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1. WO2016005874 - PROCESS FOR THE PREPARATION OF REGORAFENIB AND ITS CRYSTALLINE FORMS

Publication Number WO/2016/005874
Publication Date 14.01.2016
International Application No. PCT/IB2015/055083
International Filing Date 06.07.2015
IPC
C07D 213/81 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81Amides; Imides
CPC
C07D 213/81
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
81Amides; Imides
Applicants
  • SHILPA MEDICARE LIMITED [IN]/[IN]
Inventors
  • RAMPALLI, Sriram
  • UPALLA, Lav Kumar
  • RAMACHANDRULA, Krishna Kumar
  • PUROHIT, Prashant
  • AKSHAY KANT, Chaturvedi
Priority Data
3391/CHE/201409.07.2014IN
3396/CHE/201409.07.2014IN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF REGORAFENIB AND ITS CRYSTALLINE FORMS
(FR) PROCÉDÉ POUR LA PRÉPARATION DU RÉGORAFÉNIB ET SES FORMES CRISTALLINES
Abstract
(EN)
The present invention relates to a process for the preparation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide or Regorafenib (I): Formula (I). The present invention further relates to a process for the purification of 4-[4-({[4-chloro-3-(trifluoromethyl) phenyl] carbamoyl} amino)-3-fluorophenoxy]-N-methylpyridine-2- carboxamide or Regorafenib (I) to provide highly pure material. The present invention further relates to a process for the preparation stable crystalline material of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]- N-methyl pyridine-2-carboxamide or Regorafenib (I) useful in the preparation of pharmaceutical compositions for the treatment of cancer.
(FR)
La présente invention concerne un procédé pour la préparation de 4-[4-({[4-chloro-3- (trifluorométhyle)phényl]carbamoyl}amino)-3-fluorophénoxy]-N-méthylpyridine -2-carboxamide ou du régorafénib (I) : Formule (I). La présente invention concerne en outre un procédé pour la purification de 4-[4-({ [4-chloro-3-(trifluorométhyle)phényl]carbamoyl}amino)-3-fluorophénoxy]-N-méthylpyridine-2-carboxamide ou du régorafénib (I) pour fournir un matériau hautement pur. La présente invention concerne en outre un procédé pour la préparation d'un matériau cristallin stable de 4-[4-({[4-chloro-3-(trifluorométhyl)phényl]carbamoyl}amino) -3-fluorophénoxy]-N-méthylpyridine-2-carboxamide ou de régorafénib (I) utiles dans la préparation de compositions pharmaceutiques pour le traitement du cancer.
Also published as
Latest bibliographic data on file with the International Bureau