(WO/2006/117700) PROCESS FOR PREPARING QUETIAPINE AND QUETIAPINE FUMARATE

(WO/2006/117700) PROCESS FOR PREPARING QUETIAPINE AND QUETIAPINE FUMARATE

Latest bibliographic data on file with the International Bureau
Pub. No.:  WO/2006/117700   International Application No.:  PCT/IB2006/002286
Publication Date:09.11.2006 International Filing Date:21.04.2006
IPC: C07D 281/16 (2006.01), A61K 31/554 (2006.01), A61K 9/14 (2006.01), A61P 25/08 (2006.01)
Applicants:MEDICHEM, S.A. [ES/ES]; Fructuos Gelabert, 6-8, Sant Joan Despi, E-08970 Barcelona (ES) (All Except US).
BOSCH LLADÓ, Jordi [ES/ES]; (ES) (US Only).
BURGAROLAS MONTERO, Maria Carmen [ES/ES]; (ES) (US Only).
CHAMORRO GUTIERREZ, Iolanda [ES/ES]; (ES) (US Only).
Inventors:BOSCH LLADÓ, Jordi; (ES).
BURGAROLAS MONTERO, Maria Carmen; (ES).
CHAMORRO GUTIERREZ, Iolanda; (ES).
Priority Data:
60/673,373 21.04.2005 US
60/730,864 28.10.2005 US
Title: PROCESS FOR PREPARING QUETIAPINE AND QUETIAPINE FUMARATE
Abstract: The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][l,4]thiazepin-l l(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo [bf] [1,4] thiazepine. Thereafter, the l l-chloro-dibenzo[bf][1,4] thiazepine is reacted with 2-(2-piperazin-l-ylethoxy)-ethanol to yield, following several processing steps, quetiapine.. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Org. (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (EAPO) (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (OAPI) (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language:English (EN)
Filing Language:English (EN)

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