Method of producing N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)- 3-phenylpropylamine in its racemic or optically active form

摘要

In the present invention, there is disclosed a process for preparing N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropyl amine (tolterodine) in racemic or optically active form thereof wherein the preparation process comprises synthesis of enantiomerically enriched compounds of (R)- and (S)-3,4-dihydro-6-methyl-4-phenyl-2H-benzopyran-2-onone of the general formulae II-R and II-S and preparation of 3-(2-hydroxy-5-methylphenyl)-3-phenylpropanol of the general formula VIII in racemic or enantiomerically enriched form, protected on both oxygen atoms with a sulfa ester group. Further claimed are compounds of the general formulae VII and IX, in which X represents a protecting group being selected from the group consisting of toluene sulfonyl, methane sulfonyl and camphor sulfonyl, as well as optically active forms thereof.