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Machine translation
1. (WO2007093870) A PROCESS FOR THE PREPARATION OF RISPERIDONE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2007/093870    International Application No.:    PCT/IB2007/000289
Publication Date: 23.08.2007 International Filing Date: 08.02.2007
IPC:
C07D 417/04 (2006.01), C07D 498/04 (2006.01), C07D 239/70 (2006.01), C07D 239/88 (2006.01)
Applicants: ORCHID CHEMICALS & PHARMACEUTICALS LIMITED [IN/IN]; Orchid Towers, 313 Valluvar Kottam High Road, Nungambakkam, Tamil Nadu, 600 034 Chennai (IN) (For All Designated States Except US).
BALLA, Venkata, Sasidhar [IN/IN]; (IN) (For US Only).
UPPARAPALLI, Sampathkumar [IN/IN]; (IN) (For US Only).
VELUPPILLAI, Loganathan [IN/IN]; (IN) (For US Only).
SIVALINGAM, Lakshmi [IN/IN]; (IN) (For US Only).
SIRIPRAGADA, Mahender, Rao [IN/IN]; (IN) (For US Only)
Inventors: BALLA, Venkata, Sasidhar; (IN).
UPPARAPALLI, Sampathkumar; (IN).
VELUPPILLAI, Loganathan; (IN).
SIVALINGAM, Lakshmi; (IN).
SIRIPRAGADA, Mahender, Rao; (IN)
Agent: HARIHARAN, Rajeshwari; K & S Partners, 84-C, C-6 Lane, Off Central Avenue, Sainik Farms, New Delhi 110 062 (IN)
Priority Data:
240/CHE/2006 15.02.2006 IN
08/CHE/2007 02.01.2007 IN
Title (EN) A PROCESS FOR THE PREPARATION OF RISPERIDONE
(FR) PROCÉDÉ DE SYNTHÈSE DE LA RISPÉRIDONE
Abstract: front page image
(EN)The present invention relates to an improved process for the preparation of Risperidone of formula (I) by condensing 6-fluoro-3- (4-piperidinyl)-l, 2- benzisoxazole with 3-(2-chloroethyl)-6, 7, 8, 9-tetrahydro-2-methyl-4H-pyrido [1,2-a] pyrimidin-4-one in water and water immiscible solvents under basic conditions in the presence of a catalyst. This invention also relates to a method for purification of crude Risperidone by removing an impurity specifically named as 9-hydroxy Risperidone to undetectable level using acid chlorides and an organic base in a suitable solvent.
(FR)La présente invention concerne un procédé amélioré de synthèse de la Rispéridone de formule (I) par condensation du 6-fluoro-3-(4-pipéridinyl)-l,2-benzisoxazole avec la 3-(2-chloroéthyl)-6,7,8,9-tétrahydro-2-méthyl-4H-pyrido[1,2-a]pyrimidin-4-one dans l'eau et des solvants immiscibles à l'eau dans des conditions basiques en présence d'un catalyseur. La présente invention concerne également une méthode de purification de Rispéridone brute par élimination d'une impureté spécifique, la 9-hydroxy-Rispéridone, jusqu'à un niveau non détectable en utilisant des chlorures d'acide et une base organique dans un solvant adapté.
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, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, 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, 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)