[go: up one dir, main page]

WO2004020439A3 - Improved process for preparation of risperidone - Google Patents

Improved process for preparation of risperidone Download PDF

Info

Publication number
WO2004020439A3
WO2004020439A3 PCT/IB2003/003830 IB0303830W WO2004020439A3 WO 2004020439 A3 WO2004020439 A3 WO 2004020439A3 IB 0303830 W IB0303830 W IB 0303830W WO 2004020439 A3 WO2004020439 A3 WO 2004020439A3
Authority
WO
WIPO (PCT)
Prior art keywords
risperidone
improved process
hours
preparation
base
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/IB2003/003830
Other languages
French (fr)
Other versions
WO2004020439A2 (en
Inventor
Sunil Sadanand Nadkarni
Rajiv Ghanshyam Shah
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to BR0306204-0A priority Critical patent/BR0306204A/en
Priority to AU2003256006A priority patent/AU2003256006A1/en
Publication of WO2004020439A2 publication Critical patent/WO2004020439A2/en
Publication of WO2004020439A3 publication Critical patent/WO2004020439A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention is for an improved process for of production of risperidone of formula (I) which comprises the steps of : (a) reacting a halo compound with an oxime ín a solvent and a base at 10-40°C; (b) refluxing the reaction mixture of step (a) for 4- 10 hours; (c) adding base to the cooled refluxed mixture of step (b) whileto maintaining the temperature at 20-40°C for 10-18 hours; (d) filtering and drying the risperidone thus obtained and (e) optionally purifying risperidone obtained in step (d). The invention also discloses a new polymorphic variety of risperidone namely, risperidone form T1 having its characteristic X-ray diffraction pattern and IR data.
PCT/IB2003/003830 2002-08-30 2003-08-25 Improved process for preparation of risperidone Ceased WO2004020439A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
BR0306204-0A BR0306204A (en) 2002-08-30 2003-08-25 Improved process for preparing risperidone
AU2003256006A AU2003256006A1 (en) 2002-08-30 2003-08-25 Improved process for preparation of risperidone

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN507CA2002 2002-08-30
IN507CAL2002 2002-08-30

Publications (2)

Publication Number Publication Date
WO2004020439A2 WO2004020439A2 (en) 2004-03-11
WO2004020439A3 true WO2004020439A3 (en) 2004-07-01

Family

ID=31972123

Family Applications (1)

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

Country Status (3)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10010612B2 (en) 2007-05-25 2018-07-03 Indivior Uk Limited Sustained delivery formulations of risperidone compounds
US10058554B2 (en) 2005-09-30 2018-08-28 Indivior Uk Limited Sustained release small molecule drug formulation

Families Citing this family (3)

* 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
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
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

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0196132A2 (en) * 1985-03-27 1986-10-01 Janssen Pharmaceutica N.V. 1,2-Benzisoxazol-3-yl and 1,2-benzisothiazol-3-yl derivatives
US4957916A (en) * 1988-08-05 1990-09-18 Janssen Pharmaceutica N.V. Antipsychotic 3-piperazinylbenzazole derivatives
EP0453042A1 (en) * 1990-04-19 1991-10-23 Janssen Pharmaceutica N.V. Novel 2,9-disubstituted-4H-pyrido-[1,2-a]pyrimidin-4-ones
ES2050069A1 (en) * 1992-07-10 1994-05-01 Vita Invest Sa Prepn of anti-psychotic pyrimidinone - which is 3-(2-(4-(6-fluoro- 1,2-benzisoxazol 3-yl)piperidino) ethyl)-2-methyl- 6,7,8,9-tetra- hydro-4H-pyrido (1,2-a) pyrimidin-4-one
WO1995014691A1 (en) * 1993-11-23 1995-06-01 Janssen Pharmaceutica N.V. NOVEL 9-HYDROXY-PYRIDO[1,2-a]PYRIMIDIN-4-ONE ETHER DERIVATIVES
WO2001034113A2 (en) * 1999-11-12 2001-05-17 Alkermes Controlled Therapeutics Inc. Ii Apparatus and method for preparing microparticles
WO2002014286A1 (en) * 2000-08-14 2002-02-21 Teva Pharmaceutical Industries Ltd. 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

