ES2082722A1 - Procedimiento de preparar 8-(4-(4-(pirimidina-2-il)-piperacina-1-il)-butil)-8-aza-espiro(4.5)decabi-7,9-diona y derivados, asi como los compuestos obtenidos. - Google Patents

Procedimiento de preparar 8-(4-(4-(pirimidina-2-il)-piperacina-1-il)-butil)-8-aza-espiro(4.5)decabi-7,9-diona y derivados, asi como los compuestos obtenidos.

Info

Publication number
ES2082722A1
ES2082722A1 ES09401543A ES9401543A ES2082722A1 ES 2082722 A1 ES2082722 A1 ES 2082722A1 ES 09401543 A ES09401543 A ES 09401543A ES 9401543 A ES9401543 A ES 9401543A ES 2082722 A1 ES2082722 A1 ES 2082722A1
Authority
ES
Spain
Prior art keywords
piperazin
pyrimidin
dione
butyl
azaspiro
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
ES09401543A
Other languages
English (en)
Other versions
ES2082722B1 (es
Inventor
Tibor Mezei
Gabor Blasko
Zoltan Budai
Margit Csorgo
Eva Furdyga
Imre Klebovich
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.)
Egyt Gyogyszervegyeszeti Gyar
Egis Pharmaceuticals PLC
Original Assignee
Egyt Gyogyszervegyeszeti Gyar
Egis Pharmaceuticals PLC
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 Egyt Gyogyszervegyeszeti Gyar, Egis Pharmaceuticals PLC filed Critical Egyt Gyogyszervegyeszeti Gyar
Publication of ES2082722A1 publication Critical patent/ES2082722A1/es
Application granted granted Critical
Publication of ES2082722B1 publication Critical patent/ES2082722B1/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P25/20—Hypnotics; Sedatives

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Anesthesiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

PROCEDIMIENTO DE PREPARAR 8-[4-[4-(PIRIMIDINA-2-IL)-PIPERACINA-1-IL]-BUTIL]-8-AZA-ESPIRO[4,5]DECANO-7,9-DIONA Y DERIVADOS, ASI COMO LOS COMPUESTOS OBTENIDOS. EL PROCEDIMIENTO COMPRENDE, EN PARTICULAR, A) AISLAR LA BASE DE 8-[4-[4-(PIRIMIDINA-2-IL)-PIPERACINA-1-IL]-BUTIL]-8-AZA-ESPIRO[4,5]DECANO-7,9-DIONA Y/O B) TRATAR LA BASE DE 8-[4-[4-(PIRIMIDINA-2-IL)-PIPERACINA-1-IL]-BUTIL]-8-AZA-ESPIRO[4,5]DECANO-7,9-DIONA CON CLORURO DE HIDROGENO EN ETANOL O ISOPROPANOL; O C) TRATAR LA BASE DE 8-[4-[4-(PIRIMIDINA-2-IL)-PIPERACINA-1-IL]-BUTIL]-8-AZA-ESPIRO[4,5]DECANO-7,9-DIONA CON CLORURO DE HIDROGENO EN ACETATO DE ETILO O ISOPROPANOL. APLICABLE PARA MEJORAR LA PUREZA DE LOS COMPUESTOS OBTENIDOS, ELIMINANDO ETAPAS DE PURIFICACION.
ES09401543A 1993-07-16 1994-07-15 Procedimiento de preparar 8-(4-(4-(pirimidina-2-il)-piperacina-1-il)-butil)-8-aza-espiro(4.5)decabi-7,9-diona y derivados, asi como los compuestos obtenidos. Expired - Lifetime ES2082722B1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
HU9302040A HU217129B (hu) 1993-07-16 1993-07-16 Eljárás nagy tisztaságú buspiron gyógyászati hatóanyag előállítására

Publications (2)

Publication Number Publication Date
ES2082722A1 true ES2082722A1 (es) 1996-03-16
ES2082722B1 ES2082722B1 (es) 1996-10-01

Family

ID=10983790

Family Applications (1)

Application Number Title Priority Date Filing Date
ES09401543A Expired - Lifetime ES2082722B1 (es) 1993-07-16 1994-07-15 Procedimiento de preparar 8-(4-(4-(pirimidina-2-il)-piperacina-1-il)-butil)-8-aza-espiro(4.5)decabi-7,9-diona y derivados, asi como los compuestos obtenidos.

