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1. (WO2013050873) PROCESS FOR THE PREPARATION OF LERSIVIRINE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2013/050873    International Application No.:    PCT/IB2012/002449
Publication Date: 11.04.2013 International Filing Date: 04.10.2012
IPC:
C07D 231/18 (2006.01)
Applicants: PHIVCO UK LIMITED [GB/GB]; 980 Great West Road Brentford, Middlesex TW8 9GS (GB).
CODINA, Anna [ES/GB]; (GB).
DERRICK, Andrew [GB/GB]; (GB).
JOYCE, Richard [GB/GB]; (GB).
SUSANNE, Flavien [FR/GB]; (GB)
Inventors: CODINA, Anna; (GB).
DERRICK, Andrew; (GB).
JOYCE, Richard; (GB).
SUSANNE, Flavien; (GB)
Priority Data:
61/544,393 07.10.2011 US
Title (EN) PROCESS FOR THE PREPARATION OF LERSIVIRINE
(FR) PROCÉDÉ DE PRÉPARATION DE LERSIVIRINE
Abstract: front page image
(EN)The present invention relates to a process for the preparation of lersivirine or a pharmaceutically acceptable salt thereof comprising: (a) reacting 5-(2-oxo-1-propanoylbutoxy)isophthalonitrile and 2- hydrazinoethanol, in the presence of an acid, to form 5-{[3,5-diethyl-1 -(2- hydroxyethyl)-1 H-pyrazol-4-yl]oxy}isophthalonitrile, and optionally, (b) reacting 5-{[3,5-diethyl-1-(2-hydroxyethyl)-1 H-pyrazol-4- yl]oxy}isophthalonitrile with a suitable reagent so as to form a pharmaceutically acceptable salt of 5-{[3,5-diethyl-1-(2-hydroxyethyl)-1 H- pyrazol-4-yl]oxy}isophthalonitrile, characterised in that step (a) comprises a first stage wherein the reaction is controlled so as to maintain a reaction temperature between 15-30 °C and a second stage wherein the reaction is controlled so as to maintain a reaction temperature between 40-70 °C.
(FR)Cette invention concerne un procédé de préparation de lersivirine ou d'un sel pharmaceutiquement acceptable de celle-ci, ledit procédé comprenant : (a) la réaction d'un 5-(2-oxo-1-propanoylbutoxy)isophtalonitrile et d'un 2- hydrazino-éthanol, en présence d'un acide, pour former un 5-{[3,5-diéthyl- 1-(2-hydroxyéthyl)-1H-pyrazol-4-yl]oxy}isophtalonitrile, et éventuellement, (b) la réaction du 5-{[3,5-diéthyl-1-(2-hydroxyéthyl)- 1H-pyrazol-4-yl]oxy}isophtalonitrile avec un réactif convenable pour former un sel pharmaceutiquement acceptable de 5-{[3,5-diéthyl- 1-(2-hydroxyéthyl)-1H-pyrazol-4-yl]oxy}isophtalonitrile. Le procédé selon l'invention est caractérisé en ce que l'étape (a) comprend un premier stade qui consiste à contrôler la réaction pour maintenir la température réactionnelle entre 15 et 30°C et un second stade qui consiste à contrôler la réaction pour maintenir la température réactionnelle entre 40 et 70°C.
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, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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, 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, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)