WO2013046225A3 - Process for the preparation of paliperidone palmitate - Google Patents

Process for the preparation of paliperidone palmitate Download PDF

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Publication number
WO2013046225A3
WO2013046225A3 PCT/IN2012/000539 IN2012000539W WO2013046225A3 WO 2013046225 A3 WO2013046225 A3 WO 2013046225A3 IN 2012000539 W IN2012000539 W IN 2012000539W WO 2013046225 A3 WO2013046225 A3 WO 2013046225A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
paliperidone palmitate
paliperidone
palmitate
reacting
Prior art date
Application number
PCT/IN2012/000539
Other languages
French (fr)
Other versions
WO2013046225A2 (en
Inventor
Milind Gharpure
Dnyandev Rane
Veerabhadra SWAMY H. M.
Prashant Patil
Jitendra THORAT
Original Assignee
Glenmark Generics Limited
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 Glenmark Generics Limited filed Critical Glenmark Generics Limited
Publication of WO2013046225A2 publication Critical patent/WO2013046225A2/en
Publication of WO2013046225A3 publication Critical patent/WO2013046225A3/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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/54—Preparation of carboxylic acid anhydrides
    • C07C51/56—Preparation of carboxylic acid anhydrides from organic acids, their salts, their esters or their halides, e.g. by carboxylation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/58—Preparation of carboxylic acid halides
    • C07C51/60—Preparation of carboxylic acid halides by conversion of carboxylic acids or their anhydrides or esters, lactones, salts into halides with the same carboxylic acid part

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention provides a process for the preparation of paliperidone palmitate comprising reacting paliperidone with palmitic acid or its derivative in the presence of a mixture of an organic base and an inorganic base.
PCT/IN2012/000539 2011-08-10 2012-08-03 Process for the preparation of paliperidone palmitate WO2013046225A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN2252/MUM/2011 2011-08-10
IN2252MU2011 2011-08-10
IN3576/MUM/2011 2011-12-20
IN3576MU2011 2011-12-20

Publications (2)

Publication Number Publication Date
WO2013046225A2 WO2013046225A2 (en) 2013-04-04
WO2013046225A3 true WO2013046225A3 (en) 2013-06-13

Family

ID=47996557

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2012/000539 WO2013046225A2 (en) 2011-08-10 2012-08-03 Process for the preparation of paliperidone palmitate

Country Status (1)

Country Link
WO (1) WO2013046225A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106220622A (en) * 2016-06-30 2016-12-14 广州仁恒医药科技有限公司 A kind of preparation method of Palmic acid 9-hydroxy-risperidone
WO2018232053A2 (en) * 2017-06-15 2018-12-20 Savior Lifetec Corporation Methods for producing particles of an active ingredient
CN109400602B (en) * 2017-08-15 2021-09-28 正大天晴药业集团股份有限公司 Preparation method of paliperidone palmitate
CN113024546B (en) * 2019-12-25 2022-06-10 江苏晶立信医药科技有限公司 Preparation method of small-particle-size paliperidone palmitate
CN111533737A (en) * 2020-05-22 2020-08-14 烟台大学 4-fluorophlipiperidone palmitate and preparation method and application thereof
CN114181206A (en) * 2021-12-22 2022-03-15 辰欣药业股份有限公司 Preparation method of paliperidone palmitate
CN116678982B (en) * 2023-08-01 2023-10-27 济南辰欣医药科技有限公司 Detection method of paliperidone palmitate impurity SM1-G

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5158952A (en) * 1988-11-07 1992-10-27 Janssen Pharmaceutica N.V. 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
US5254556A (en) * 1988-11-07 1993-10-19 Janssen Pharmaceutica N.V. 3-piperidinyl-1,2-benzisoxazoles
CN1206347A (en) * 1996-05-20 1999-01-27 詹森药业有限公司 Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters
CN1278730A (en) * 1997-11-17 2001-01-03 詹森药业有限公司 Aqueous suspensions of submicron 9-hydroxyrisperidone fatty acid esters
CN101163702A (en) * 2005-04-25 2008-04-16 詹森药业有限公司 Preparation of aseptic 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4h-pyridio[1,2-a]pyrimidin-4-one palmitate ester
WO2009089076A2 (en) * 2008-01-10 2009-07-16 Teva Pharmaceutical Industries Ltd. Processes for the preparation and purification of paliperidone palmitate

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5158952A (en) * 1988-11-07 1992-10-27 Janssen Pharmaceutica N.V. 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
US5254556A (en) * 1988-11-07 1993-10-19 Janssen Pharmaceutica N.V. 3-piperidinyl-1,2-benzisoxazoles
CN1206347A (en) * 1996-05-20 1999-01-27 詹森药业有限公司 Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters
CN1278730A (en) * 1997-11-17 2001-01-03 詹森药业有限公司 Aqueous suspensions of submicron 9-hydroxyrisperidone fatty acid esters
CN101163702A (en) * 2005-04-25 2008-04-16 詹森药业有限公司 Preparation of aseptic 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4h-pyridio[1,2-a]pyrimidin-4-one palmitate ester
WO2009089076A2 (en) * 2008-01-10 2009-07-16 Teva Pharmaceutical Industries Ltd. Processes for the preparation and purification of paliperidone palmitate

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
ANONYM.: "Crystalline form of 3-[2-[4-(6-fluoro-1,2 benzoisoxazol-3-yl)-1 -piperidyl]ethyl]-6,7,8,9 -tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one palmitate ester.", IP.COM JOURNAL, 4 June 2008 (2008-06-04), XP013125187 *
GUY, J.B. ET AL.: "Higher Aliphatic Compounds. Part VII. The Binary Systems, Palmitamide-Stearamide, Palmitanilide-Stearanilide, and Methyl Palmitate-Methyl Stearate. Purification of Palmitic and Stearic Acids.", JOURNAL OF CHEMICAL SOCIETY(RESUMED), 1 January 1939 (1939-01-01), pages 615 - 618, XP009117471 *
SMITH, J.C. CXI.: "Higher Aliphatic Compounds. Part I. The Systems Ethyl Palmitate-Ethyl Stearate and Hexadecyl Alcohol-Octadecyl Alcohol.", JOURNAL OF CHEMICAL SOCIETY(RESUMED), 1 January 1931 (1931-01-01), pages 802 - 807, XP009117470 *

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