AR033262A1 - Procedimiento para la preparacion de 2-[5-(4-fluorofenil)-3-piridilmetilaminometil]-cromano - Google Patents

Procedimiento para la preparacion de 2-[5-(4-fluorofenil)-3-piridilmetilaminometil]-cromano

Info

Publication number
AR033262A1
AR033262A1 ARP020101480A ARP020101480A AR033262A1 AR 033262 A1 AR033262 A1 AR 033262A1 AR P020101480 A ARP020101480 A AR P020101480A AR P020101480 A ARP020101480 A AR P020101480A AR 033262 A1 AR033262 A1 AR 033262A1
Authority
AR
Argentina
Prior art keywords
formula
salts
procedure
fluorophenyl
pyridylmethylaminomethyl
Prior art date
Application number
ARP020101480A
Other languages
English (en)
Inventor
Heinz Bokel
Neuenfeld Steffen Dr
Elke Simon
Udo Helm
Helmut Reubold
Ludwig Gantzert
Ralf Knierieme
Devant Ralf Dr
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR033262A1 publication Critical patent/AR033262A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Se describe un procedimiento para la preparacion de 2-[5-(4-fluorofenil)-3-piridilmetilaminometil]cromano de formula (1) de sus enantiomeros y de sus sales, caracterizado porque (1) se hace reaccionar el 5-(4-fluorofenil)piridin-3-carbaldehido de formula (2) directamente con 2-aminometilcromano o sus sales en condiciones reductivas para obtener el compuesto de formula (1), y (2) si se desea, se transforma el compuesto resultante de formula (1) en una de sus sales aceptables desde el punto de vista fisiologico por tratamiento con un ácido. La ventaja del procedimiento frente al procedimiento descripto en la patente estadounidense 5767132 radica en la disminucion del producto secundario debido a la supresion de la doble alquilacion. Al optar este procedimiento se obtiene un ingrediente activo que no contiene producto secundario con dos radicales de arilpiridina, lo cual facilita la purificacion del ingrediente activo. Además, frente a las aminaciones reductivas que se producen en condiciones estándar el procedimiento mencionado más arriba presenta la ventaja de necesitar de una menor cantidad de reactivos y una menor carga térmica. Esto, a su vez, implica una menor cantidad de impurezas y de reacciones secundarias. El 2-[5-(4-fluorofenil)-3-piridilmetilaminometil]cromano de formula (1) y sus sales son antagonistas selectivos del receptor para dopamina D2 y agonistas del receptor para 5-HT1A.
ARP020101480A 2001-04-26 2002-04-24 Procedimiento para la preparacion de 2-[5-(4-fluorofenil)-3-piridilmetilaminometil]-cromano AR033262A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10120619A DE10120619A1 (de) 2001-04-26 2001-04-26 2-(5-(4-Fluorphenyl)-3-pyridylmethylaminomethyl-chroman

Publications (1)

Publication Number Publication Date
AR033262A1 true AR033262A1 (es) 2003-12-10

Family

ID=7682908

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020101480A AR033262A1 (es) 2001-04-26 2002-04-24 Procedimiento para la preparacion de 2-[5-(4-fluorofenil)-3-piridilmetilaminometil]-cromano

Country Status (24)

