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1. (WO2009142522) PROCESS FOR PREPARATION OF SOLIFENACIN AND/OR THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF OF HIGH PHARMACEUTICAL PURITY
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/142522    International Application No.:    PCT/PL2009/000054
Publication Date: 26.11.2009 International Filing Date: 22.05.2009
IPC:
C07D 453/02 (2006.01)
Applicants: ZAKLADY FARMACEUTYCZNE POLPHARMA SA [PL/PL]; ul. Pelplinska 19 83-200 Starogard Gdanski (PL) (For All Designated States Except US).
ZEGROCKA-STENDEL, Oliwia [PL/PL]; (PL) (For US Only).
ZAGRODZKA, Joanna [PL/PL]; (PL) (For US Only).
LASZCZ, Marta [PL/PL]; (PL) (For US Only)
Inventors: ZEGROCKA-STENDEL, Oliwia; (PL).
ZAGRODZKA, Joanna; (PL).
LASZCZ, Marta; (PL)
Agent: KRZYWDZINSKA, Ewa; lnstytut Farmaceutyczny ul. Rydygiera 8 PL-01-793 Warszawa (PL)
Priority Data:
385265 23.05.2008 PL
Title (EN) PROCESS FOR PREPARATION OF SOLIFENACIN AND/OR THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF OF HIGH PHARMACEUTICAL PURITY
(FR) PROCEDE DE PREPARATION DE SOLIFENACINE ET/OU DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES DE HAUTE PURETE PHARMACEUTIQUE
Abstract: front page image
(EN)A process for the preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity is characterized in that 3-(R)-quinuclidinoloxy anion generated in situ from 3-(R)-quinuclidinol in a presence of strong base in polar organic solvent is subject to acylation with (S)-1 -phenyl-1,2,3, 4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98%, while maintaining constant anion excess in a reaction mixture, and after reaction completion solifenacin base is optionally transformed into solifenacin salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98% is obtained in a reaction of (S)-1-phenyl-1,2,3, 4- tetrahydroisoquinoline and molar excess of phosgene in a presence of tertiary aromatic amine in aromatic hydrocarbon, and isolated in a crystalline form.
(FR)L’invention concerne un procédé de préparation de solifénacine et/ou de ses sels pharmaceutiquement acceptables de haute pureté pharmaceutique. Ce procédé se caractérise en ce que : un anion 3-(R)-quinuclidinoloxy généré in situ à partir de 3-(R)-quinuclidinol en présence d’une base forte dans un solvant organique polaire, est soumis à une acylation avec du chlorure de (S)-1-phényl-1,2,3,4-tétrahydroisoquinolinecarbonyle d’une pureté chimique d’au moins 98%, un excès d’anions étant maintenu constant dans un mélange de réaction; et, après la réaction, une base solifénacine est transformée facultativement en sel de solifénacine selon des procédures standard. Du chlorure de (S)-1-phényl-1,2,3,4-tétrahydroisoquinolinecarbonyle d’une pureté chimique d’au moins 98% est obtenu dans une réaction de (S)-1-phényl-1,2,3,4-tétrahydroisoquinoline et d’un excès molaire de phosgène, en présence d’une amine aromatique tertiaire dans un hydrocarbure aromatique, et isolé sous une forme cristalline.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, 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, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (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, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, 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)