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ES2074966A1 - PROCEDURE TO OBTAIN 3- (2- (4- (6-FLUO-RURO-BENZO (D) ISOXAZOL-3-IL) -PIPERIDIN-1-IL) -ETIL) -2-METHYL-6, 7,8 , 9-TETRAHIDRO-4H-PIRIDO- (1,2-A) PIRIMIDIN-4-ONA. - Google Patents

PROCEDURE TO OBTAIN 3- (2- (4- (6-FLUO-RURO-BENZO (D) ISOXAZOL-3-IL) -PIPERIDIN-1-IL) -ETIL) -2-METHYL-6, 7,8 , 9-TETRAHIDRO-4H-PIRIDO- (1,2-A) PIRIMIDIN-4-ONA.

Info

Publication number
ES2074966A1
ES2074966A1 ES09400252A ES9400252A ES2074966A1 ES 2074966 A1 ES2074966 A1 ES 2074966A1 ES 09400252 A ES09400252 A ES 09400252A ES 9400252 A ES9400252 A ES 9400252A ES 2074966 A1 ES2074966 A1 ES 2074966A1
Authority
ES
Spain
Prior art keywords
ona
methyl
isoxazol
piperidin
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.)
Granted
Application number
ES09400252A
Other languages
Spanish (es)
Other versions
ES2074966B1 (en
Inventor
Barjoan Pere Dalmases
Olondriz Francisco Marquillas
Clotet Joan Huguet
Rovira Anna Bosch
CASTILLO NIETO Juan DEL
Ges Jose Caldero
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.)
Vita Invest SA
Original Assignee
Vita Invest 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
Application filed by Vita Invest SA filed Critical Vita Invest SA
Priority to ES09400252A priority Critical patent/ES2074966B1/en
Priority to GR950100035A priority patent/GR1002344B/en
Priority to SK156-95A priority patent/SK281752B6/en
Priority to IS4259A priority patent/IS1766B/en
Priority to CZ1995329A priority patent/CZ286398B6/en
Priority to PT101654A priority patent/PT101654B/en
Priority to EG11595A priority patent/EG20877A/en
Priority to NO950501A priority patent/NO306022B1/en
Priority to AT0024995A priority patent/AT405401B/en
Priority to FI950579A priority patent/FI110000B/en
Priority to HU9500418A priority patent/HU222110B1/en
Priority to RU95101859/04A priority patent/RU2123004C1/en
Priority to PL95307200A priority patent/PL181420B1/en
Priority to KR1019950002516A priority patent/KR100221108B1/en
Publication of ES2074966A1 publication Critical patent/ES2074966A1/en
Application granted granted Critical
Publication of ES2074966B1 publication Critical patent/ES2074966B1/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

PROCEDIMIENTO PARA LA OBTENCION DE 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. EL PROCEDIMIENTO CONSISTE EN HACER REACCIONAR LA 3-(2-AMINOETIL)-2-METIL-6,7,8,9-TETRAHIDRO-4H-PIRIDO[1,2-A]PIRIMIDIN-4-ONA, DE FORMULA II, CON COMPUESTOS DE FORMULA GENERAL III, DONDE "Y" Y "Z" SON GRUPOS SALIENTES, IGUALES O DISTINTOS ENTRE SI, TALES COMO HALOGENO O UN GRUPO ALQUIL O ARILSULFONILOXI, EN PRESENCIA DE UN DISOLVENTE Y UNA BASE ADECUADOS, PARA PROPORCIONAR LA 3-2-[4-6-FLUORO-BENZO[D]ISOXAZOL-3-IL)-PIPERIDIN-1-IL]ETIL-2-METIL-6,7,8,9-TETRAHIDRO-4H-PIRIDO[L,2-A]PIRIMIDIN-4-ONA DE FORMULA GENERAL I. DICHO COMPUESTO TIENE APLICACIONES FARMACEUTICAS POR SUS PROPIEDADES ANTIPSICOTICAS. SE REIVINDICAN ASIMISMO LOS PRODUCTOS DE FORMULAS II Y III, NECESARIOS PARA EL DESARROLLO DE LA PRESENTE INVENCION.PROCEDURE FOR OBTAINING 3-2- [4- (6-FLUORO-BENZO [D] ISOXAZOL-3-IL) -PIPERIDIN-1-IL] -ETHYL-2-METHYL-6,7,8,9-TETRAHYDRO -4H-PYRID [1,2, -A] -PYRIMIDIN-4-ONA. THE PROCEDURE CONSISTS OF REACTING 3- (2-AMINOETHYL) -2-METHYL-6,7,8,9-TETRAHYDRO-4H-PYRID [1,2-A] PYRIMIDIN-4-ONA, FROM FORMULA II, WITH COMPOUNDS OF GENERAL FORMULA III, WHERE "Y" AND "Z" ARE OUTGOING GROUPS, EQUAL OR DIFFERENT FROM EACH OTHER, SUCH AS HALOGEN OR AN ALKYL OR ARYLSULFONYLOXY GROUP, IN THE PRESENCE OF A SUITABLE SOLVENT AND BASE, TO PROVIDE THE 3-2 - [4-6-FLUORO-BENZO [D] ISOXAZOL-3-IL) -PIPERIDIN-1-IL] ETHYL-2-METHYL-6,7,8,9-TETRAHYDRO-4H-PYRID [L, 2-A ] PIRIMIDIN-4-ONA OF GENERAL FORMULA I. SAID COMPOUND HAS PHARMACEUTICAL APPLICATIONS FOR ITS ANTIPSYCHOTIC PROPERTIES. THE PRODUCTS OF FORMULAS II AND III, NECESSARY FOR THE DEVELOPMENT OF THE PRESENT INVENTION, ARE ALSO CLAIMED.

