ES2587527T3 - Preparación de 3-[2-[4-((6-fluoro-1,2-bencisoxazol-3-il)-l-piperidinil)-6,7,8,9-tetrahidro-9-hidroxi-2-metil-4H-pirido[1,2 a]-primidin-4-ona (paliperidona) y palmitato de paliperidona - Google Patents

Preparación de 3-[2-[4-((6-fluoro-1,2-bencisoxazol-3-il)-l-piperidinil)-6,7,8,9-tetrahidro-9-hidroxi-2-metil-4H-pirido[1,2 a]-primidin-4-ona (paliperidona) y palmitato de paliperidona Download PDF

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Publication number
ES2587527T3
ES2587527T3 ES12792315.9T ES12792315T ES2587527T3 ES 2587527 T3 ES2587527 T3 ES 2587527T3 ES 12792315 T ES12792315 T ES 12792315T ES 2587527 T3 ES2587527 T3 ES 2587527T3
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Prior art keywords
pyrido
tetrahydro
methyl
hydroxy
paliperidone
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ES12792315.9T
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English (en)
Inventor
Ravi Ponnaiah
Praveen Kumar Neela
Kosireddy RAVANABABU
Kallepally SUDHEER
Narasimharao Venkata
Guruswamy Batthini
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    • 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)

Abstract

Procedimiento para preparar éster de palmitato de 3-(2-cloroetil)-6,7,8,9-tetrahidro-2-metil-9-hidroxi-4Hpirido[ 1,2-a]pirimidin-4-ona de fórmula V**Fórmula** que comprende las etapas de: (i) combinar 3-(2-cloroetil)-6,7,8,9-tetrahidro-2-metil-9-hidroxi-4H-pirido[1,2-a]pirimidin-4-ona de fórmula IV con un derivado de ácido graso en presencia de un derivado de piridina, al menos una base y al menos un disolvente orgánico para obtener una mezcla de reacción y (ii) añadir haluro de ácido a la mezcla de reacción obtenida en la etapa (i) y mantener la mezcla durante un tiempo suficiente para dar el compuesto, éster de palmitato de 3-(2-cloroetil)-6,7,8,9-tetrahidro-2-metil-9- hidroxi-4H-pirido[1,2-a]pirimidin-4-ona de fórmula V:**Fórmula**

Description

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Claims (1)

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ES12792315.9T 2011-05-31 2012-05-30 Preparación de 3-[2-[4-((6-fluoro-1,2-bencisoxazol-3-il)-l-piperidinil)-6,7,8,9-tetrahidro-9-hidroxi-2-metil-4H-pirido[1,2 a]-primidin-4-ona (paliperidona) y palmitato de paliperidona Active ES2587527T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN1854CH2011 2011-05-31
INCH18542011 2011-05-31
PCT/IN2012/000375 WO2012164582A1 (en) 2011-05-31 2012-05-30 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.

Publications (1)

Publication Number Publication Date
ES2587527T3 true ES2587527T3 (es) 2016-10-25

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Application Number Title Priority Date Filing Date
ES12792315.9T Active ES2587527T3 (es) 2011-05-31 2012-05-30 Preparación de 3-[2-[4-((6-fluoro-1,2-bencisoxazol-3-il)-l-piperidinil)-6,7,8,9-tetrahidro-9-hidroxi-2-metil-4H-pirido[1,2 a]-primidin-4-ona (paliperidona) y palmitato de paliperidona

Country Status (5)

Country Link
US (1) US8940749B2 (es)
EP (1) EP2683717B1 (es)
ES (1) ES2587527T3 (es)
PL (1) PL2683717T3 (es)
WO (1) WO2012164582A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013080220A2 (en) * 2011-11-28 2013-06-06 Davuluri Rammohan Rao 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.
KR101867988B1 (ko) * 2016-11-02 2018-06-15 주식회사 엔지켐생명과학 팔리페리돈 중간체 및 이를 이용한 팔리페리돈의 제조방법
CN112110914A (zh) * 2019-06-19 2020-12-22 上海天慈中商药业有限公司 一种帕潘立酮棕榈酸酯的制备方法
CN111533737A (zh) * 2020-05-22 2020-08-14 烟台大学 4-氟帕利哌酮棕榈酸酯及其制备方法和应用
CN111440168A (zh) * 2020-05-22 2020-07-24 烟台大学 6-甲氧基帕利哌酮棕榈酸酯制备方法及应用

Family Cites Families (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
TW487572B (en) * 1996-05-20 2002-05-21 Janssen Pharmaceutica Nv Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters
JP5249748B2 (ja) 2005-04-25 2013-07-31 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 無菌３−［２−［４−（６−フルオロ−１，２−ベンズイソオキサゾール−３−イル）−１−ピペリジニル］エチル］−６，７，８，９−テトラヒドロ−９−ヒドロキシ−２−メチル−４Ｈ−ピリド［１，２−ａ］ピリミジン−４−オンパルミチン酸エステルの製造
US20090048272A1 (en) * 2007-08-16 2009-02-19 Pratap Reddy Padi Preparation of paliperidone
US20090209757A1 (en) * 2008-01-10 2009-08-20 Santiago Ini Processes for the preparation and purification of paliperidone palmitate

Also Published As

Publication number Publication date
US20140073787A1 (en) 2014-03-13
EP2683717A1 (en) 2014-01-15
WO2012164582A1 (en) 2012-12-06
EP2683717B1 (en) 2016-05-25
PL2683717T3 (pl) 2016-11-30
US8940749B2 (en) 2015-01-27
EP2683717A4 (en) 2014-08-27

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