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1. (WO2007004234) A PROCESS FOR THE PREPARATION OF 2-[2-(4-DIBENZO[b,f] [L,4] THIAZEPIN-11-yl-1- PIPERAZINYL)ETHOXY] ETHANOL FUMARATE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2007/004234    International Application No.:    PCT/IN2005/000379
Publication Date: 11.01.2007 International Filing Date: 23.11.2005
IPC:
C07D 281/16 (2006.01)
Applicants: USV LIMITED [IN/IN]; BSD Marg, Govandi, Mumbai 400 088 (IN) (For All Designated States Except US).
Tarur, Venkatasubramanian, Radhakrishnan [IN/IN]; (IN) (For US Only).
SATHE, Dhananjay, Govind [IN/IN]; (IN) (For US Only).
NAIDU, Avinash, Venkatraman [IN/IN]; (IN) (For US Only).
AHER, Umesh, Parashram [IN/IN]; (IN) (For US Only).
PATIL , Sachin, Shivaji [IN/IN]; (IN) (For US Only)
Inventors: Tarur, Venkatasubramanian, Radhakrishnan; (IN).
SATHE, Dhananjay, Govind; (IN).
NAIDU, Avinash, Venkatraman; (IN).
AHER, Umesh, Parashram; (IN).
PATIL , Sachin, Shivaji; (IN)
Agent: MADAN, Jose, A.; Khaitan & Co, Advocates, Notaries, Patent & Trade Mark Attorneys, Meher Chambers, 4th & 5th Floors, R K Marg, Ballard Estate, Mumbai 400 038, Maharashtra (IN)
Priority Data:
787/MUM/2005 04.07.2005 IN
Title (EN) A PROCESS FOR THE PREPARATION OF 2-[2-(4-DIBENZO[b,f] [L,4] THIAZEPIN-11-yl-1- PIPERAZINYL)ETHOXY] ETHANOL FUMARATE
(FR) PROCÉDÉ DE PRÉPARATION DU FUMARATE DE 2-[2-(4-DIBENZO[b,f][L,4]THIAZÉPIN-11-YL-1-PIPÉRAZINYL)ÉTHOXY]ÉTHANOL
Abstract: front page image
(EN)A process for the preparation of 2-[2-(4-Dibenzo[b,f] [l,4] thiazepin-11-yl-1- &rgr;iperazinyl)ethoxy] ethanol fumarate commonly known as Quetiapine hemifumarate. Dibenzo[b,f] [l,4] thiazepin-11-[10H]one is halogenated with a halogenating agent in the ratio of 1 : 0.5 to 3 w/v in an organic solvent in the presence of an organic base at reflux temperature followed by condensation of the reaction with piperazine without isolating the imino chloride. The piperazinyl-dibenzo[b,f] [l,4] thiazepine is converted to Quetiapine hemifumarate which is purified by crystallization with alcohol at reflux temperature and precipitated it by cooling the reaction mixture and recovered by filtration.
(FR)La présente invention concerne un procédé de préparation du fumarate de 2-[2-(4-dibenzo[b,f][l,4]thiazépin-11-yl-1-pipérazinyl)éthoxy]éthanol généralement connu sous le nom de hémifumarate de quétiapine. La dibenzo[b,f][l,4]thiazépin-11-[10H]one est halogénée grâce un agent d'halogénation utilisé dans un rapport de 1/0,5 à 3 en poids par volume dans un solvant organique en présence d'une base organique à la température de reflux suivi de la condensation du produit de la réaction avec la pipérazine sans isoler l’iminochlorure. La pipérazinyl-dibenzo[b,f][l,4]thiazépine est convertie en hémifumarate de quétiapine, lequel est purifié par cristallisation dans un alcool à la température de reflux et précipité en refroidissant le mélange réactionnel et recueilli par filtration.
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 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, HU, IE, IS, IT, LT, LU, LV, MC, NL, 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)