ES2050069A1 - Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona. - Google Patents

Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona.

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Publication number
ES2050069A1
ES2050069A1 ES9201424A ES9201424A ES2050069A1 ES 2050069 A1 ES2050069 A1 ES 2050069A1 ES 9201424 A ES9201424 A ES 9201424A ES 9201424 A ES9201424 A ES 9201424A ES 2050069 A1 ES2050069 A1 ES 2050069A1
Authority
ES
Spain
Prior art keywords
methyl
pyrido
pyrimidin
ethyl
benzisoxazol
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
ES9201424A
Other languages
English (en)
Other versions
ES2050069B1 (es
Inventor
Olondriz Francisco Marquillas
Rovira Anna Bosch
Barjoan Pere Dalmases
Ges Jose Maria 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 ES9201424A priority Critical patent/ES2050069B1/es
Publication of ES2050069A1 publication Critical patent/ES2050069A1/es
Application granted granted Critical
Publication of ES2050069B1 publication Critical patent/ES2050069B1/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Abstract

PROCEDIMIENTO PARA LA OBTENCION DE 3-[2- [4-(6-FLUORO-1, 2-BENZISOXAZOL-3-IL) PIPERIDI-NO] ETIL] -2-6,7,8,9-TETRAHIDRO-4H-PIRIDO [1,2-A] PIRIMIDIN-4-ONA. EL PROCEDIMIENTO CONSISTE EN HACER REACCIONAR UN COMPUESTO DE FORMULA Z-CHSI2 SC CHBS2 SC-L, DONDE Z ES EL RADICAL 2-METIL-4-OXO-6,7,8,9-TETRAHIDRO-4H-PIRIDO [1,2-ALPIRIMIDIN-3-ILO Y L UN GRUPO SALIENTE COMO HALOGENO O UN ALQUIL O ARILSULFONILO, CON LA 4-(2,4-DIFLUOROBENZOIL) PIPERIDINA, PARA DAR LA 3-[2- [(2,4-DIFLUOROBENZOIL) PIPERIDINI] ETIL]-2-METIL-6,7,8,9-TETRAHIDRO-4H-PIRIDO- [1,2-A] PIRIMIDIN-4-ONA, QUE POR REACCION CON HIDROCLORURO DE HIDROXILAMINA DA LA CORRESPONDIENTE OXIMA 3-[2- [4-(2, 4-DIFLORUOFENIL)-1-(HIDROXIMINO) METIL] PIPERIDINI] ETIL]-2-METIL-6,7,8,9-TETRAHIDRO-4H-PIRIDO [1,2-A] PIRIMIDIN-4-ONA, LA CUAL SECICLA EN CONDICIONES BASICAS A LA 3-[2-[4- (6-FLUORO-1, 2-BENZISOXAZOL-3-IL) PIPERIDINO) ETIL]-2-METIL-6,7,8,9-TETRAHIDRO-4H-PIRIDO [1, 2-A] PIRIMIDIN-4-ONA. SE OBTIENE EL COMPUESTO 3-[2- [4- (6-FLUORO-1, 2-PIRIDO [1,2-A] PIRIMIDIN-4-ONA, DE FORMULA I. DICHO COMPUESTO TIENE APLICACIONES FARMACEUTICAS POR SUS PROPIEDADES ANTISICOTICAS.
ES9201424A 1992-07-10 1992-07-10 Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona. Expired - Lifetime ES2050069B1 (es)

Priority Applications (1)

Application Number Priority Date Filing Date Title
ES9201424A ES2050069B1 (es) 1992-07-10 1992-07-10 Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)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
ES9201424A ES2050069B1 (es) 1992-07-10 1992-07-10 Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona.

Publications (2)

Publication Number Publication Date
ES2050069A1 true ES2050069A1 (es) 1994-05-01
ES2050069B1 ES2050069B1 (es) 1994-12-16

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
ES9201424A Expired - Lifetime ES2050069B1 (es) 1992-07-10 1992-07-10 Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona.

