WO2013080220A3 - Process for preparation of 3-[2-[4-(6-fluro-1, 2-benzisoxazol-3-yl)-1-piperidtnyl]ethyl]-6, 7, 8, 9-tetrahydro-9-hydroxy-2-methyl-4h-pyriodo[1, 2-a]pyrimidin-4-one - Google Patents
Process for preparation of 3-[2-[4-(6-fluro-1, 2-benzisoxazol-3-yl)-1-piperidtnyl]ethyl]-6, 7, 8, 9-tetrahydro-9-hydroxy-2-methyl-4h-pyriodo[1, 2-a]pyrimidin-4-one Download PDFInfo
- Publication number
- WO2013080220A3 WO2013080220A3 PCT/IN2012/000771 IN2012000771W WO2013080220A3 WO 2013080220 A3 WO2013080220 A3 WO 2013080220A3 IN 2012000771 W IN2012000771 W IN 2012000771W WO 2013080220 A3 WO2013080220 A3 WO 2013080220A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- preparation
- pyriodo
- piperidtnyl
- fluro
- benzisoxazol
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 title 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title 1
- VOMKSBFLAZZBOW-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC3=C(C)N=C4N(C3=O)CCCC4OC(=O)CCCCCCCCCCCCCCC)=NOC2=C1 VOMKSBFLAZZBOW-UHFFFAOYSA-N 0.000 abstract 1
- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000007062 hydrolysis Effects 0.000 abstract 1
- 238000006460 hydrolysis reaction Methods 0.000 abstract 1
- 229960001057 paliperidone Drugs 0.000 abstract 1
- 229960000635 paliperidone palmitate Drugs 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A process for the preparation of paliperidone from the hydrolysis of paliperidone palmitate in the presence of an acid in a solvent.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN4104/CHE/2011 | 2011-11-28 | ||
IN4104CH2011 | 2011-11-28 |
Publications (2)
Publication Number | Publication Date |
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WO2013080220A2 WO2013080220A2 (en) | 2013-06-06 |
WO2013080220A3 true WO2013080220A3 (en) | 2013-07-25 |
Family
ID=48536197
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IN2012/000771 WO2013080220A2 (en) | 2011-11-28 | 2012-11-26 | An improved process for the preparation of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydio-9-hydroxy-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one. |
Country Status (1)
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WO (1) | WO2013080220A2 (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN112110914A (en) * | 2019-06-19 | 2020-12-22 | 上海天慈中商药业有限公司 | Preparation method of paliperidone palmitate |
CN111533737A (en) * | 2020-05-22 | 2020-08-14 | 烟台大学 | 4-Flupaliperidone palmitate and its preparation method and application |
CN111440168A (en) * | 2020-05-22 | 2020-07-24 | 烟台大学 | Preparation method and application of 6-methoxy paliperidone palmitate |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20090048272A1 (en) * | 2007-08-16 | 2009-02-19 | Pratap Reddy Padi | Preparation of paliperidone |
WO2009089076A2 (en) * | 2008-01-10 | 2009-07-16 | Teva Pharmaceutical Industries Ltd. | Processes for the preparation and purification of paliperidone palmitate |
WO2011067220A1 (en) * | 2009-12-01 | 2011-06-09 | Chemo Ibérica, S.A. | A process for the purification of paliperidone |
WO2011074017A1 (en) * | 2009-12-17 | 2011-06-23 | Alkem Laboratories Ltd. | A novel process for the preparation of paliperidone |
WO2012164582A1 (en) * | 2011-05-31 | 2012-12-06 | Ramamohan Rao Davuluri | Preparation of 3-[2-[4-((6-fluoro-1, 2-benzisoxazol-3-yl)-l-piperidinyl)-6, 7, 8, 9-tetrahydro-9-hydroxy-2-methyl-4h-pyrido[ 1, 2-a]-pyrimidin-4-one (paliperidone) and paliperidone palmitate. |
-
2012
- 2012-11-26 WO PCT/IN2012/000771 patent/WO2013080220A2/en active Application Filing
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20090048272A1 (en) * | 2007-08-16 | 2009-02-19 | Pratap Reddy Padi | Preparation of paliperidone |
WO2009089076A2 (en) * | 2008-01-10 | 2009-07-16 | Teva Pharmaceutical Industries Ltd. | Processes for the preparation and purification of paliperidone palmitate |
WO2011067220A1 (en) * | 2009-12-01 | 2011-06-09 | Chemo Ibérica, S.A. | A process for the purification of paliperidone |
WO2011074017A1 (en) * | 2009-12-17 | 2011-06-23 | Alkem Laboratories Ltd. | A novel process for the preparation of paliperidone |
WO2012164582A1 (en) * | 2011-05-31 | 2012-12-06 | Ramamohan Rao Davuluri | Preparation of 3-[2-[4-((6-fluoro-1, 2-benzisoxazol-3-yl)-l-piperidinyl)-6, 7, 8, 9-tetrahydro-9-hydroxy-2-methyl-4h-pyrido[ 1, 2-a]-pyrimidin-4-one (paliperidone) and paliperidone palmitate. |
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WO2013080220A2 (en) | 2013-06-06 |
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