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1. WO2012143937 - PROCESS FOR PREPARATION OF RILPIVIRINE INTERMEDIATE

Publication Number WO/2012/143937
Publication Date 26.10.2012
International Application No. PCT/IN2012/000246
International Filing Date 09.04.2012
IPC
C07C 255/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
01having cyano groups bound to acyclic carbon atoms
32having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
34with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
C07C 253/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
253Preparation of carboxylic acid nitriles
30by reactions not involving the formation of cyano groups
C07D 239/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
CPC
A61P 31/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07C 253/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
253Preparation of carboxylic acid nitriles
04by reaction of cyanogen halides, e.g. ClCN, with organic compounds
C07C 253/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
253Preparation of carboxylic acid nitriles
30by reactions not involving the formation of cyano groups
C07C 269/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
269Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
06by reactions not involving the formation of carbamate groups
C07D 239/48
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46Two or more oxygen, sulfur or nitrogen atoms
48Two nitrogen atoms
Applicants
  • EMCURE PHARMACEUTICALS LIMITED [IN]/[IN]
  • GURJAR, Mukund Keshav [IN]/[IN] (UsOnly)
  • MAIKAP, Golakchandra, Sudarshan [IN]/[IN] (UsOnly)
  • JOSHI, Shashikant, Gangaram [IN]/[IN] (UsOnly)
  • BADHE, Sachin, Aravind [IN]/[IN] (UsOnly)
  • MEHTA Samit, Satish [IN]/[IN] (UsOnly)
Inventors
  • GURJAR, Mukund Keshav
  • MAIKAP, Golakchandra, Sudarshan
  • JOSHI, Shashikant, Gangaram
  • BADHE, Sachin, Aravind
  • MEHTA Samit, Satish
Agents
  • BHAT, Sunil
Priority Data
1223/MUM/201115.04.2011IN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR PREPARATION OF RILPIVIRINE INTERMEDIATE
(FR) PROCÉDÉ PERFECTIONNÉ DE PRÉPARATION DE RILPIVIRINE
Abstract
(EN)
Disclosed is process for the preparation of a key Rilpivirine intermediate namely, (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-amino-l-carboxybenzyl phenylamine (VI) with acrylonitrile in presence of palladium acetate, followed by treatment with an acid and its subsequent conversion to the hydrochloride salt (II), wherein the undesired Z isomer is less than 0.5% and provides Rilpivirine hydrochloride having Z isomer less than 0.1%.
(FR)
La présente invention porte sur la préparation d'un intermédiaire clé pour la Rilpivirine, à savoir le chlorhydrate de (E)-4-(2-cyanoéthényl)-2,6-diméthylphénylamine (II) par un procédé comprenant la réaction du sel tétrafluoroborate de l'ion diazonium de la 2,6-diméthyl-4-amino-1-carboxybenzylphénylamine (VI) avec de l'acrylonitrile en présence d'acétate de palladium, suivie du traitement avec un acide et de sa conversion subséquente en sel de type chlorhydrate (II), l'isomère Z non souhaité étant présent à hauteur de moins de 0,5 %, la préparation produisant du chlorhydrate de Rilpivirine ayant une teneur en isomère Z inférieure à 0,1 %.
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