Country Link
US (1) US7045629B2 (es)
EP (1) EP1383763B1 (es)
JP (1) JP2004526797A (es)
KR (1) KR100839168B1 (es)
CN (1) CN100430391C (es)
AR (1) AR033262A1 (es)
AT (1) ATE306485T1 (es)
AU (1) AU2002257763B2 (es)
BR (1) BR0209179A (es)
CA (1) CA2445207C (es)
CZ (1) CZ301615B6 (es)
DE (2) DE10120619A1 (es)
DK (1) DK1383763T3 (es)
ES (1) ES2250647T3 (es)
HK (1) HK1077302A1 (es)
HU (1) HU229151B1 (es)
MX (1) MXPA03009684A (es)
MY (1) MY130616A (es)
PL (1) PL208705B1 (es)
RU (1) RU2288229C2 (es)
SI (1) SI1383763T1 (es)
SK (1) SK287477B6 (es)
WO (1) WO2002088117A2 (es)
ZA (1) ZA200309164B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4896518B2 (ja) * 2002-12-13 2012-03-14 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド ニコチンアミド系キナーゼ阻害薬
JP2008530229A (ja) * 2005-02-17 2008-08-07 ワイス シクロアルキル縮合インドール、ベンゾチオフェン、ベンゾフランおよびインデン誘導体
RU2007139541A (ru) * 2005-04-22 2009-05-27 Вайет (Us) Производные хромана и хромена и их применение
JP5139275B2 (ja) * 2005-06-21 2013-02-06 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング （ｒ）−（−）−２−［５−（４−フルオロフェニル）−３−ピリジルメチルアミノメチル］クロマンを含有する固体医薬組成物
RU2450006C2 (ru) * 2006-04-18 2012-05-10 Эбботт Лэборетриз Антагонисты ванилоидного рецептора подтипа 1(vr1) и их применение
ES2574179T3 (es) * 2010-07-20 2016-06-15 Glaxo Group Limited Procedimiento para preparar derivados de pirano-[2,3-c]piridina

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4135474A1 (de) * 1991-10-28 1993-04-29 Bayer Ag 2-aminomethyl-chromane
FR2701479B1 (fr) * 1993-02-11 1995-05-12 Pf Medicament Nouveaux dérivés hétérocycliques de l'aminométhyl-4 pipéridine, leur préparation et leur application en thérapeutique.
CN1052006C (zh) * 1993-08-19 2000-05-03 詹森药业有限公司 血管收缩剂二氢苯并吡喃衍生物,制备方法和用途
GB9318431D0 (en) * 1993-09-06 1993-10-20 Boots Co Plc Therapeutic agents
SI0707007T1 (en) * 1994-10-14 2002-04-30 Merck Patent Gmbh (R)-(-)-2-(5-(4-fluorophenyl)-3-pyridylmethylaminomethyl)chromane as CNS active agent
DE10005150A1 (de) * 2000-02-07 2001-08-09 Merck Patent Gmbh Verfahren zur Herstellung von 5-Arylnicotinaldehyden

Also Published As

Publication number Publication date
EP1383763A2 (de) 2004-01-28
SI1383763T1 (sl) 2006-04-30
HU229151B1 (hu) 2013-09-30
AU2002257763B2 (en) 2007-03-15
WO2002088117A3 (de) 2002-12-27
ZA200309164B (en) 2004-09-29
WO2002088117A2 (de) 2002-11-07
CA2445207C (en) 2010-03-02
CZ20033214A3 (cs) 2004-02-18
KR100839168B1 (ko) 2008-06-17
KR20040010616A (ko) 2004-01-31
MY130616A (en) 2007-07-31
JP2004526797A (ja) 2004-09-02
DE10120619A1 (de) 2002-10-31
HK1077302A1 (en) 2006-02-10
US20040138266A1 (en) 2004-07-15
ES2250647T3 (es) 2006-04-16
HUP0303969A3 (en) 2011-02-28
PL208705B1 (pl) 2011-05-31
MXPA03009684A (es) 2004-02-12
CZ301615B6 (cs) 2010-05-05
ATE306485T1 (de) 2005-10-15
BR0209179A (pt) 2004-08-03
US7045629B2 (en) 2006-05-16
HUP0303969A2 (hu) 2004-04-28
RU2288229C2 (ru) 2006-11-27
RU2003132433A (ru) 2005-04-20
CN1622944A (zh) 2005-06-01
EP1383763B1 (de) 2005-10-12
CN100430391C (zh) 2008-11-05
SK14332003A3 (sk) 2004-04-06
SK287477B6 (sk) 2010-11-08
CA2445207A1 (en) 2002-11-07
DK1383763T3 (da) 2006-02-06
PL363281A1 (en) 2004-11-15
DE50204535D1 (de) 2006-02-23

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