Dipharma S.p.a.

Dipharma Francis S.r.l.

Roberto Rossi

Pietro Allegrini

Gabriele Razzetti

Simone Mantegazza

Graziano Castaldi

Marcello Rasparini

Lino Colombo

Gianpiero Ventimigla

A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers,  

Process for the preparation of pyridine compounds

A novel process for the preparation of tolterodine, i.e. (R)&#x2014;N, N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine, in the racemic form, as well as intermediates useful for its preparation.

Process for the preparation of tolterodine

A novel process prepares tolterodine, i.e. (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine, in the racemic form, as well as intermediates useful for its preparation. Tolterodine free base may be prepared by reacting diisopropyl-(3-phenyl-3-p-tolyloxy-propyl)-amine and 60% aqueous sulfuric acid for three hours under stirring at room temperature. The reaction mixture is then poured over ice/water and then alkalized with 50% NaOH.

A process for the preparation of 6-methyl-4-(R)-phenyl-chroman-2-one and 6-methyl-4-(S)-phenyl-chroman-2-one, intermediates for the synthesis of tolterodine and its (S) enantiomer, by reaction of 6-methyl-coumarin with phenylboronic acids, esters and derivatives thereof, in the presence of chiral catalysts.

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Pavia, Italy

Roberto Rossi