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1. (WO2008100651) PREPARATION OF DARIFENACIN AND ITS SALTS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2008/100651    International Application No.:    PCT/US2008/050388
Publication Date: 21.08.2008 International Filing Date: 07.01.2008
IPC:
C07D 207/06 (2006.01), C07D 307/79 (2006.01), C07D 405/06 (2006.01)
Applicants: DR. REDDY'S LABORATORIES LTD. [IN/IN]; 7-1-27 Ameerpet, Hyderabad, 500 016, Andhra Pradesh (IN) (For All Designated States Except US).
DR. REDDY'S LABORATORIES, INC. [US/US]; 200 Somerset Corporate Boulevard 7th Floor, Bridgewater, NJ 08807 (US) (For All Designated States Except US).
KATKAM, Srinivas [IN/IN]; (IN) (For US Only).
VADDADI, Pattabhiramayya [IN/IN]; (IN) (For US Only).
SUNKARA, Vishnuvardhan [IN/IN]; (IN) (For US Only).
MUTTAVARAPU, Muralimohan [IN/IN]; (IN) (For US Only).
KULKARNI, Lalitha Dattatray [IN/IN]; (IN) (For US Only).
SAGYAM, Rajeshwar, Reddy [IN/IN]; (IN) (For US Only).
PITTA, Jaya, Prakash [IN/IN]; (IN) (For US Only).
BUCHNIKONDA, Ravinder [IN/IN]; (IN) (For US Only).
MUNAGALA, Sridhar [IN/IN]; (IN) (For US Only)
Inventors: KATKAM, Srinivas; (IN).
VADDADI, Pattabhiramayya; (IN).
SUNKARA, Vishnuvardhan; (IN).
MUTTAVARAPU, Muralimohan; (IN).
KULKARNI, Lalitha Dattatray; (IN).
SAGYAM, Rajeshwar, Reddy; (IN).
PITTA, Jaya, Prakash; (IN).
BUCHNIKONDA, Ravinder; (IN).
MUNAGALA, Sridhar; (IN)
Agent: CEPEDA, Milagros A.; Dr. Reddy's Laboratories, Inc., 7th floor, 200 Somerset Corporate Boulevard, Bridgewater, NJ 08807 (US)
Priority Data:
34/CHE/2007 05.01.2007 IN
60/894,711 14.03.2007 US
2060/CHE/2007 13.09.2007 IN
Title (EN) PREPARATION OF DARIFENACIN AND ITS SALTS
(FR) PRÉPARATION DE DARIFÉNACINE ET SES SELS
Abstract: front page image
(EN)Provided are various processes and compounds related to darifenacin and/or its salts. For example, there is provided a process for preparing a free base of darifenacin: Formula, or the salt thereof, the process including reacting 3-(S)-(cyanodiphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-yl) ethyl] pyrrolidine of the Formula (IV), or a salt thereof: Formula (IV) with a base effective to convert the nitrile group of the compound of the Formula (IV) to the amide group of the darifenacin in an organic solvent, the reaction being carried out in the organic solvent, with a proviso that the solvent is not 2-methyl-butan-2-ol, and with further proviso that the reaction produces less than about 0.5 % of the compound of the Formula (Ic): Formula (Ic) in the reaction mass, as measured by HPLC. Various embodiments and variants are provided.
(FR)L'invention concerne plusieurs procédés et composés associés à la darifénacine et/ou à ses sels. L'invention concerne par exemple un procédé de préparation d'une base libre de darifénacine : Formule ou de son sel. Le procédé comprend la mise en réaction de la 3-(S)-(cyanodiphénylméthyl)-1-[2-(2,3-dihydrobenzofuran-5-yl)éthyl] pyrrolidine de formule (IV) ou un de ses sels : Formule (IV) avec une base efficace pour transformer le groupement nitrile du composé de formule (IV) en groupement amide de la darifénacine dans un solvant organique, à condition que le solvant ne soit pas le 2-méthyl-butan-2-ol et que la réaction produise une quantité inférieure à environ 0,5 % du composé de formule (Ic) : Formule (Ic) dans la masse réactionnelle, telle que mesurée par HPLC. L'invention concerne également plusieurs modes de réalisation et plusieurs variantes.
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, 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, 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)