HUP0104873A2 - Javított eljárás 3-{2-[4-(6-fluor-1,2-benzizoxazol-3-il)-1-piperidinil]-etil}-6,7,8,9-tetrahidro-2-metil-4H-pirido[1,2-a]pirimidin-4-on előállítására - Google Patents

Javított eljárás 3-{2-[4-(6-fluor-1,2-benzizoxazol-3-il)-1-piperidinil]-etil}-6,7,8,9-tetrahidro-2-metil-4H-pirido[1,2-a]pirimidin-4-on előállítására

Info

Publication number
HUP0104873A2
HUP0104873A2 HU0104873A HUP0104873A HUP0104873A2 HU P0104873 A2 HUP0104873 A2 HU P0104873A2 HU 0104873 A HU0104873 A HU 0104873A HU P0104873 A HUP0104873 A HU P0104873A HU P0104873 A2 HUP0104873 A2 HU P0104873A2
Authority
HU
Hungary
Prior art keywords
formula
acid addition
pyrido
pyrimidin
piperidinyl
Prior art date
Application number
HU0104873A
Other languages
English (en)
Inventor
László Pongó
József Reiter
László Koncz
Gyula Simig
Kálmán Nagy
Donáth Györgyi Vereczkeyné
György Clementis
Gyuláné Körtvélyessy
Gábor Berecz
Péter Slégel
János Szulágyi
Original Assignee
EGIS Gyógyszergyár Rt.
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 EGIS Gyógyszergyár Rt. filed Critical EGIS Gyógyszergyár Rt.
Priority to HU0104873A priority Critical patent/HU227118B1/hu
Publication of HU0104873D0 publication Critical patent/HU0104873D0/hu
Priority to DK02803068T priority patent/DK1461338T3/da
Priority to US10/495,362 priority patent/US7307168B2/en
Priority to PT02803068T priority patent/PT1461338E/pt
Priority to EP02803068A priority patent/EP1461338B1/en
Priority to CZ2004698A priority patent/CZ2004698A3/cs
Priority to AT02803068T priority patent/ATE361298T1/de
Priority to DE60219957T priority patent/DE60219957T8/de
Priority to SI200230569T priority patent/SI1461338T1/sl
Priority to SK254-2004A priority patent/SK2542004A3/sk
Priority to PCT/HU2002/000120 priority patent/WO2003042212A1/en
Priority to JP2003544048A priority patent/JP4297785B2/ja
Priority to ES02803068T priority patent/ES2286332T3/es
Priority to PL02369233A priority patent/PL369233A1/xx
Publication of HUP0104873A2 publication Critical patent/HUP0104873A2/hu
Publication of HUP0104873A3 publication Critical patent/HUP0104873A3/hu
Priority to BG108757A priority patent/BG108757A/bg
Publication of HU227118B1 publication Critical patent/HU227118B1/hu