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0196132A2 (en) * 1985-03-27 1986-10-01 Janssen Pharmaceutica N.V. 1,2-Benzisoxazol-3-yl and 1,2-benzisothiazol-3-yl derivatives
US4957916A (en) * 1988-08-05 1990-09-18 Janssen Pharmaceutica N.V. Antipsychotic 3-piperazinylbenzazole derivatives
EP0453042A1 (en) * 1990-04-19 1991-10-23 Janssen Pharmaceutica N.V. Novel 2,9-disubstituted-4H-pyrido-[1,2-a]pyrimidin-4-ones
ES2050069A1 (en) * 1992-07-10 1994-05-01 Vita Invest Sa Prepn of anti-psychotic pyrimidinone - which is 3-(2-(4-(6-fluoro- 1,2-benzisoxazol 3-yl)piperidino) ethyl)-2-methyl- 6,7,8,9-tetra- hydro-4H-pyrido (1,2-a) pyrimidin-4-one
WO1995014691A1 (en) * 1993-11-23 1995-06-01 Janssen Pharmaceutica N.V. NOVEL 9-HYDROXY-PYRIDO[1,2-a]PYRIMIDIN-4-ONE ETHER DERIVATIVES
WO2001034113A2 (en) * 1999-11-12 2001-05-17 Alkermes Controlled Therapeutics Inc. Ii Apparatus and method for preparing microparticles
WO2002014286A1 (en) * 2000-08-14 2002-02-21 Teva Pharmaceutical Industries Ltd. 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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"List of Pharmaceutical Substances, 12th edition, Q - R", 2001, ABDATA PHARMA-DATEN-SERVICE, ESCHBORN/TAUNUS, XP002273389 *
HALEBLIAN J ET AL: "PHARMACEUTICAL APPLICATIONS OF POLYMORPHISM", JOURNAL OF PHARMACEUTICAL SCIENCES, AMERICAN PHARMACEUTICAL ASSOCIATION. WASHINGTON, US, vol. 58, no. 8, 1 August 1969 (1969-08-01), pages 911 - 929, XP002020518, ISSN: 0022-3549 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10058554B2 (en) 2005-09-30 2018-08-28 Indivior Uk Limited Sustained release small molecule drug formulation
US11110093B2 (en) 2005-09-30 2021-09-07 Indivior Uk Limited Sustained release small molecule drug formulation
US10010612B2 (en) 2007-05-25 2018-07-03 Indivior Uk Limited Sustained delivery formulations of risperidone compounds
US10376590B2 (en) 2007-05-25 2019-08-13 Indivior Uk Limited Sustained delivery formulations of risperidone compound
US11712475B2 (en) 2007-05-25 2023-08-01 Indivior Uk Limited Sustained delivery formulations of risperidone compound

Also Published As

Publication number Publication date
WO2004020439A2 (en) 2004-03-11
AU2003256006A8 (en) 2004-03-19
BR0306204A (en) 2004-09-08
AU2003256006A1 (en) 2004-03-19

Similar Documents

Publication Publication Date Title
Zhang et al. Catalyst-free synthesis of quinazoline derivatives using low melting sugar–urea–salt mixture as a solvent
WO2004020439A3 (en) Improved process for preparation of risperidone
WO2003042169A3 (en) Process for synthesizing aspartic and glutamic acid derivatives and diazoketone intermediates thereof
BR0205683A (en) Process for the preparation of piperazine derivatives, and mesylate of a compound
CN112574190A (en) Method for synthesizing chlorantraniliprole
WO2008103367A3 (en) Method for assembling high-purity chemical libraries, proapoptotic compounds discovered by same
CN110818631A (en) Pyridine thiourea derivative and preparation method and application thereof
CA2425561A1 (en) Process to prepare 1,4-dihydropyridine intermediates and derivatives thereof
CN104710429B (en) Method for chiral spirocyclic phosphoric acid catalyzed synthesis of optically active quinoxaline derivative
Zahouily et al. Uncatalysed preparation of α-amino phosphonates under solvent free conditions
WO2007012983A3 (en) Process of producing amorolfine
CN101155795B (en) Process for producing substituted thiophenesulfonyl isocyanates
Gulevskaya et al. Oxidative arylamination of 1, 3-dinitrobenzene and 3-nitropyridine under anaerobic conditions: The dual role of the nitroarenes
Du et al. One-pot preparation of fluorinated propargylamines under microwave irradiation and solvent-free conditions
WO2008119734A3 (en) Process for the manufacture of organic compounds
JP3448635B2 (en) Sulfenamide compound and method for producing the same
Guo et al. Synthesis of 2, 3-dihydroquinazolinimines and 1, 3-diiminoisoindolines catalyzed by rare earth metal alkyl complexes through tandem addition/cyclization of nitriles with amines
JP2008514554A (en) Hydrogenation of α, β-unsaturated carbonyl compounds.
WO2004031153A3 (en) Enantioselective alkylation of tricyclic compounds
KR101710057B1 (en) A process for preparing amine compound using carbon-supported cobalt-rhodium nanoparticel catalyzed hydrogen-free recuctive amination
Aryanasab et al. A novel one-pot synthesis of 2-alkylthio-1, 3, 4-oxadiazoles in water
JP3338872B2 (en) Method for producing 1,2-benzisothiazolinone compound
CN117886718B (en) A method for preparing asymmetric urea compounds with high selectivity and asymmetric urea compounds
WO2011158813A1 (en) Method for producing n-substituted-2-amino-4-(hydroxymethylphosphinyl)-2-butenoic acid
PT1817274E (en) Method for producing amino- or hydroxybenzonitriles

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
WWE Wipo information: entry into national phase

Ref document number: 200503938

Country of ref document: ZA

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP