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1. WO2011004242 - AN IMPROVED PROCESS FOR THE PREPARATION OF DUTASTERIDE

Publication Number WO/2011/004242
Publication Date 13.01.2011
International Application No. PCT/IB2010/001661
International Filing Date 07.07.2010
IPC
C07J 73/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
73Steroids in which the cyclopentahydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
CPC
C07J 73/005
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
73Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
001by one hetero atom
005by nitrogen as hetero atom
Applicants
  • AUROBINDO PHARMA LIMITED [IN]/[IN] (AllExceptUS)
  • MALLELA, Sambhu, Prasad, Sarma [IN]/[IN] (UsOnly)
  • NANDI, Sukumar [IN]/[IN] (UsOnly)
  • GONA, Balanarasimha, Reddy [IN]/[IN] (UsOnly)
  • AKKINA, Naresh [IN]/[IN] (UsOnly)
  • ANANTA, Rani [IN]/[IN] (UsOnly)
  • AMINUL, Islam [IN]/[IN] (UsOnly)
  • MEENAKSHISUNDERAM, Sivakumaran [IN]/[IN] (UsOnly)
Inventors
  • MALLELA, Sambhu, Prasad, Sarma
  • NANDI, Sukumar
  • GONA, Balanarasimha, Reddy
  • AKKINA, Naresh
  • ANANTA, Rani
  • AMINUL, Islam
  • MEENAKSHISUNDERAM, Sivakumaran
Priority Data
1634/CHE/200909.07.2009IN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) AN IMPROVED PROCESS FOR THE PREPARATION OF DUTASTERIDE
(FR) PROCÉDÉ AMÉLIORÉ DE PRÉPARATION DU DUTASTÉRIDE
Abstract
(EN)
The present invention provides an improved process for the preparation of Dutasteride (I) which comprises: (i) reacting 4-aza-5α-androst-1-en-3-one-17β-carboxylic acid (VII), Formula VII, with sulfonic acid anhydride (RSO2)2O in presence of base to produce an intermediate compound of Formula (XIII), Formula XIII, wherein R represents C1-6 alkyl, C1-6 halo alkyl, C6-10 aryl, halo aryl; (ii) condensing compound of Formula (XIII) with 2,5-bis(trifluoromethyl)aniline (III), Formula (III), in the presence or absence of a base to produce Dutasteride (I).
(FR)
La présente invention concerne un procédé amélioré de préparation du dutastéride (I) qui consiste à : (i) faire réagir l'acide 4-aza-5α-androst-1-en-3-one-17β-carboxylique (VII), de formule VII, avec un anhydride d'acide sulfonique (RSO2)2O en présence d'une base pour produire un composé intermédiaire de formule (XIII), dans laquelle R représente un groupe alkyle en C1-6, halogénoalkyle en C1-6, aryle en C6-10, halogénoaryle; (ii) condenser le composé de formule (XIII) avec de la 2,5-bis(trifluorométhyl)aniline (III), de formule (III), en présence ou en l'absence d'une base pour produire le dutastéride (I).
Also published as
Latest bibliographic data on file with the International Bureau