ES09400252A 1994-02-11 1994-02-11 PROCEDURE FOR OBTAINING 3- (2- (4- (6-FLUORO-BENZO (D) ISOXAZOL-3-IL) PIPERIDIN-1-IL) -ETIL) -2-METHYL-6,7,8,9- TETRAHIDRO-4H-PIRIDO- (1,2-A) PIRIMIDIN-4-ONA. Expired - Fee Related ES2074966B1 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
ES09400252A ES2074966B1 (en) 1994-02-11 1994-02-11 PROCEDURE FOR OBTAINING 3- (2- (4- (6-FLUORO-BENZO (D) ISOXAZOL-3-IL) PIPERIDIN-1-IL) -ETIL) -2-METHYL-6,7,8,9- TETRAHIDRO-4H-PIRIDO- (1,2-A) PIRIMIDIN-4-ONA.
GR950100035A GR1002344B (en) 1994-02-11 1995-02-01 A method for obtaining 3-{2-£4-(6-fluoro-benzo£D|isoxazol-3yl)piperidine -1-il|-ethyl}-2-methyl-6,7,8,9-tetrahudro-4H-pyrido£1,2-A|pyrimidine-4-one.
SK156-95A SK281752B6 (en) 1994-02-11 1995-02-07 METHOD OF PREPARATION 3- {2- [4- (6-FLUORBENZO [D] IZOXAZOL-3-YL) PIPERIDINE-1-YL] ETYL} -2-METHYL-6,7,8,9-TETRAHYDRO-4H-PYRIDOL [ 1,2-A] PYRIMIDIN-4-ONE AND THE PRODUCTS OF THIS METHOD
IS4259A IS1766B (en) 1994-02-11 1995-02-08 Process for obtaining 3- {2- [4- (6-fluoro-benzo [D] isoxazol-3-yl) piperidin-1-yl] ethyl} -2-methyl-6,7,8,9- tetrahydro-4H-pyrido [1,2-a] pyrimidin-4-one
CZ1995329A CZ286398B6 (en) 1994-02-11 1995-02-08 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
EG11595A EG20877A (en) 1994-02-11 1995-02-09 A method for obtaining 3- (2- 4-6- fluoro - benzo (d) isoxazol -3- yl) piperidine 1-il) -ethyl) -2- methyl - 6,7,8-tetrahydro-4h-pyrido (1,2-a) pyrimidine -4- one
NO950501A NO306022B1 (en) 1994-02-11 1995-02-09 Process for obtaining 3- {2- [4- (6-fluoro-benzo [d] isoxazol-3-yl) piperidin-1-yl] ethyl} -2-methyl-6,7,8,9-tetrahydro -4H-pyrido [1,2-a] pyrimidin-4-one
PT101654A PT101654B (en) 1994-02-11 1995-02-09 3- (6-FLUORO-BENZO- (D) -ISOXAZOL-3-YL) PIPERIDIN-1-YL} -ETHYL] -2-METHYL-6,7, 8,9-TETRAHYDRO-4H-PYRIDO- {1,2-A} PYRIMIDIN-4-ONA
AT0024995A AT405401B (en) 1994-02-11 1995-02-10 PROCESS FOR THE PREPARATION OF 3- (2- (4- (6-FLUORO-BENZO (D) ISOXAZOL-3-YL) PIPERIDINE-1-YL) -ETHYL) - 2-METHYL-6,7,8,9-TETRAHYDRO -4H- PYRIDO (1,2-A) PYRIMIDIN-4-ON
FI950579A FI110000B (en) 1994-02-11 1995-02-10 Process for obtaining 3- {2- [4- (6-fluoro-benzo [d] isoxazol-3-yl) piperidin-1-yl] -ethyl} -2-methyl-6,7,8,9-tetrahydro -4H-pyrido [1,2-a] pyrimidine-4-one
HU9500418A HU222110B1 (en) 1994-02-11 1995-02-10 Process 3- {2- [4- (6-Fluoro-benzo [d] isoxazol-3-yl) -piperidin-1-yl] -ethyl} -2-methyl-6,7,8,9-tetrahydro-4H pyrido [1,2-a] pyrimidin-4-one and intermediates of the process
RU95101859/04A RU2123004C1 (en) 1994-02-11 1995-02-10 METHOD OF PREPARING 3-(2-[4-6-FLUOROBENZO [d] ISOXAZOL-3- YL] PIPERIDINE-1-Y) EHTYL-2-METHYL-6,7,8,9-TETRAHYDRY-4H- PYRIDO [1,2-a] PYRIMIDIN-4-ONE AND INTERMEDIATE COMPOUNDS FOR PREPARING THEREOF
PL95307200A PL181420B1 (en) 1994-02-11 1995-02-10 [d] isoxazol-3-yl) piperidin-1-yl] ethyl} -2-methyl-6,7,8,9-tetrahydro-4H-pyrido [1,2-a] pyrimidin-4-one and new compounds intermediate PL
KR1019950002516A KR100221108B1 (en) 1994-02-11 1995-02-11 3-2-[4-6--[d]-3--1-]--2--6789--4H-[12-a]-4-

