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1. WO2011004391 - AN IMPROVED PROCESS FOR THE PREPARATION OF ELETRIPTAN AND ITS SALT THEREOF

Publication Number WO/2011/004391
Publication Date 13.01.2011
International Application No. PCT/IN2010/000432
International Filing Date 24.06.2010
IPC
C07D 403/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/404 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
CPC
C07D 403/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • MATRIX LABORATORIES LTD [IN]/[NA] (AllExceptUS)
  • KARUSALA, Nageswara Rao (UsOnly)
  • CHAVHAN, Bhausaheb (UsOnly)
  • SIGAMSETTY, Radha Krishna (UsOnly)
  • KOTHAKONDA, Sudarshan Rao (UsOnly)
  • CHANDUPATLA, Siva Kumar (UsOnly)
  • DATTA, Debashish (UsOnly)
Inventors
  • KARUSALA, Nageswara Rao
  • CHAVHAN, Bhausaheb
  • SIGAMSETTY, Radha Krishna
  • KOTHAKONDA, Sudarshan Rao
  • CHANDUPATLA, Siva Kumar
  • DATTA, Debashish
Agents
  • NARAHARI, Babu Ambati
Priority Data
1487/CHE/200925.06.2009IN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) AN IMPROVED PROCESS FOR THE PREPARATION OF ELETRIPTAN AND ITS SALT THEREOF
(FR) PROCÉDÉ AMÉLIORÉ D'ÉLABORATION D'ÉLÉTRIPTANE ET SON SEL CORRESPONDANT
Abstract
(EN)
The present invention relates to an improved process for the preparation of Eletriptan hydrobromide by hydrolyzing (R)-1-acetyl-5-(2-phenylsulphonylethenyl)-3-(N- methylpyrrolidin-2-ylmethyl)-1 H-indole, followed by reduction in the presence of a metal catalyst, methanesulphonicacid in a solvent, to get the Eletriptan methanesulphonate. Setting free of the methanesulphonate salt with a base and the compound is extracted into an organic solvent, optionally passed the organic layer through silica gel column, the solvent is evaporated to get residue. The residue is dissolved in another solvent followed by addition of aqueous hydrobromic acid to get Eletriptan hydrobromide.
(FR)
L'invention concerne un procédé amélioré d'élaboration d'hydrobromure d'élétriptane par hydrolyse de (R)-1-acétyl-5-(2-phénylsulphonyléthényl)-3-(N- méthylpyrrolidin-2-ylméthyl)-1 H-indole, puis par réduction en présence d'un catalyseur métallique, de l'acide méthane sulfonique dans un solvant, pour l'élaboration de méthane sulfonate d'élétriptane. On libère le sel de méthane sulfonate avec une base et le composé est extrait sous forme de solvant organique, éventuellement en traversant la couche organique à travers une colonne de gel de silice, et le solvant est soumis à évaporation pour la formation d'un résidu. Le résidu est dissous dans un autre solvant puis on ajoute de l'acide hydrobromique aqueux pour obtenir de l'hydrobromure d'élétriptane.
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