Abstract: 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.
Type:
Grant
Filed:
February 21, 2006
Date of Patent:
February 26, 2008
Assignee:
Dipharma S.p.A.
Inventors:
Gabriele Razzetti, Simone Mantegazza, Roberto Rossi, Pietro Allegrini
Abstract: A process for the preparation of clopidogrel (1) by reaction of the N,N?-bis-4,5,6,7-tetrahydro-[3,2-c]-thienopyridyl methane (12) with (R)-2-chlorophenylacetic acid derivatives of formula (13) in which X and R have the meanings as indicated in the disclosure.
Type:
Grant
Filed:
April 22, 2003
Date of Patent:
February 12, 2008
Assignee:
Dipharma S.p.A.
Inventors:
Graziano Castaldi, Giuseppe Barreca, Alberto Bologna
Abstract: A process for the preparation of benzo[d]isoxazol-3-yl-methanesulfonic acid of formula (I), or a salt thereof, and the intermediates thereof, useful as an intermediate in the preparation of zonisamide.
Abstract: A process for the preparation of terbinafine, comprising the reaction of a compound of formula (II), or a salt thereof, wherein X is a leaving group, with tert-butylacetylene, in the presence of a platinum catalyst
Type:
Grant
Filed:
November 21, 2003
Date of Patent:
October 30, 2007
Assignee:
Dipharma S.p.A.
Inventors:
Antonio Tarquini, Graziano Castaldi, Gianluca Galdi, Pietro Allegrini
Abstract: New crystalline form of ziprasidone hydrochloride hemihydrate, process for its preparation, its use for the purification of ziprasidone, its pharmaceutical compositions and their use in therapy.
Abstract: A process for the preparation of compounds of formula (III), intermediates useful for the synthesis of cilostazol, which process comprises reacting haloimine of formula (V) wherein X is halogen, with trimethylsilyl azide.
Abstract: A process for the preparation of benzylimidazole derivatives useful as intermediates for preparation of losartan, novel intermediates for their preparation and a process for the preparation of losartan.
Type:
Grant
Filed:
October 21, 2004
Date of Patent:
January 16, 2007
Assignee:
Dipharma S.p.A.
Inventors:
Pietro Allegrini, Gabriele Razzetti, Graziano Castaldi, Vittorio Lucchini
Abstract: 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.
Type:
Grant
Filed:
March 29, 2005
Date of Patent:
October 10, 2006
Assignee:
Dipharma S.p.A.
Inventors:
Lino Colombo, Roberto Rossi, Pietro Allegrini, Graziano Castaldi
Abstract: A novel process for the preparation of 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.
Type:
Application
Filed:
February 21, 2006
Publication date:
August 24, 2006
Applicant:
DIPHARMA S.P.A.
Inventors:
Gabriele Razzetti, Simone Mantegazza, Roberto Rossi, Pietro Allegrini
Abstract: A process for the preparation of pantoprazole and the salts thereof, comprising the reaction of a mercaptoimidazole with a picoline, to give a 2-pyridinyl-methylsulfinyl-2-benzimidazole intermediate, the oxidation thereof with ?-phthalimidoperhexanoic acid and the subsequent methoxylation.
Type:
Grant
Filed:
September 22, 2004
Date of Patent:
July 25, 2006
Assignee:
Dipharma S.p.A.
Inventors:
Caterina Napoletano, Eleonora Porta, Pietro Allegrini, Graziano Castaldi