ES2197801B1 - Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona. - Google Patents

Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona.

Info

Publication number
ES2197801B1
ES2197801B1 ES200200531A ES200200531A ES2197801B1 ES 2197801 B1 ES2197801 B1 ES 2197801B1 ES 200200531 A ES200200531 A ES 200200531A ES 200200531 A ES200200531 A ES 200200531A ES 2197801 B1 ES2197801 B1 ES 2197801B1
Authority
ES
Spain
Prior art keywords
methyl
isoxazol
piperidin
fluoro
benzo
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.)
Expired - Fee Related
Application number
ES200200531A
Other languages
English (en)
Other versions
ES2197801A1 (es
Inventor
Rafael Foguet Ambros
Jorge Ramentol Massana
Diego Fernandez Cano
Miguel P Armengol Montserrat
Francesc X Camps Camprubi
Juan Sallares Rosell
Ines Petschen Olive
Mireia Pasto Aguila
Esther Gordo Campon
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.)
Ferrer Internacional SA
Original Assignee
Ferrer Internacional SA
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
Priority to ES200200531A priority Critical patent/ES2197801B1/es
Application filed by Ferrer Internacional SA filed Critical Ferrer Internacional SA
Priority to RU2004129763/04A priority patent/RU2272037C9/ru
Priority to MXPA04008289A priority patent/MXPA04008289A/es
Priority to PCT/EP2003/002157 priority patent/WO2003074522A1/en
Priority to KR1020047013537A priority patent/KR100680003B1/ko
Priority to PL03370502A priority patent/PL370502A1/xx
Priority to AU2003219010A priority patent/AU2003219010A1/en
Priority to BR0308139-7A priority patent/BR0308139A/pt
Priority to US10/503,478 priority patent/US7205405B2/en
Priority to CNB038044870A priority patent/CN1315826C/zh
Priority to NZ534463A priority patent/NZ534463A/en
Priority to EP03714770A priority patent/EP1480978A1/en
Priority to CA002474811A priority patent/CA2474811A1/en
Priority to JP2003572990A priority patent/JP2005525366A/ja
Priority to UA20040907250A priority patent/UA80114C2/uk
Priority to IL16375003A priority patent/IL163750A0/xx
Publication of ES2197801A1 publication Critical patent/ES2197801A1/es
Priority to ZA200405939A priority patent/ZA200405939B/en
Priority to MA27800A priority patent/MA26353A1/fr
Priority to TNP2004000139A priority patent/TNSN04139A1/en
Priority to NO20043447A priority patent/NO20043447L/no
Priority to CO04085289A priority patent/CO5611140A2/es
Priority to CR7462A priority patent/CR7462A/es
Publication of ES2197801B1 publication Critical patent/ES2197801B1/es
Application granted granted Critical
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Abstract

Procedimiento de obtención de la 3-{2-[4-(6-fluoro- benzo[d]isoxazol-3-il)-piperidin-1-il]etil}-2-metil-6,7,8,9- tetrahidro-4H-pirido-[1,2-a]pirimidin-4-ona. Consiste en la condensación del (2-metil-4-oxo-6,7,8,9-tetrahidro-4H-pirido[1,2- a]pirimidin-3-il)-acetaldehído con el 6-fluoro-3-(4-piperidinil)- 1,2-benzisoxazol para dar lugar a la enamina intermedia 3-{2-[4- (6-fluoro-benzo[d]isoxazol-3-il)-piperidin-1-il]-vinil}-2-metil- 6,7,8,9-tetrahidro-pirido[1,2-a]pirimidin-4-ona seguido de reducción de la misma.
ES200200531A 2002-03-05 2002-03-05 Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona. Expired - Fee Related ES2197801B1 (es)

Priority Applications (22)

