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1. (WO2007004237) A PROCESS FOR THE PREPARATION OF MONTELUKAST
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/004237 International Application No.: PCT/IN2006/000226
Publication Date: 11.01.2007 International Filing Date: 30.06.2006
IPC:
C07D 215/18 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having 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
16
with 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
18
Halogen atoms or nitro radicals
Applicants:
MATRIX LABORATORIES LTD; 1-1-151/1, IV Floor Sairam Towers, Alexander Road Secunderabad 500 003, IN (AllExceptUS)
CHAVA, Satyanarayana [IN/IN]; IN (UsOnly)
GORANTLA, Seeta, Ramanjaneyulu [IN/IN]; IN (UsOnly)
INDUKURI, Venkata, Sunil, Kumar [IN/IN]; IN (UsOnly)
Inventors:
CHAVA, Satyanarayana; IN
GORANTLA, Seeta, Ramanjaneyulu; IN
INDUKURI, Venkata, Sunil, Kumar; IN
Agent:
RAO, Ramana, V.; Matrix Laboratories Ltd Plot No. 38, Phase-IV IDA, Jeedimetla Hyderabad 500 055, IN
Priority Data:
872/CHE/200505.07.2005IN
Title (EN) A PROCESS FOR THE PREPARATION OF MONTELUKAST
(FR) PROCEDE DE PREPARATION DE MONTELUKAST
Abstract:
(EN) The present invention relates to a process for the preparation of Montelukast or a salt thereof comprises, i) condensing Methyl -2-[3-[3-(2-(7 - chloroquinolin -2-yl) ethenyl] phenyl] -3 -chloro propyljbenzoate obtained above with l-(mercaptomethyl) cyclopropane acetic acid in presence of alkali carbonates such as Cesium Carbonate, followed by salification with organic amine ii) neutralizing the organic amine salt as obtained above with organic/inorganic acid followed by reaction with methylmagnesium chloride in the presence of Cerium Chloride followed by treatment with organic base yields montelukast amine salt iii) converting the montelukast amine salt to Montelukast Free acid iv) saltification of Montelukast free acid with Sodium hydroxide affords Montelukast Sodium.
(FR) L'invention concerne un procédé permettant de préparer du montelukast ou un sel de celui-ci, qui consiste i) à condenser méthyl 2[3-[3-(2-(7 - chloroquinoline -2-yl) éthényl] phényl]-3 -chloro propyl]benzoate obtenu avec de l'acide 1-(mercaptométhyl) cyclopropane acétique en présence de carbonates alcalins tels que le carbonate de césium, et salifier avec une amine organique, ii) à neutraliser le sel d'amine organique obtenu avec un acide organique/inorganique et faire réagir avec du chlorure de méthylmagnésium en présence du chlorure de cérium et traiter avec une base organique pour produire un sel d'amine de montelukast, iii) à convertir le sel d'amine de montelukast en acide libre de montelukast, iv) à salifier l'acide libre de montelukast avec de l'hydroxyde de sodium pour obtenir du sodium de montelukast.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP1940793US20100168432