Country Status (20)

Country Link
US (1) US5473072A (es)
EP (1) EP0634411B1 (es)
JP (1) JPH07165755A (es)
KR (1) KR950003287A (es)
AT (1) ATE180480T1 (es)
BG (1) BG98904A (es)
CA (1) CA2128164A1 (es)
CZ (1) CZ287531B6 (es)
DE (1) DE59408299D1 (es)
ES (1) ES2082722B1 (es)
FR (1) FR2709128B1 (es)
GB (1) GB2280185B (es)
HR (1) HRP940408B1 (es)
HU (1) HU217129B (es)
IT (1) IT1271677B (es)
PL (1) PL176708B1 (es)
RU (1) RU2131875C1 (es)
SK (1) SK281622B6 (es)
UA (1) UA44687C2 (es)
ZA (1) ZA945210B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2146593A1 (en) * 1994-05-05 1995-11-06 Jack Melton Large-scale process for azapirone synthesis
US20040127501A1 (en) * 2002-09-24 2004-07-01 Zhengming Chen Therapeutic agents useful for treating pain

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3713634A (en) * 1969-08-23 1973-01-30 Dravo Corp Device for sealing travelling grates
DE3806009A1 (de) * 1987-02-25 1988-09-08 Egyt Gyogyszervegyeszeti Gyar Verfahren und zwischenprodukte 8-(4'-(4''-(pyrimidin-2'''-yl)-piperazin-1''-yl)-but-2'-inyl)-8-aza-spiro(4,5)decan-7,9-dion beziehungsweise 8-(4'-(4''-(pyrimidin-2'''-yl)-piperazin-1''-yl)-but-2'-enyl)-8-aza-spiro(4,5)decan-7,9-dion zur herstellung von 8-(4'-(4''-(pyrimidin-2'''-yl)-piperazin-1''yl)-butyl)-8-aza-spiro(4,5)decan-7,9-dion, verfahren zur herstellung dieser zwischenprodukte, diese enthaltende arzneimittel und verfahren zur herstellung der ausgangsstoffe 8-aza-spiro(4,5)decan-7,9-di-(on)-8-prop-2'-in zur herstellung der letzteren
EP0304941A1 (en) * 1987-08-28 1989-03-01 Bristol-Myers Squibb Company Pharmaceutically useful polymorphic modification of buspirone
EP0304940A1 (en) * 1987-08-28 1989-03-01 Bristol-Myers Squibb Company Process for converting the lower melting polymorphic crystalline form of Buspirone hydrochloride into the higher melting form thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE759371A (fr) * 1969-11-24 1971-05-24 Bristol Myers Co Azaspirodecanediones heterocycliques et procedes pour leur preparation
JPS6310760A (ja) * 1986-07-01 1988-01-18 Sumitomo Pharmaceut Co Ltd イミド誘導体の新規製造法
JPS6310786A (ja) * 1986-07-01 1988-01-18 Sumitomo Pharmaceut Co Ltd 新規イミド誘導体およびその製造法
US5130315A (en) * 1991-01-10 1992-07-14 Raymond R. Wittekind 1-piperazinyl-2-butenes and -2-butynes

