Abstract: A process for the preparation of a compound of formula (I) is disclosed, which comprises: a) the reaction of a compound of formula (II) with zinc azide of formula (III) Zn(N3)2??(III) in the presence of a solvent of formula R1—OH, wherein R1 is herein defined, to obtain a compound of formula (IV), b) its conversion into a compound of formula (V); c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); and d) the hydrolysis thereof.
Type:
Grant
Filed:
April 29, 2010
Date of Patent:
November 22, 2011
Assignee:
Dipharma Francis S.r.l.
Inventors:
Gabriele Razzetti, Pietro Allegrini, Dario Pastorello
Abstract: Linezolid salts, useful as such and as intermediates in a process for the preparation of novel and known crystalline linezolid forms, in particular known as Form III.
Type:
Grant
Filed:
September 3, 2008
Date of Patent:
August 2, 2011
Assignee:
DiPharma Francis s.r.l.
Inventors:
Chiara Vladiskovic, Emanuele Attolino, Pietro Allegrini, Gabriele Razzetti
Abstract: Disclosed is a process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having a low content of impurities such as tolterodine and tolterodine isobutyrate.
Type:
Application
Filed:
December 20, 2010
Publication date:
June 23, 2011
Applicant:
DIPHARMA FRANCIS S.R.L.
Inventors:
Marco ARTICO, Emanuele ATTOLINO, Pietro ALLEGRI
Abstract: The present invention relates to a process for the preparation of (R)-(1-Naphthalen-1-yl-ethyl)-[3-(3-trifluoromethyl-phenyl)-propyl]-amine or a salt thereof, in particular the hydrochloride, and intermediates useful in its synthesis.
Type:
Application
Filed:
November 24, 2010
Publication date:
May 26, 2011
Applicant:
DIPHARMA FRANCIS s.r.l.
Inventors:
Pietro ALLEGRINI, Emanuele Attolino, Davide Rossi
Abstract: Disclosed is a crystalline form of rufinamide selected from: a substantially anhydrous and approximately monosolvated with trifluoroacetic acid crystalline form, hereinafter designated as Form ?, and a crystalline form, hereinafter designated as Form ?, characterised by an XRPD spectrum as shown in FIG. 3, wherein the most intense peaks fall at 4.5, 9.0, 13.5, 18.0, 18.8, 19.5, 20.6, 24.6, 25.7, 26.5, 27.4, 27.9, 28.7, 30.0 and 31.8±0.2° in 2?.
Type:
Application
Filed:
August 3, 2010
Publication date:
February 10, 2011
Applicant:
DIPHARMA FRANCIS S.R.L.
Inventors:
Gabriele RAZZETTI, Chiara VLADISKOVIC, Pietro ALLEGRINI
Abstract: Process for the preparation of crystalline anhydrous (R)-2-[[[3-methyl-4-(2,2,2-trifluoroetoxy)-2-piridyl]methyl]sulphinyl]benzimidazole (dexlansoprazole).
Abstract: A process for the preparation of 2(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]-7(8H)-pyrazinyl]-1-(2,4,5-trifluorophenyl)-2-butanamine and intermediates useful for the synthesis thereof.
Type:
Application
Filed:
March 19, 2010
Publication date:
December 30, 2010
Applicant:
DIPHARMA FRANCIS S.R.L.
Inventors:
Pietro ALLEGRINI, Emanuele ATTOLINO, Gianmaria DELL'ANNA, Mario MICHIELETTI
Abstract: Process for the preparation of intermediates useful in the synthesis of [1[S(R)],2?,4?]-4-cyclohexyl-1-[[[(2-methyl-1-oxypropoxy)propoxy](4-phenylbutyl)phosphinyl]acetyl]-L-proline, and the synthesis thereof, in particular as sodium salt.
Type:
Application
Filed:
May 24, 2010
Publication date:
November 25, 2010
Applicant:
DIPHARMA FRANCIS S.r.l.
Inventors:
Gabriele RAZZETTI, Sergio Riva, Pietro Allegrini, Mario Michieletti, Emanuele Attolino
Abstract: A process for the preparation of a compound of formula (I) is disclosed, which comprises: a) the reaction of a compound of formula (II) with zinc azide of formula (III) Zn(N3)2??(III) in the presence of a solvent of formula R1—OH, wherein R1 is herein defined, to obtain a compound of formula (IV), b) its conversion into a compound of formula (V); c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); and d) the hydrolysis thereof.
Type:
Application
Filed:
April 29, 2010
Publication date:
November 18, 2010
Applicant:
DIPHARMA FRANCIS S.r.l.
Inventors:
Gabriele RAZZETTI, Pietro Allegrini, Dario Pastorello
Abstract: A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ?CR8— or ?N—; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.
Type:
Grant
Filed:
October 29, 2007
Date of Patent:
September 7, 2010
Assignee:
Dipharma Francis S.R.L.
Inventors:
Pietro Allegrini, Marcello Rasparini, Gabriele Razzetti, Simone Mantegazza, Vittorio Lucchini, Alberto Bologna
Abstract: A process for the preparation of entacapone, in particular as the polymorphic form A, comprising the preparation of a compound of formula (V), wherein R is C1-C6 alkyl, by condensation of N,N-diethyl-cyano-acetamide with a compound of formula (IV), wherein R is C1-C6 alkyl, in the presence of a strong basic agent; the dealkylation of the compound of formula (V) to obtain entacapone, and the crystallization thereof from methyl ethyl ketone is performed to yield the polymorphic form A. The polymorphic form A of entacapone may be used to treat Parkinson's disease and/or to enhance effectiveness of muscle control.
Type:
Grant
Filed:
December 18, 2007
Date of Patent:
July 6, 2010
Assignee:
Dipharma Francis s.r.l.
Inventors:
Simone Mantegazza, Pietro Allegrini, Gabriele Razzetti
Abstract: A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R,S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; (the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.
Abstract: A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ?CR8— or ?N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and each R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.
Abstract: A process for the preparation of (1S,3?R)-quiniclidin-3?-yl-1-phenyl-3,4-dihydro-1H-isoquinolin-2-carboxylate, namely solifenacin, comprising the reaction of a compound of formula (IV) with a compound of formula (V), as herein defined, and the subsequent reaction with 3-quinuclidinol.
Type:
Application
Filed:
January 30, 2009
Publication date:
August 13, 2009
Applicant:
Dipharma Francis S.r.l.
Inventors:
Pietro Allegrini, Lino Colombo, Marco Brusasca, Chiara Vladiskovic, Gabriele Razzetti, Emanuele Attolino
Abstract: Ziprasidone base or a pharmaceutically acceptable salt thereof free from colored impurities, in particular those giving the product a “slightly pink to pink” coloration.
Type:
Grant
Filed:
March 7, 2006
Date of Patent:
July 21, 2009
Assignee:
Dipharma Francis S.r.l.
Inventors:
Gianpiero Ventimiglia, Pietro Allegrini, Gabriele Razzetti, Domenico Magrone, Alberto Bologna
Abstract: Novel crystalline hydrate form of (S)-1-phenylethylammonium (R)-diphenyl-methanesulphinyl-acetate and its use in a process for the preparation of (R)-benzhydrylsulphinylacetamide.
Type:
Application
Filed:
November 4, 2008
Publication date:
June 18, 2009
Applicant:
DIPHARMA FRANCIS S.R.L.
Inventors:
Giuseppe Barreca, Pietro Allegrini, Gabriele Razzetti