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1. WO2014118796 - AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM

Publication Number WO/2014/118796
Publication Date 07.08.2014
International Application No. PCT/IN2013/000312
International Filing Date 13.05.2013
IPC
C07D 215/18 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with 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
18Halogen atoms or nitro radicals
A61K 31/47 2006.1
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
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
A61P 11/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
CPC
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
C07D 215/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with 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
18Halogen atoms or nitro radicals
Applicants
  • MELODY HEALTHCARE PVT. LTD. [IN]/[IN]
Inventors
  • PATEL, Dayabhai Somabhai
  • GHOGARE, Anil Balkrishna
  • VISHE, Kishor Tukaram
Agents
  • P. ARUNA SREE
Priority Data
281/MUM/201331.01.2013IN
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM
(FR) PROCÉDÉ IN SITU POUR LA PRÉPARATION DE MONTÉLUKAST SODIQUE HAUTEMENT PUR
Abstract
(EN) The present invention disclosed herein is a cost effective, in-situ process for the preparation of montelukast or its pharmaceutically acceptable salts of formula (1) by reacting optically pure (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methyl ethyl) phenyl]-propan-I-ol with methane sulfonyl chloride to afford mesylate derivative of formula (2) substantially free of impurities; followed by insitu condensing the same with disodium salt of mercapto-cyclopropyl acetic acid of formula (3) to afford montelukast free acid in good yield and purity, then converting the montelukast free acid into its substituted amine salt of formula (4). Further the montelukast substituted amine is converted into its pharmaceutically acceptable salt.
(FR) La présente invention décrite ici est un procédé in situ, rentable pour la préparation de montélukast ou de ses sels pharmaceutiquement acceptables de formule (1) par réaction de (S)-1-{3-[2-(7-chloroquinolin-2-yl)éthylène]-phényl}-3-[2-(1-hydroxy-1-méthyl éthyl) phényl]-propan-1-ol optiquement pur avec du chlorure de méthane sulfonyle pour fournir un dérivé mésylate de formule (2) sensiblement exempt d'impuretés ; suivie par la condensation in situ de celui-ci avec un sel disodique d'acide mercapto-cyclopropyl acétique de formule (3) pour fournir l'acide libre de montélukast dans un bon rendement et une bonne pureté, puis la conversion de l'acide libre de montélukast en son sel d'amine substituée de formule (4). De plus l'amine substituée de montélukast est convertie en son sel pharmaceutiquement acceptable.
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