ES2074966B1 - 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. - Google Patents

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.

Info

Publication number
ES2074966B1
ES2074966B1 ES09400252A ES9400252A ES2074966B1 ES 2074966 B1 ES2074966 B1 ES 2074966B1 ES 09400252 A ES09400252 A ES 09400252A ES 9400252 A ES9400252 A ES 9400252A ES 2074966 B1 ES2074966 B1 ES 2074966B1
Authority
ES
Spain
Prior art keywords
pirido
pirimidin
ona
methyl
isoxazol
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
ES09400252A
Other languages
Spanish (es)
Other versions
ES2074966A1 (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 NO950501A priority patent/NO306022B1/en
Priority to PT101654A priority patent/PT101654B/en
Priority to EG11595A priority patent/EG20877A/en
Priority to PL95307200A priority patent/PL181420B1/en
Priority to HU9500418A priority patent/HU222110B1/en
Priority to FI950579A priority patent/FI110000B/en
Priority to AT0024995A priority patent/AT405401B/en
Priority to RU95101859/04A priority patent/RU2123004C1/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] -ETILL-2-METHYL-6,7,8,9-TETRAHYDRO -4H-PIRIDO [1,2, -A] -PIRIMIDIN-4-ONA. THE PROCEDURE CONSISTS OF REACTIONING 3- (2-AMINOETHYL) -2-METHYL-6,7,8,9-TETRAHYDRO-4H-PIRIDO [1,2-A] PIRIMIDIN-4-ONA, OF FORMULA II, WITH COMPOUNDS OF GENERAL FORMULA III, WHERE "Y" AND "Z" ARE OUTGOING, EQUAL OR DIFFERENT GROUPS, SUCH AS HALOGEN OR A RENT OR ARILSULFONILOXI GROUP, IN THE PRESENCE OF A SUITABLE SOLVENT AND BASE, TO PROVIDE 3-2 - [4-6-FLUORO-BENZO [D] ISOXAZOL-3-IL) -PIPERIDIN-1-IL] ETIL-2-METHYL-6,7,8,9-TETRAHIDRO-4H-PIRIDO [L, 2-A ] PIRIMIDIN-4-ONA OF GENERAL FORMULA I. SUCH 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 for preparation of 3-{2-[4-(6-fluorine-benzo [d] isoxasol-3-yl)piperidine-1-yl]ethyl}-2-methyl-6,7,8,9- tetrahydro-4h-pyridol[1,2-a]pyrimidin-4-one and intermediates 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
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
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
PL95307200A PL181420B1 (en) 1994-02-11 1995-02-10 Method of obtaining 3-[2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4h-pyridil[1,2-a]pyrimidin-4-one and intermediate compounds
HU9500418A HU222110B1 (en) 1994-02-11 1995-02-10 Process for producing 3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)piperidine-1-il]-ethyl}-2-methyl-6,7,8,9-tetrahydro-4h-pyrido[1,2-a]pyrimidine-4-one and intermediates
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
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
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
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 ES2074966A1 (en) 1995-09-16
ES2074966B1 true 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)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2101646B1 (en) * 1995-04-12 1998-04-01 Ferrer Int NEW COMPOUND DERIVED FROM CHROMENE.
ES2144355B1 (en) * 1997-12-30 2001-01-01 Ferrer Int COMPOUNDS DERIVED FROM THE CHROME.
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
WO2002014286A1 (en) 2000-08-14 2002-02-21 Teva Pharmaceutical Industries Ltd. Preparation of risperidone
KR20040034996A (en) 2002-10-18 2004-04-29 한미약품 주식회사 Improved method for the preparation of risperidone
EP1560814A1 (en) 2002-11-13 2005-08-10 Synthon B.V. Process for making risperidone and intermediates therefor
BRPI0809837A2 (en) * 2007-04-19 2014-11-11 Youxin Li "COMPOSITION FOR TREATING MENTAL DISORDERS, BALANCE OF COMPOSITE FOR TREATING MENTAL DISORDERS, PHARMACEUTICAL COMPOSITION AND USE OF COMPOSITE FOR TREATING MENTAL DISORDERS"

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4352811A (en) * 1981-11-12 1982-10-05 Hoechst-Roussel Pharmaceuticals Inc. 3-(1-Substituted-4-piperidyl)-1,2-benzisoxazoles
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
US4980365A (en) * 1987-07-13 1990-12-25 Hoechst-Roussel Pharmaceuticals Inc. N-substituted-5,6-dimethoxy-1,2-benzisoxazole-3-propanamine and related compounds as analgesic and hypotensive agents

Also Published As

Publication number Publication date
FI110000B (en) 2002-11-15
NO950501L (en) 1995-08-14
AT405401B (en) 1999-08-25
NO306022B1 (en) 1999-09-06
RU95101859A (en) 1997-03-20
IS1766B (en) 2001-03-15
KR950032196A (en) 1995-12-20
SK15695A3 (en) 1995-10-11
PL181420B1 (en) 2001-07-31
IS4259A (en) 1995-08-12
NO950501D0 (en) 1995-02-09
CZ32995A3 (en) 1995-09-13
HU222110B1 (en) 2003-04-28
ATA24995A (en) 1998-12-15
KR100221108B1 (en) 1999-09-15
CZ286398B6 (en) 2000-04-12
ES2074966A1 (en) 1995-09-16
EG20877A (en) 2000-05-31
HU9500418D0 (en) 1995-03-28
FI950579A0 (en) 1995-02-10
SK281752B6 (en) 2001-07-10
GR1002344B (en) 1996-05-24
PL307200A1 (en) 1995-08-21
PT101654B (en) 2002-01-30
PT101654A (en) 1995-09-12
RU2123004C1 (en) 1998-12-10
HUT70169A (en) 1995-09-28
FI950579A (en) 1995-08-12

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