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1. (WO2016088094) PROCESS FOR THE PREPARATION OF BARICITINIB AND AN INTERMEDIATE THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2016/088094    International Application No.:    PCT/IB2015/059364
Publication Date: 09.06.2016 International Filing Date: 04.12.2015
IPC:
C07D 487/04 (2006.01)
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: AZAD, Md Abul Kalam; (IN).
PANDEY, Gyanendra; (IN).
SINGH, Kaptan; (IN).
PRASAD, Mohan; (IN)
Priority Data:
3554/DEL/2014 05.12.2014 IN
Title (EN) PROCESS FOR THE PREPARATION OF BARICITINIB AND AN INTERMEDIATE THEREOF
(FR) PROCÉDÉ DE SYNTHÈSE DE BARICITINIB ET D’UN INTERMÉDIAIRE DE CELUI-CI
Abstract: front page image
(EN)The present invention provides a process for the preparation of baricitinib and an intermediate thereof. The present invention provides a convenient, economical, and industrially advantageous two-step process for the preparation of [4-(IH-pyrazol-4-yl)-7Hpyrrolo[2,3-d] pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention involves the use of an alkali or alkaline earth metal hydroxide, carbonate, or bicarbonate as a base for reacting 4-chloro-7H-pyrrolo[2,3-d]pyrimidine of Formula (III) with chloromethyl pivalate of Formula (IV), and the use of an unprotected pyrazole borolane of Formula (VIII) for the conversion of (4-chloro-7H-pyrrolo[2,3-d] pynmidin-7- yl)methyl 2,2-dimethylpropanoate of Formula V into [4-(1 H-pyrazol-4-yl)-7Hpyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention provides [4-(1 H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (I) in high yield.
(FR)La présente invention concerne un procédé de synthèse du baricitinib et d'un intermédiaire de celui-ci. La présente invention concerne un procédé en deux étapes pratique, économique et industriellement avantageux pour la synthèse de pivalate de [4-(1H-pyrazol-4-yl) -7H-pyrrolo-[2,3-d]-pyrimidin-7-yl]méthyle de Formule (II). Le procédé selon la présente invention implique l'utilisation d'un hydroxyde, carbonate ou bicarbonate de métal alcalin ou alcalino-terreux en tant que base pour la réaction de la 4-chloro-7H-pyrrolo[2,3-d]pyrimidine de Formule (III) avec le pivalate de chlorométhyle de Formule (IV), et l'utilisation d’un pyrazole borolane non protégé de Formule (VIII) pour la conversion du 2,2-diméthylpropanoate de (4-chloro-7H-pyrrolo[2,3-d]pyrimidin-7-yl) méthyle de Formule V en pivalate de [4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]méthyle de Formule (II). Le procédé selon la présente invention concerne le pivalate de [4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]méthyle de Formule (I) avec un rendement élevé.
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 (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)