Application Number Priority Date Filing Date Title
ES200200531A ES2197801B1 (es) 2002-03-05 2002-03-05 Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona.
UA20040907250A UA80114C2 (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-(1,2-a) pyrimidin-4-one and derivatives
MXPA04008289A MXPA04008289A (es) 2002-03-05 2003-03-03 Procedimiento de obtencion de la 3- {2-[4 -(6-fluorobenzo [d]isoxazol- 3-il) piperidin- 1-il] -etil}-2 -metil-6, 7, 8, 9-tetrahidro- 4h-pirido -[1, 2-a] pirimidin -4-ona.
IL16375003A IL163750A0 (en) 2002-03-05 2003-03-03 Process for preparing (2-(4-(6-fluorobenzo(D)isoxazol-3-yl)-piperidin-1yl)-ethyl)-2- methyl-6,7,8,9-tetrahydro-4H-pyrido-(1,
PL03370502A PL370502A1 (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-(1,2-a) pyrimidin-4-one
AU2003219010A AU2003219010A1 (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-(1,2-a) pyrimidin-4-one
BR0308139-7A BR0308139A (pt) 2002-03-05 2003-03-03 Processo para preparação de 3-(2-(4-(6-fluorbenzo(d)isoxazol-3-il)-piperidin-1-il)-etil )-2-metil-6,7,8,9-tetraidro-4h-pirido-(1,2-a)-pirimidin-4-o na
US10/503,478 US7205405B2 (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d)isoxazol-3-yl)-piperidin-1-yl)-ethyl)-2-methyl- 6,7,8,9-tetrahydro-4h-pyrido-(1,2-a)pyrimidin-4-one
CNB038044870A CN1315826C (zh) 2002-03-05 2003-03-03 用于制备3－(2－(4－(6－氟苯并(d)异噁唑－3－基)－哌啶－1－基)－乙基)－2－甲基－6,7,8,9－四氢－4h－吡啶并－(1,2－a)嘧啶－4－酮的方法
NZ534463A NZ534463A (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1-yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido-(1,2-a) pyrimidin-4-one
EP03714770A EP1480978A1 (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-(1,2-a) pyrimidin-4-one
CA002474811A CA2474811A1 (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-(1,2-a) pyrimidin-4-one
RU2004129763/04A RU2272037C9 (ru) 2002-03-05 2003-03-03 Способ получения 3-{2-[4-(6-фторбензо[d]изоксазол-3-ил)пиперидин-1-ил]этил}-2-метил-6,7,8,9-тетрагидро-4н-пиридо[1,2-а]пиримидин-4-она, промежуточные производные для его получения и способ получения промежуточного производного
PCT/EP2003/002157 WO2003074522A1 (en) 2002-03-05 2003-03-03 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-(1,2-a) pyrimidin-4-one
KR1020047013537A KR100680003B1 (ko) 2002-03-05 2003-03-03 3-(2-(4-(6-플로로벤조(ｄ)아이소옥사졸-3-일)-피페리딘-1-일)-에틸)-2-메틸-6,7,8,9-테트라하이드로-4ｈ-피리도-(1,2-ａ)피리미딘-4-온의 제조방법
JP2003572990A JP2005525366A (ja) 2002-03-05 2003-03-03 ３−｛２−［４−（６−フルオロベンゾ［ｄ］イソオキサゾール−３−イル）−ピペリジン−１−イル］−エチル｝−２−メチル−６，７，８，９−テトラヒドロ−４Ｈ−ピリド−［１，２−ａ］ピリミジン−４−オンの調製方法
ZA200405939A ZA200405939B (en) 2002-03-05 2004-07-26 Process for preparing 3-(2-(4-(6-fluorobenzoÄdÜisoxazol-3-yl)-piperidin-1-yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido-(1,2-a)pyrimidin-4-one
MA27800A MA26353A1 (fr) 2002-03-05 2004-07-27 Procede pour la preparation de 3-{2-[4-(6-fluorobenzo[d] isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-[1,2-a]pyrimidin-4-one
TNP2004000139A TNSN04139A1 (en) 2002-03-05 2004-07-29 Process for preparing 3-(2-(4-(6-fluorobenzo(d) isoxazol-3-yl)-piperidin-1yl)-ethyl)-2-methyl-6,7,8,9-tetrahydro-4h-pyrido-(1,2-a) pyrimidin -4-one
NO20043447A NO20043447L (no) 2002-03-05 2004-08-18 Fremgangsmate for fremstilling av 3-(2-(4-(6-fluorbenzo(D)isoksazol-3-yl)-piperidin- l yl)-etyl)-2-metyl-6,7,8,9-tetrahydro-4H-pyrido-(1,2-A)pyrimidin-4-on
CO04085289A CO5611140A2 (es) 2002-03-05 2004-08-31 Procedimiento de obtencion de la 3-{2-[4-(6-fluorobenzo[d] isoxazol-3-il)-piperidin-1-il]-etil}-2-metil-6,7,8,9-tetrahidro-4h-pirido-[1,2-a]pirimidin-4-ona
CR7462A CR7462A (es) 2002-03-05 2004-09-03 Procedimiento de obtencion de la 3-[2-[4-(6-fluorobenzo[d]isoxazol-3-il)-piperidin-1-il]-etil}-2-metil-6,7,8,9-tetrahidro-4h-pirido-[1,2-a]pirimidin-4-ona