Country Status (1)

Country Link
ES (1) ES2050069B1 (es)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2004009591A1 (en) * 2002-07-22 2004-01-29 Aurobindo Pharma Ltd. A process for the preparation of antipsychotic risperidone
WO2004035573A1 (en) * 2002-10-18 2004-04-29 Hanmi Pharm. Co., Ltd. Method for preparing risperidone
WO2004020439A3 (en) * 2002-08-30 2004-07-01 Sunil Sadanand Nadkarni Improved process for preparation of risperidone
WO2006005974A1 (en) * 2004-07-08 2006-01-19 Richter Gedeon Vegyészeti Gyár Rt. A process for the preparation of risperidone
WO2006046082A1 (en) * 2004-10-25 2006-05-04 Richter Gedeon Vegyészeti Gyár Rt. A process for the preparation of risperidone
US7256195B2 (en) 2000-08-14 2007-08-14 Teva Pharmaceutical Industries Ltd. Preparation of risperidone
CN100390146C (zh) * 2002-11-13 2008-05-28 斯索恩有限公司 制备利培酮的方法和用于该方法的中间体
CN115057809A (zh) * 2022-07-15 2022-09-16 扬州市普林斯医药科技有限公司 一种4-(2,4-二氟苯甲酰基)-哌啶的制备方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050232995A1 (en) 2002-07-29 2005-10-20 Yam Nyomi V Methods and dosage forms for controlled delivery of paliperidone and risperidone

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0110435A1 (en) * 1982-11-01 1984-06-13 Janssen Pharmaceutica N.V. Novel ((bis(aryl)methylene)-1-piperidinyl)alkyl-pyrimidinones
ES8705881A1 (es) * 1985-03-27 1987-05-16 Janssen Pharmaceutica Nv Un procedimiento para la preparacion de 1-2-benzazoles
EP0368388A2 (en) * 1988-11-07 1990-05-16 Janssen Pharmaceutica N.V. 3-Piperidinyl-1,2-benzisoxazoles
EP0453042A1 (en) * 1990-04-19 1991-10-23 Janssen Pharmaceutica N.V. Novel 2,9-disubstituted-4H-pyrido-[1,2-a]pyrimidin-4-ones

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0110435A1 (en) * 1982-11-01 1984-06-13 Janssen Pharmaceutica N.V. Novel ((bis(aryl)methylene)-1-piperidinyl)alkyl-pyrimidinones
ES8705881A1 (es) * 1985-03-27 1987-05-16 Janssen Pharmaceutica Nv Un procedimiento para la preparacion de 1-2-benzazoles
EP0368388A2 (en) * 1988-11-07 1990-05-16 Janssen Pharmaceutica N.V. 3-Piperidinyl-1,2-benzisoxazoles
EP0453042A1 (en) * 1990-04-19 1991-10-23 Janssen Pharmaceutica N.V. Novel 2,9-disubstituted-4H-pyrido-[1,2-a]pyrimidin-4-ones

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2004009591A1 (en) * 2002-07-22 2004-01-29 Aurobindo Pharma Ltd. A process for the preparation of antipsychotic risperidone
WO2004020439A3 (en) * 2002-08-30 2004-07-01 Sunil Sadanand Nadkarni Improved process for preparation of risperidone
US7202360B2 (en) 2002-10-18 2007-04-10 Hanmi Pharm Co., Ltd. Method for preparing risperidone
WO2004035573A1 (en) * 2002-10-18 2004-04-29 Hanmi Pharm. Co., Ltd. Method for preparing risperidone
CN100390146C (zh) * 2002-11-13 2008-05-28 斯索恩有限公司 制备利培酮的方法和用于该方法的中间体
US7405298B2 (en) 2002-11-13 2008-07-29 Synthon Ip Inc. Process for making risperidone and intermediates therefor
WO2006005974A1 (en) * 2004-07-08 2006-01-19 Richter Gedeon Vegyészeti Gyár Rt. A process for the preparation of risperidone
EA011748B1 (ru) * 2004-07-08 2009-06-30 Рихтер Гедеон Ведьесети Дьяр Рт. Способ получения рисперидона
WO2006046082A1 (en) * 2004-10-25 2006-05-04 Richter Gedeon Vegyészeti Gyár Rt. A process for the preparation of risperidone
CN115057809A (zh) * 2022-07-15 2022-09-16 扬州市普林斯医药科技有限公司 一种4-(2,4-二氟苯甲酰基)-哌啶的制备方法
CN115057809B (zh) * 2022-07-15 2024-02-13 扬州市普林斯医药科技有限公司 一种4-(2,4-二氟苯甲酰基)-哌啶的制备方法

Also Published As

Publication number Publication date
ES2050069B1 (es) 1994-12-16

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