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1. IN281/MUM/2013 - "AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM."

Office
India
Application Number 281/MUM/2013
Application Date 31.01.2013
Publication Number 281/MUM/2013
Publication Date 14.11.2014
Grant Number 321661
Grant Date 27.09.2019
Publication Kind B
IPC
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
C07D 215/16
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
C07D 215/38
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
38Nitrogen atoms
A61
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
Applicants MELODY HEALTHCARE PVT. LTD.
Inventors PATEL, DAYABHAI SOMABHAI
GHOGARE, ANIL BALKRISHNA
VISHE, KISHOR TUKARAM
Title
(EN) "AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM."
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 (I) by reacting optically pure (S)-l-{3-[2-(7-chloroquinolin-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1 -methyl ethyl) phenyl]-propan-l-ol with methane sulfonyl chloride to afford mesylate derivative of formula (2) substantially free of impurities; followed by 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.
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