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES200200531A ES2197801B1 (es) 2002-03-05 2002-03-05 Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona.

Publications (2)

Publication Number Publication Date
ES2197801A1 ES2197801A1 (es) 2004-01-01
ES2197801B1 true ES2197801B1 (es) 2005-03-16

Family

ID=27772022

Family Applications (1)

Application Number Title Priority Date Filing Date
ES200200531A Expired - Fee Related ES2197801B1 (es) 2002-03-05 2002-03-05 Procedimiento de obtencion de la 3-(2-(4-(6-fluoro-benzo(d)isoxazol-3-il) piperidin-1-il)-etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido-(1,2-a ) pirimidin-4-ona.

Country Status (22)

Country Link
US (1) US7205405B2 (es)
EP (1) EP1480978A1 (es)
JP (1) JP2005525366A (es)
KR (1) KR100680003B1 (es)
CN (1) CN1315826C (es)
AU (1) AU2003219010A1 (es)
BR (1) BR0308139A (es)
CA (1) CA2474811A1 (es)
CO (1) CO5611140A2 (es)
CR (1) CR7462A (es)
ES (1) ES2197801B1 (es)
IL (1) IL163750A0 (es)
MA (1) MA26353A1 (es)
MX (1) MXPA04008289A (es)
NO (1) NO20043447L (es)
NZ (1) NZ534463A (es)
PL (1) PL370502A1 (es)
RU (1) RU2272037C9 (es)
TN (1) TNSN04139A1 (es)
UA (1) UA80114C2 (es)
WO (1) WO2003074522A1 (es)
ZA (1) ZA200405939B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003049744A1 (en) * 2001-12-05 2003-06-19 Barr Laboratories, Inc. Oral contraceptives to prevent pregnancy and diminish premenstrual symptomatology
KR20040025224A (ko) * 2002-09-18 2004-03-24 주식회사 대웅 2-(2-메틸-4-옥소-6,7,8,9-테트라하이드로-4Ｈ-피리도[1,2-ａ]피리미딘-3-일)아세트알데히드 및 그 제조방법

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
CA2000786C (en) * 1988-11-07 1999-01-26 Cornelus G. M. Janssen 3-piperidinyl-1,2-benzisoxazoles
GB9008850D0 (en) * 1990-04-19 1990-06-13 Janssen Pharmaceutica Nv Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones
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
CO5611140A2 (es) 2006-02-28
IL163750A0 (en) 2005-12-18
MXPA04008289A (es) 2004-11-26
CA2474811A1 (en) 2003-09-12
NO20043447L (no) 2004-08-18
RU2272037C9 (ru) 2006-06-20
EP1480978A1 (en) 2004-12-01
RU2272037C1 (ru) 2006-03-20
WO2003074522A1 (en) 2003-09-12
ES2197801A1 (es) 2004-01-01
KR20040091679A (ko) 2004-10-28
TNSN04139A1 (en) 2007-03-12
PL370502A1 (en) 2005-05-30
KR100680003B1 (ko) 2007-02-08
JP2005525366A (ja) 2005-08-25
US20050143395A1 (en) 2005-06-30
ZA200405939B (en) 2006-06-28
MA26353A1 (fr) 2004-10-01
NZ534463A (en) 2006-02-24
CN1639163A (zh) 2005-07-13
BR0308139A (pt) 2005-01-04
AU2003219010A1 (en) 2003-09-16
UA80114C2 (en) 2007-08-27
US7205405B2 (en) 2007-04-17
CN1315826C (zh) 2007-05-16
CR7462A (es) 2005-02-10

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