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES09400252A ES2074966B1 (en) 1994-02-11 1994-02-11 PROCEDURE FOR OBTAINING 3- (2- (4- (6-FLUORO-BENZO (D) ISOXAZOL-3-IL) PIPERIDIN-1-IL) -ETIL) -2-METHYL-6,7,8,9- TETRAHIDRO-4H-PIRIDO- (1,2-A) PIRIMIDIN-4-ONA.

Publications (2)

Publication Number Publication Date
ES2074966A1 true ES2074966A1 (en) 1995-09-16
ES2074966B1 ES2074966B1 (en) 1996-06-16

Family

ID=8285178

Family Applications (1)

Application Number Title Priority Date Filing Date
ES09400252A Expired - Fee Related ES2074966B1 (en) 1994-02-11 1994-02-11 PROCEDURE FOR OBTAINING 3- (2- (4- (6-FLUORO-BENZO (D) ISOXAZOL-3-IL) PIPERIDIN-1-IL) -ETIL) -2-METHYL-6,7,8,9- TETRAHIDRO-4H-PIRIDO- (1,2-A) PIRIMIDIN-4-ONA.

Country Status (14)

Country Link
KR (1) KR100221108B1 (en)
AT (1) AT405401B (en)
CZ (1) CZ286398B6 (en)
EG (1) EG20877A (en)
ES (1) ES2074966B1 (en)
FI (1) FI110000B (en)
GR (1) GR1002344B (en)
HU (1) HU222110B1 (en)
IS (1) IS1766B (en)
NO (1) NO306022B1 (en)
PL (1) PL181420B1 (en)
PT (1) PT101654B (en)
RU (1) RU2123004C1 (en)
SK (1) SK281752B6 (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2103237A1 (en) * 1995-04-12 1997-09-01 Ferrerinternacional S A New compound derived from chromene
ES2144355A1 (en) * 1997-12-30 2000-06-01 Ferrer Int 7- not (PIPERIDIN-1-YL)- PROPOXY -CHROMEN-4-ONE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE
WO2001085731A1 (en) * 2000-05-05 2001-11-15 Rpg Life Sciences Limited A PROCESS FOR THE PREPARATION OF ANTI-PSCHOTIC 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
US7202360B2 (en) 2002-10-18 2007-04-10 Hanmi Pharm Co., Ltd. Method for preparing risperidone
US7256195B2 (en) 2000-08-14 2007-08-14 Teva Pharmaceutical Industries Ltd. Preparation of risperidone
US7405298B2 (en) 2002-11-13 2008-07-29 Synthon Ip Inc. Process for making risperidone and intermediates therefor

