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1. WO2016071303 - PROCESS FOR THE PREPARATION OF (1S,2R)-MILNACIPRAN

Publication Number WO/2016/071303
Publication Date 12.05.2016
International Application No. PCT/EP2015/075513
International Filing Date 03.11.2015
IPC
C07C 231/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
C07C 233/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
CPC
C07B 2200/07
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
07Optical isomers
C07C 231/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
02from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
12by reactions not involving the formation of carboxamide groups
C07C 231/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
16Preparation of optical isomers
18by stereospecific synthesis
C07C 2601/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2601Systems containing only non-condensed rings
02with a three-membered ring
Applicants
  • QUIMICA SINTETICA, S.A. [ES]/[ES]
Inventors
  • BARRECA, Giuseppe
  • ROMANO', Bruno Gaetano
Agents
  • PALLADINO, Massimo
  • GERVASI, Gemma
  • PALLINI, Diego
  • CINQUANTINI, Bruno
  • APPOLONI, Romano
  • CATTANEO, Elisabetta
  • VALENZA, Silvia
  • ZACCARO, Elisabetta
  • LUALDI, Lorenzo
  • BRIGHENTI, Livio
  • LORENZI, Silvana
  • COPPO, Alessandro
  • CELONA, Antonio
  • DE BORTOLI, Tiziano
  • GIRLANDO, Mario
  • SAVI, Massimiliano
Priority Data
MI2014A00188304.11.2014IT
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF (1S,2R)-MILNACIPRAN
(FR) PROCÉDÉ POUR LA PRÉPARATION DE (1S,2R)-MILNACIPRAN
Abstract
(EN)
The invention relates to a process for the preparation of Levomilnacipran, a compound useful in the treatment of depression, comprising the following steps: a) directly converting the enantiomerically enriched form of alcohol (D) into the enantiomerically enriched form of the phthalimido derivative (C) by treatment with phthalimide in the presence of a trialkyl or triarylphosphine and of a dialkyl azodicarboxylate, formula (I) wherein the amount of phthalimide is comprised between 1 and 1.3 equivalents with respect to the molar amount of alcohol (D) used, and the amounts of both the phosphine and the azodicarboxylate are comprised, independently from each other, between 1 and 1.5 equivalents with respect to the molar amount of alcohol (D) used; b) deblocking the enantiomerically enriched form of the phthalimido derivative (C) to obtain Levomilnacipran, formula (II).
(FR)
L'invention concerne un procédé pour la préparation de lévomilnacipran, un composé utile dans le traitement de la dépression, ledit procédé comprenant les étapes suivantes : a) la conversion directe de la forme énantiomériquement enrichie de l'alcool (D) en la forme énantiomériquement enrichie du dérivé phtalimido (C) par traitement avec du phtalimide en présence d'un trialkyle ou d'une triarylphosphine et d'un azodicarboxylate de dialkyle, de formule (I), la quantité de phtalimide étant comprise entre 1 et 1,3 équivalent par rapport à la quantité molaire d'alcool (D) utilisé, et les quantités à la fois de la phosphine et de l'azodicarboxylate étant comprises, indépendamment l'une de l'autre, entre 1 et 1,5 équivalent par rapport à la quantité molaire d'alcool (D) utilisé ; b) le déblocage de la forme énantiomériquement enrichie du dérivé phtalimido (C) pour obtenir le lévomilnacipran, formule (II).
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