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

A találmány tárgya javított eljárás az (I) képletű 3-{2-[4-(6-fluor-1,2-benzizoxazol-3-il)-1-piperidinil]-etil}-6,7,8,9-tetrahidro-2-metil-4H-pirido[1,2a]pirimidin-4-on (risperidon) és gyógyászatilagalkalmas savaddíciós sói előállítására a (II) képletű oximnakalkálifém-hidroxid, alkálifém-karbonát vagy alkálifém-(1-4 szénatomosalkoxid) jelenlétében közömbös szerves oldószerben végzettgyűrűzárása, a képződő (I) képletű bázis savaddíciós sóvá alakításavagy a savaddíciós sóból az (I) képletű bázis felszabadítása útján. Atalálmány értelmében egy (XIV) általános képletű halogénszármazékot,ahol Hal jelentése halogénatom, egy (V) képletű piperidin-oximmal vagysavaddíciós sójával reagáltatnak bázis jelenlétében, és a képződő (II)képletű oxim gyűrűzárásánál közömbös oldószerként 1-4 szénatomosalkanolt alkalmaznak. Ó
HU0104873A 2001-11-13 2001-11-13 Process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzizoxazol-3-yl)-1-piperidinyl]-ethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one HU227118B1 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
HU0104873A HU227118B1 (en) 2001-11-13 2001-11-13 Process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzizoxazol-3-yl)-1-piperidinyl]-ethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
PL02369233A PL369233A1 (en) 2001-11-13 2002-11-13 Improved process for the preparation 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-a]pyrimidin-4-one
SI200230569T SI1461338T1 (sl) 2001-11-13 2002-11-13 Izboljšan postopek za pripravo 3-(2-(4-(6-fluoro-1,2-benzizoksazol-3-il)-1-piperidinil)etil)-6,7, 8,9-tetrahidro-2-metil-4H-pirido(1,2-A)pirimidin-4-ona
PCT/HU2002/000120 WO2003042212A1 (en) 2001-11-13 2002-11-13 Improved process for the preparation 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-a]pyrimidin-4-one
PT02803068T PT1461338E (pt) 2001-11-13 2002-11-13 Processo melhorado para a preparação de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)-1-piperidinil)etil)-6,7,8,9-tetra-hidro-2-metil-4h-pirido [1,2-a] pirimidin-4-ona
EP02803068A EP1461338B1 (en) 2001-11-13 2002-11-13 Improved process for the preparation 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-a)pyrimidin-4-one
CZ2004698A CZ2004698A3 (cs) 2001-11-13 2002-11-13 Zlepšený způsob přípravy 3-{2-[4-(6-fluor-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-onu
AT02803068T ATE361298T1 (de) 2001-11-13 2002-11-13 Verbessertes verfahren zur herstellung von 3-(2- (4-(6-fluor-1,2-benzisoxazol-3-yl)-1-
DE60219957T DE60219957T8 (de) 2001-11-13 2002-11-13 Verbessertes verfahren zur herstellung von 3-(2-(4-(6-fluor-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-2-methyl-4h-pyrido(1,2-a)pyrimidin-4-on
DK02803068T DK1461338T3 (da) 2001-11-13 2002-11-13 Forbedret fremgangsmåde til fremstillingen af 3-(2-(4-(6-fluor-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido(1,2-A)pyrimidin-4-on
SK254-2004A SK2542004A3 (en) 2001-11-13 2002-11-13 Improved process for the preparation 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
US10/495,362 US7307168B2 (en) 2001-11-13 2002-11-13 Process for the preparation of 3-{2-′4- (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyllethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido′1,2-methyl-4h-pyrido′,2-a!pyrimidin-4-one
JP2003544048A JP4297785B2 (ja) 2001-11-13 2002-11-13 ３−｛２−［４−（６−フルオロ−１，２−ベンズイソキサゾール−３−イル）−１−ピペリジニル］エチル｝−６，７，８，９−テトラヒドロ−２−メチル−４Ｈ−ピリド［１，２−ａ］ピリミジン−４−オンの改良した製法
ES02803068T ES2286332T3 (es) 2001-11-13 2002-11-13 Procedimiento mejorado para la preparacion de 3-(2-(4-(6-fluoro-1,2-bencisoxazol-3-il)-1-piperidinil)etil)-6,7,8,9-tetrahidro-2-metil-4h-pirido(1,2-a)pirimidin-4-ona.
BG108757A BG108757A (bg) 2001-11-13 2004-06-11 Подобрен метод за получаване на 3-{2-[4-(6-флуоро-1,2-бензизоксазол-3-ил)-1-пиперидинил]етил}-6,7,8,9-тетрахидро-2-метил-4н-пиридо[1,2-а]пиримидин-4-он

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
HU0104873A HU227118B1 (en) 2001-11-13 2001-11-13 Process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzizoxazol-3-yl)-1-piperidinyl]-ethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one

Publications (4)

