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1. (WO2016016769) A PROCESS FOR THE PREPARATION OF PALBOCICLIB
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2016/016769 International Application No.: PCT/IB2015/055528
Publication Date: 04.02.2016 International Filing Date: 21.07.2015
IPC:
C07D 471/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants:
SUN PHARMACEUTICAL INDUSTRIES LIMITED [IN/IN]; Sun House, Plot No. 201 B/1 Western Express Highway Goregaon (E) Mumbai, Maharashtra 400 063, IN
Inventors:
TYAGI, Vipin; IN
MOHAMMAD, Kallimulla; IN
RAI, Bishwa Prakash; IN
PRASAD, Mohan; IN
Priority Data:
2154/DEL/201431.07.2014IN
Title (EN) A PROCESS FOR THE PREPARATION OF PALBOCICLIB
(FR) PROCÉDÉ DE PRÉPARATION DE PALBOCICLIB
Abstract:
(EN) The present invention relates to a process for the preparation of palbociclib utilizing a silyl-protected crotonic acid derivative to produce a silyl-protected 2-chloro-4-(cyclopentylamino)-5-(1-methyl-2-carboxy-ethen-1-yl)pyrmidine followed by intramolecular cyclization of the pyrmidine intermediate to produce 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one which is then converted to palbociclib.
(FR) La présente invention concerne un procédé de préparation de palbociclib à l'aide d'un dérivé d'acide crotonique silyl-protégé pour produire une 5-(1-méthyl-3 carboxy-prop-1-én-1-yl)-2-chloro-pipérazine silyl-protégée suivie par une cyclisation intramoléculaire du composé, intermédiaire de pipérazine, pour produire de la 2-chloro-8-cyclopentyl-5-méthyl-8 H-pyrido [2,3-d] pyrimidin-7-one qui est ensuite convertie en palbociclib.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, 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, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP3174878US20170217962IN201717006454