ES2074966A1 - 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 - Google Patents
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-oneInfo
- 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
- tetrahydro
- pyrimidine
- methyl
- isoxazol
- pyrido
- 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
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
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 The process comprises reacting 3-(2-aminoethyl)-2-methyl- 6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-4-one of formula II with compounds of general formula III where Y and Z are projecting groups which may be the same or different such as halogen or an alkyl or aryl sulphonyloxy group in the presence of an appropriate solvent and base to provide 3-2-[4-6-fluoro- benzo[d]isoxazol-3-yl)piperidin-I-yl]-ethyl-2-methyl- 6,7,8,9-tetrahydro-4Hpyrido [1,2-a] pyrimidine-4-one of general formula I. The said compound has pharmaceutical applications on account of its antipsychotic properties. Products of formulae II and III which are necessary for the performance of this invention are also claimed.
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 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)
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 (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5315336B2 (en) * | 2007-04-19 | 2013-10-16 | 又欣 李 | Novel compounds for the treatment of psychiatric disorders and their preparation and use |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES8506705A1 (en) * | 1981-11-12 | 1985-08-01 | Hoechst Roussel Pharma | 3-(1-Substituted-4-piperidyl)-1,2-benzisoxazoles, a process for the preparation thereof, a pharmaceutical composition comprising the same, and their use as medicaments. |
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 |
-
1994
- 1994-02-11 ES ES09400252A patent/ES2074966B1/en not_active Expired - Fee Related
-
1995
- 1995-02-01 GR GR950100035A patent/GR1002344B/en not_active IP Right Cessation
- 1995-02-07 SK SK156-95A patent/SK281752B6/en not_active IP Right Cessation
- 1995-02-08 IS IS4259A patent/IS1766B/en unknown
- 1995-02-08 CZ CZ1995329A patent/CZ286398B6/en not_active IP Right Cessation
- 1995-02-09 EG EG11595A patent/EG20877A/en active
- 1995-02-09 NO NO950501A patent/NO306022B1/en not_active IP Right Cessation
- 1995-02-09 PT PT101654A patent/PT101654B/en active IP Right Grant
- 1995-02-10 RU RU95101859/04A patent/RU2123004C1/en not_active IP Right Cessation
- 1995-02-10 AT AT0024995A patent/AT405401B/en not_active IP Right Cessation
- 1995-02-10 HU HU9500418A patent/HU222110B1/en not_active IP Right Cessation
- 1995-02-10 PL PL95307200A patent/PL181420B1/en not_active IP Right Cessation
- 1995-02-10 FI FI950579A patent/FI110000B/en not_active IP Right Cessation
- 1995-02-11 KR KR1019950002516A patent/KR100221108B1/en not_active IP Right Cessation
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES8506705A1 (en) * | 1981-11-12 | 1985-08-01 | Hoechst Roussel Pharma | 3-(1-Substituted-4-piperidyl)-1,2-benzisoxazoles, a process for the preparation thereof, a pharmaceutical composition comprising the same, and their use as medicaments. |
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)
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 |
---|---|
FI950579A0 (en) | 1995-02-10 |
RU95101859A (en) | 1997-03-20 |
HU9500418D0 (en) | 1995-03-28 |
NO950501D0 (en) | 1995-02-09 |
SK15695A3 (en) | 1995-10-11 |
KR100221108B1 (en) | 1999-09-15 |
PT101654A (en) | 1995-09-12 |
PL307200A1 (en) | 1995-08-21 |
CZ32995A3 (en) | 1995-09-13 |
ATA24995A (en) | 1998-12-15 |
SK281752B6 (en) | 2001-07-10 |
EG20877A (en) | 2000-05-31 |
ES2074966B1 (en) | 1996-06-16 |
NO950501L (en) | 1995-08-14 |
HUT70169A (en) | 1995-09-28 |
AT405401B (en) | 1999-08-25 |
CZ286398B6 (en) | 2000-04-12 |
RU2123004C1 (en) | 1998-12-10 |
PL181420B1 (en) | 2001-07-31 |
KR950032196A (en) | 1995-12-20 |
GR1002344B (en) | 1996-05-24 |
HU222110B1 (en) | 2003-04-28 |
NO306022B1 (en) | 1999-09-06 |
FI950579A (en) | 1995-08-12 |
IS1766B (en) | 2001-03-15 |
FI110000B (en) | 2002-11-15 |
IS4259A (en) | 1995-08-12 |
PT101654B (en) | 2002-01-30 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
GC2A | Exploitation certificate registered application with search report |
Effective date: 20030305 |
|
FD2A | Announcement of lapse in spain |
Effective date: 20141120 |