodine (HT); and (e) carrying out acylation of the phenolic hydroxy group HT or of (R)-HT obtained in step (d) by isobutyryl chloride or isobutyric anhydride to obtain fesoterodine, (f) optionally converting fesoterodine into a salt thereof; or wherein steps (d)-(e) are replaced by the steps of: (d′) carrying out acylation of the phenolic hydroxy group of 3-(5-formyl-2-hydroxyphenyl)-N,N-diisopropyl-3-phenylpropylamine obtained in step (c) by isobutyryl chloride or isobutyric anhydride, (e′) followed by selective reduction of formyl group; wherein optionally any of the compounds of the steps (d)-(e) or (d′)-(e′) are separated into enantiomers.