Publication Number Publication Date
HU0104873D0 HU0104873D0 (en) 2002-01-28
HUP0104873A2 true HUP0104873A2 (hu) 2003-08-28
HUP0104873A3 HUP0104873A3 (en) 2003-11-28
HU227118B1 HU227118B1 (en) 2010-07-28

Family

ID=89979882

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0104873A HU227118B1 (en) 2001-11-13 2001-11-13 Process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzizoxazol-3-yl)-1-piperidinyl]-ethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one

Country Status (14)

Country Link
US (1) US7307168B2 (hu)
EP (1) EP1461338B1 (hu)
JP (1) JP4297785B2 (hu)
AT (1) ATE361298T1 (hu)
BG (1) BG108757A (hu)
CZ (1) CZ2004698A3 (hu)
DE (1) DE60219957T8 (hu)
DK (1) DK1461338T3 (hu)
ES (1) ES2286332T3 (hu)
HU (1) HU227118B1 (hu)
PL (1) PL369233A1 (hu)
PT (1) PT1461338E (hu)
SK (1) SK2542004A3 (hu)
WO (1) WO2003042212A1 (hu)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004009591A1 (en) * 2002-07-22 2004-01-29 Aurobindo Pharma Ltd. A process for the preparation of antipsychotic risperidone
EP1560814A1 (en) 2002-11-13 2005-08-10 Synthon B.V. Process for making risperidone and intermediates therefor
HUP0401379A3 (en) * 2004-07-08 2006-04-28 Richter Gedeon Vegyeszet Process for the preparation of risperidon
HUP0402163A2 (en) * 2004-10-25 2006-05-29 Richter Gedeon Vegyeszet Process for the preparation of risperidone
HUP0600555A3 (en) * 2006-07-03 2008-10-28 Egis Gyogyszergyar Nyrt Use of 4-chloro-5-{2-[4-(6-fluoro-1,2-benz[d]izoxazol-3-yl)piperidin-1-yl]ethylamino}2-methyl-3(2h)-piridazinon for the production of pharmaceutical compositions for influencing cognitive functions and causing neuroprotective effect

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
GB9008850D0 (en) * 1990-04-19 1990-06-13 Janssen Pharmaceutica Nv Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones
ES2085234B1 (es) * 1994-02-24 1997-01-16 Vita Invest Sa Agente activo sobre el sistema nervioso central, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen.
CZ295402B6 (cs) * 2000-05-05 2005-08-17 Rpg Life Sciences Limited Způsob přípravy antipsychotického 3-[2-[4-(6-fluor-1,2-benzizoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-onu

Also Published As

Publication number Publication date
PL369233A1 (en) 2005-04-18
SK2542004A3 (en) 2004-12-01
ATE361298T1 (de) 2007-05-15
DE60219957D1 (de) 2007-06-14
DE60219957T2 (de) 2008-01-17
WO2003042212A1 (en) 2003-05-22
HU0104873D0 (en) 2002-01-28
JP4297785B2 (ja) 2009-07-15
HUP0104873A3 (en) 2003-11-28
CZ2004698A3 (cs) 2004-09-15
EP1461338B1 (en) 2007-05-02
JP2005513019A (ja) 2005-05-12
PT1461338E (pt) 2007-07-23
ES2286332T3 (es) 2007-12-01
BG108757A (bg) 2005-03-31
US7307168B2 (en) 2007-12-11
HU227118B1 (en) 2010-07-28
US20050004141A1 (en) 2005-01-06
DE60219957T8 (de) 2008-04-24
DK1461338T3 (da) 2007-09-03
EP1461338A1 (en) 2004-09-29

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Legal Events

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HC9A Change of name, address

Owner name: EGIS GYOGYSZERGYAR NYILVANOSAN MUEKOEDOE RESZV, HU

Free format text: FORMER OWNER(S): EGIS GYOGYSZERGYAR RT., HU

MM4A Lapse of definitive patent protection due to non-payment of fees