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WO2010082110A3 - Novel process for preparing pure 6-fluoro-3-piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to paliperidone - Google Patents

Novel process for preparing pure 6-fluoro-3-piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to paliperidone Download PDF

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Publication number
WO2010082110A3
WO2010082110A3 PCT/IB2010/000041 IB2010000041W WO2010082110A3 WO 2010082110 A3 WO2010082110 A3 WO 2010082110A3 IB 2010000041 W IB2010000041 W IB 2010000041W WO 2010082110 A3 WO2010082110 A3 WO 2010082110A3
Authority
WO
WIPO (PCT)
Prior art keywords
paliperidone
piperidin
fluoro
conversion
novel process
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/IB2010/000041
Other languages
French (fr)
Other versions
WO2010082110A2 (en
Inventor
Keval Rameshchandra Sodagar
Vineet Malik
Brijesh Nitinkumar Kapadia
Sudhir Hukamchand Jain
Sanjay Natvarlal Parikh
Arun Omprakash Sharma
Uday Rajaram Bapat
Bakulesh Mafatial Khamar
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.)
Cadila Pharmaceuticals Ltd
Original Assignee
Cadila 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 Cadila Pharmaceuticals Ltd filed Critical Cadila Pharmaceuticals Ltd
Publication of WO2010082110A2 publication Critical patent/WO2010082110A2/en
Publication of WO2010082110A3 publication Critical patent/WO2010082110A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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

Abstract

The invention relates to novel process for providing substantially pure 6-Fluoro-3- piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to Paliperidone having dimer compound of structural formula-1 A is less than 0.2 % and HPLC purity > 99.7%.
PCT/IB2010/000041 2009-01-13 2010-01-12 Novel process for preparing pure 6-fluoro-3-piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to paliperidone Ceased WO2010082110A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN79/MUM/2009 2009-01-13
IN79MU2009 2009-01-13

Publications (2)

Publication Number Publication Date
WO2010082110A2 WO2010082110A2 (en) 2010-07-22
WO2010082110A3 true WO2010082110A3 (en) 2010-09-10

Family

ID=42340158

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2010/000041 Ceased WO2010082110A2 (en) 2009-01-13 2010-01-12 Novel process for preparing pure 6-fluoro-3-piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to paliperidone

Country Status (1)

Country Link
WO (1) WO2010082110A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011015936A2 (en) * 2009-08-04 2011-02-10 Orchid Chemicals And Pharmaceuticals Ltd An improved process for the preparation of pure paliperidone
CN111087204B (en) * 2019-12-31 2021-11-05 山西凯迪建材有限公司 A kind of mineral admixture ternary cementitious material and preparation method thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4458076A (en) * 1983-05-31 1984-07-03 Hoechst-Roussel Pharmaceuticals 3-(4-Piperidinyl)-1,2-benzisothiazoles
US5783705A (en) * 1997-04-28 1998-07-21 Texas Biotechnology Corporation Process of preparing alkali metal salys of hydrophobic sulfonamides
US20080171875A1 (en) * 2006-08-14 2008-07-17 Santiago Ini Process for the synthesis of 9-hydroxy risperidone (paliperidone)

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4458076A (en) * 1983-05-31 1984-07-03 Hoechst-Roussel Pharmaceuticals 3-(4-Piperidinyl)-1,2-benzisothiazoles
US5783705A (en) * 1997-04-28 1998-07-21 Texas Biotechnology Corporation Process of preparing alkali metal salys of hydrophobic sulfonamides
US20080171875A1 (en) * 2006-08-14 2008-07-17 Santiago Ini Process for the synthesis of 9-hydroxy risperidone (paliperidone)

Also Published As

Publication number Publication date
WO2010082110A2 (en) 2010-07-22

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