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 compounds of formula (I): HO-A-ONO2??(I) wherein A is a C2-C6 alkylene chain, the compounds of formula (I) being synthesized by nitration of the corresponding alkanediols with “stabilized” nitric acid is herein disclosed. The process is safer to operators and allows to obtain advantageous yields on an industrial scale.
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 ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.
Type:
Application
Filed:
November 13, 2006
Publication date:
May 24, 2007
Applicants:
DIPHARMA S. P. A., LUNDBECK PHARMACEUTICALS ITALY S. P. A.
Inventors:
Jacopo Zanon, Oscar Martini, Francesco Ciardella, Luca Gregori, Federico Sbrogio, Andrea Castellin
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