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1. WO2009074478 - PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE

Publication Number WO/2009/074478
Publication Date 18.06.2009
International Application No. PCT/EP2008/066559
International Filing Date 01.12.2008
IPC
C07C 231/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
12by reactions not involving the formation of carboxamide groups
C07C 251/24 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
251Compounds containing nitrogen atoms doubly- bound to a carbon skeleton
02containing imino groups
24having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
C07C 237/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
04the carbon skeleton being acyclic and saturated
08having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
A61K 31/165 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
165having aromatic rings, e.g. colchicine, atenolol, progabide
A61P 25/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
CPC
A61K 31/165
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
165having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/197
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
A61K 31/198
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA],
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Applicants
  • NEWRON PHARMACEUTICALS S.P.A. [IT]/[IT] (AllExceptUS)
  • BARBANTI, Elena [IT]/[IT] (UsOnly)
  • FARAVELLI, Laura [IT]/[IT] (UsOnly)
  • SALVATI, PATRICIA [IT]/[IT] (UsOnly)
  • CANEVOTTI, Renato [IT]/[IT] (UsOnly)
  • PONZINI, Francesco [IT]/[IT] (UsOnly)
Inventors
  • BARBANTI, Elena
  • FARAVELLI, Laura
  • SALVATI, PATRICIA
  • CANEVOTTI, Renato
  • PONZINI, Francesco
Agents
  • SGARBI, Renato
Priority Data
07023937.111.12.2007EP
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE
(FR) PROCÉDÉ DE PRODUCTION DE 2-[4-(3- OU 2-FLUOROBENZYLOXY)BENZYLAMINO] PROPANAMIDES D'UN DEGRÉ DE PURETÉ ÉLEVÉ
Abstract
(EN) A process for obtaining therapeutically active 2-[4-(3- and 2-(flurobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2- [4 -(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C1-C5 lower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.
(FR) L'invention concerne un procédé d'obtention de 2-[4-(3- ou 2-fluorobenzyloxy)benzylamino]propanamides thérapeutiquement actifs et de leurs sels avec des acides pharmaceutiquement acceptables avec un degré de pureté élevé, notamment avec une teneur en impuretés dérivées de dibenzyle inférieure à 0,03 %, de préférence inférieure à 0,01 % en poids. Le procédé est réalisé en soumettant les bases de Schiff intermédiaires 2-[4-(3- et 2-fluorobenzyloxy)benzylidèneamino]propanamides à une réaction de réduction avec un réducteur choisi parmi le borohydrure de sodium et le borohydrure de potassium dans une quantité appropriée d'un solvant organique choisi parmi les alcanols inférieurs en C1 à C5, en autorisant la formation et la présence pendant une partie importante de la réaction de réduction d'une suspension de la base de Schiff dans la solution saturée de la base de Schiff dans le même solvant organique.
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