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2197801B1 (en) * 2002-03-05 2005-03-16 Ferrer Internacional,S.A PROCEDURE FOR OBTAINING THE 3- (2- (4- (6-FLUORO-BENZO (D) ISOXAZOL-3-IL) PIPERIDIN-1-IL) -ETIL) -2-METHYL-6,7,8,9- TETRAHIDRO-4H-PIRIDO- (1,2-A) PIRIMIDIN-4-ONA.
RU2310653C1 (en) * 2006-07-17 2007-11-20 Государственное образовательное учреждение высшего профессионального образования "Кубанский государственный технологический университет" (ГОУВПО "КубГТУ") METHOD FOR PREPARING DERIVATIVES OF 2-METHYL-5-(5-METHYL-2-FURYL)-4,10-DIHYDRO-3H-PYRIDAZINO[1,6-b]ISOQUINOLINE-10-ONE (VARIANTS)
RU2459824C2 (en) * 2007-04-19 2012-08-27 Юсинь ЛИ New compounds for mental disorders, preparing and using them

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES8506705A1 (en) * 1981-11-12 1985-08-01 Hoechst Roussel Pharma PROCEDURE FOR THE PREPARATION OF 3- (1-SUBSTITUTED-4-PIPERIDIL) -1, 2-BENZSOXAZOLES
EP0196132A2 (en) * 1985-03-27 1986-10-01 Janssen Pharmaceutica N.V. 1,2-Benzisoxazol-3-yl and 1,2-benzisothiazol-3-yl derivatives
EP0299349A2 (en) * 1987-07-13 1989-01-18 Hoechst-Roussel Pharmaceuticals Incorporated N-substituted-5,6-dimethoxy-1,2-benzisoxazole-3-propanamine and related compounds, a process for their preparation and their use as medicaments

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AT327199B (en) * 1971-10-14 1976-01-26 Sumitomo Chemical Co PROCESS FOR PRODUCING NEW NITROCHINAZOLINONES
US4485107A (en) * 1982-11-01 1984-11-27 Janssen Pharmaceutica N.V. [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES8506705A1 (en) * 1981-11-12 1985-08-01 Hoechst Roussel Pharma PROCEDURE FOR THE PREPARATION OF 3- (1-SUBSTITUTED-4-PIPERIDIL) -1, 2-BENZSOXAZOLES
EP0196132A2 (en) * 1985-03-27 1986-10-01 Janssen Pharmaceutica N.V. 1,2-Benzisoxazol-3-yl and 1,2-benzisothiazol-3-yl derivatives
EP0299349A2 (en) * 1987-07-13 1989-01-18 Hoechst-Roussel Pharmaceuticals Incorporated N-substituted-5,6-dimethoxy-1,2-benzisoxazole-3-propanamine and related compounds, a process for their preparation and their use as medicaments

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2103237A1 (en) * 1995-04-12 1997-09-01 Ferrerinternacional S A New compound derived from chromene
ES2144355A1 (en) * 1997-12-30 2000-06-01 Ferrer Int 7- not (PIPERIDIN-1-YL)- PROPOXY -CHROMEN-4-ONE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE
WO2001085731A1 (en) * 2000-05-05 2001-11-15 Rpg Life Sciences Limited A PROCESS FOR THE PREPARATION OF ANTI-PSCHOTIC 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
US7256195B2 (en) 2000-08-14 2007-08-14 Teva Pharmaceutical Industries Ltd. Preparation of risperidone
US7202360B2 (en) 2002-10-18 2007-04-10 Hanmi Pharm Co., Ltd. Method for preparing risperidone
US7405298B2 (en) 2002-11-13 2008-07-29 Synthon Ip Inc. Process for making risperidone and intermediates therefor

Also Published As

Publication number Publication date
PT101654A (en) 1995-09-12
HUT70169A (en) 1995-09-28
FI950579A0 (en) 1995-02-10
RU95101859A (en) 1997-03-20
KR100221108B1 (en) 1999-09-15
IS1766B (en) 2001-03-15
GR1002344B (en) 1996-05-24
IS4259A (en) 1995-08-12
SK281752B6 (en) 2001-07-10
SK15695A3 (en) 1995-10-11
ATA24995A (en) 1998-12-15
NO950501L (en) 1995-08-14
RU2123004C1 (en) 1998-12-10
CZ32995A3 (en) 1995-09-13
FI110000B (en) 2002-11-15
PL181420B1 (en) 2001-07-31
ES2074966B1 (en) 1996-06-16
EG20877A (en) 2000-05-31
CZ286398B6 (en) 2000-04-12
AT405401B (en) 1999-08-25
NO950501D0 (en) 1995-02-09
HU9500418D0 (en) 1995-03-28
PL307200A1 (en) 1995-08-21
HU222110B1 (en) 2003-04-28
KR950032196A (en) 1995-12-20
FI950579L (en) 1995-08-12
NO306022B1 (en) 1999-09-06
PT101654B (en) 2002-01-30

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