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3713634A (en) * 1969-08-23 1973-01-30 Dravo Corp Device for sealing travelling grates
DE3806009A1 (de) * 1987-02-25 1988-09-08 Egyt Gyogyszervegyeszeti Gyar Verfahren und zwischenprodukte 8-(4'-(4''-(pyrimidin-2'''-yl)-piperazin-1''-yl)-but-2'-inyl)-8-aza-spiro(4,5)decan-7,9-dion beziehungsweise 8-(4'-(4''-(pyrimidin-2'''-yl)-piperazin-1''-yl)-but-2'-enyl)-8-aza-spiro(4,5)decan-7,9-dion zur herstellung von 8-(4'-(4''-(pyrimidin-2'''-yl)-piperazin-1''yl)-butyl)-8-aza-spiro(4,5)decan-7,9-dion, verfahren zur herstellung dieser zwischenprodukte, diese enthaltende arzneimittel und verfahren zur herstellung der ausgangsstoffe 8-aza-spiro(4,5)decan-7,9-di-(on)-8-prop-2'-in zur herstellung der letzteren
EP0304941A1 (en) * 1987-08-28 1989-03-01 Bristol-Myers Squibb Company Pharmaceutically useful polymorphic modification of buspirone
EP0304940A1 (en) * 1987-08-28 1989-03-01 Bristol-Myers Squibb Company Process for converting the lower melting polymorphic crystalline form of Buspirone hydrochloride into the higher melting form thereof

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, Vol. 110, N‘ 25, 19 Junio 1989 (Columbus, Ohio, USA), pßgina 652, columna 1, resumen n‘ 231663z KOJIMA y col. "Preparation of (piperazinylbutynil)- and (piperazinylbutenyl) bicicloheptane derivates as tranquilizers" * Resumen * *
CHEMICAL ABSTRACTS, Vol. 110, N‘ 3, 16 Enero 1989 (Columbus, Ohio, USA), pßgina 557, columna 1, resumen n‘ 23914e, KOJIMA y col. "Preparation of N-(piperazinylbutyl) imide derivatives as tranquilizers and psychotropics" * Resumen * *
ISHIZUMI y col. "Synthesis and Anxiolytic Activity of N-Substituted Cyclic Imides (1R*,2S*,3R*,4S*)-N-[4-[4-(2- Pyrimidinyl)-1-piperazinyl]butyl]-2,3-bicyclo[2.2.1] heptanedicarboximide (Tandospirone) and related compounds 1,2". CHEMICAL & PHARMACEUTICAL BULLETIN, Vol. 39, N‘ 9, Septiembre 1991, pßginas 2288-2300 *
KUHNERT-BRANDST€TTE R.M. y PORSCHE, V. "Contribution to Polymorphism of Drugs 6th Communication: Bupicomide, Buspirone Hydrochloride, Heptolamide, Levobunolol Hydrochloride, Naftifine Hydrochloride and Piretanide"; SCIENTIA PHARMACEUTICA, Vol. 58, 1990, pßginas 37-53 *

Also Published As

Publication number Publication date
ZA945210B (en) 1996-01-15
RU94026281A (ru) 1996-05-27
IT1271677B (it) 1997-06-04
HU9302040D0 (en) 1993-10-28
GB9414325D0 (en) 1994-09-07
GB2280185B (en) 1997-04-16
US5473072A (en) 1995-12-05
FR2709128B1 (fr) 1996-02-23
HRP940408A2 (en) 1996-10-31
ITMI941492A1 (it) 1996-01-18
SK281622B6 (sk) 2001-05-10
BG98904A (bg) 1995-05-31
EP0634411B1 (de) 1999-05-26
ITMI941492A0 (it) 1994-07-18
RU2131875C1 (ru) 1999-06-20
HU217129B (hu) 1999-11-29
HRP940408B1 (en) 2000-02-29
CA2128164A1 (en) 1995-01-17
SK86194A3 (en) 1995-03-08
JPH07165755A (ja) 1995-06-27
CZ287531B6 (en) 2000-12-13
PL176708B1 (pl) 1999-07-30
UA44687C2 (uk) 2002-03-15
HUT69720A (en) 1995-09-28
PL304313A1 (en) 1995-01-23
CZ170994A3 (en) 1995-04-12
KR950003287A (ko) 1995-02-16
GB2280185A (en) 1995-01-25
FR2709128A1 (fr) 1995-02-24
DE59408299D1 (de) 1999-07-01
EP0634411A1 (de) 1995-01-18
ES2082722B1 (es) 1996-10-01
ATE180480T1 (de) 1999-06-15

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