BR0306204A - Improved process for preparing risperidone - Google Patents

Improved process for preparing risperidone

Info

Publication number
BR0306204A
BR0306204A BR0306204-0A BR0306204A BR0306204A BR 0306204 A BR0306204 A BR 0306204A BR 0306204 A BR0306204 A BR 0306204A BR 0306204 A BR0306204 A BR 0306204A
Authority
BR
Brazil
Prior art keywords
risperidone
improved process
hours
preparing
base
Prior art date
Application number
BR0306204-0A
Other languages
Portuguese (pt)
Inventor
Sunil Sadanand Nadkarni
Rajiv Ghanshyam Shah
Original Assignee
Torrent Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Torrent Pharmaceuticals Ltd filed Critical Torrent Pharmaceuticals Ltd
Publication of BR0306204A publication Critical patent/BR0306204A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

"PROCESSO MELHORADO PARA A PREPARAçãO DE RISPERIDONA". A invenção é para um processo melhorado para a produção de risperidona da fórmula (I) que compreende as etapas de: (a) reagir um composto halo com uma oxima em um solvente e uma base em 10-40<198>C; (b) refluxar a mistura de reação da etapa (a) durante 4-10 horas; (C) adicionar base à mistura refluxada resfriada da etapa (b) ao mesmo tempo em que manter a temperatura em 20-40<198>c durante 10-18 horas; (d) filtrar e secar a risperidona desse modo obtida e (e) opcionalmente purificar a risperidona obtida na etapa (d). A invenção também divulga uma variedade polimórfica nova de risperidona isto é, a forma T1 de risperidona tendo seus dados de IR e padrão de difração de raio X característicos."IMPROVED PROCESS FOR PREPARING RISPERIDONE". The invention is for an improved process for the production of risperidone of formula (I) comprising the steps of: (a) reacting a halo compound with an oxime in a solvent and a base at 10-40Â ° C; (b) refluxing the reaction mixture from step (a) for 4-10 hours; (C) adding base to the cooled reflux mixture of step (b) while maintaining the temperature at 20-40 ° C for 10-18 hours; (d) filtering and drying the risperidone thus obtained and (e) optionally purifying the risperidone obtained in step (d). The invention also discloses a novel polymorphic variety of risperidone i.e. the T1 form of risperidone having its characteristic IR and X-ray diffraction pattern data.

BR0306204-0A 2002-08-30 2003-08-25 Improved process for preparing risperidone BR0306204A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN507CA2002 2002-08-30
PCT/IB2003/003830 WO2004020439A2 (en) 2002-08-30 2003-08-25 Improved process for preparation of risperidone

Publications (1)

Publication Number Publication Date
BR0306204A true BR0306204A (en) 2004-09-08

Family

ID=31972123

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0306204-0A BR0306204A (en) 2002-08-30 2003-08-25 Improved process for preparing risperidone

Country Status (3)

Country Link
AU (1) AU2003256006A1 (en)
BR (1) BR0306204A (en)
WO (1) WO2004020439A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IS7290A (en) * 2004-05-28 2005-11-29 Actavis Group Pharmaceutical formulations containing risperidone
US8852638B2 (en) 2005-09-30 2014-10-07 Durect Corporation Sustained release small molecule drug formulation
CN101801415B (en) 2007-05-25 2015-09-23 Rb医药品有限公司 The sustained delivery formulations of risperidone compounds
CN105367570B (en) * 2015-12-08 2017-10-10 天津市亨必达化学合成物有限公司 A kind of preparation method of Risperidone crystalline substance I type materials
CN105481854B (en) * 2015-12-08 2017-11-10 天津市亨必达化学合成物有限公司 A kind of preparation method of the brilliant III type material of Risperidone

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
US4957916A (en) * 1988-08-05 1990-09-18 Janssen Pharmaceutica N.V. Antipsychotic 3-piperazinylbenzazole derivatives
GB9008850D0 (en) * 1990-04-19 1990-06-13 Janssen Pharmaceutica Nv Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones
ES2050069B1 (en) * 1992-07-10 1994-12-16 Vita Invest Sa PROCEDURE FOR OBTAINING 3- (2- (4- (6-FLUORO-1,2-BENZISOXAZOL-3-IL) PIPERIDINO) ETIL) -2-METHYL-6,7,8,9-TETRAHIDRO-4H-PIRIDO (1,2-A) PIRIMIDIN-4-ONA.
EP0730594B1 (en) * 1993-11-23 1999-09-08 Janssen Pharmaceutica N.V. 9-HYDROXY-PYRIDO [1,2-a]PYRIMIDIN-4-ONE ETHER DERIVATIVES
US6331317B1 (en) * 1999-11-12 2001-12-18 Alkermes Controlled Therapeutics Ii Inc. Apparatus and method for preparing microparticles
HUP0302874A2 (en) * 2000-08-14 2003-12-29 Teva Pharmaceutical Industries Ltd. Process for preparation of risperidone
US20020193386A1 (en) * 2002-03-28 2002-12-19 Inigo Pfeiffer Polymorphic form of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-alpha]pyrimidin-4-one and formulations thereof

Also Published As

Publication number Publication date
AU2003256006A8 (en) 2004-03-19
WO2004020439A2 (en) 2004-03-11
WO2004020439A3 (en) 2004-07-01
AU2003256006A1 (en) 2004-03-19

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Legal Events

Date Code Title Description
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]