AR016818A1 - Proceso para preparar un compuesto polimorfo estable de 10,10-bis((2-fluor 4-piridinil)metil)-9(10h)-antracenona cristalina, y la mezcla de compuestosiniciales de la etapa (1) y el compuesto de la etapa (2); dicho compuesto polimorfo de forma 2, composicion farmaceutica que lo contiene y metodo detr - Google Patents

Proceso para preparar un compuesto polimorfo estable de 10,10-bis((2-fluor 4-piridinil)metil)-9(10h)-antracenona cristalina, y la mezcla de compuestosiniciales de la etapa (1) y el compuesto de la etapa (2); dicho compuesto polimorfo de forma 2, composicion farmaceutica que lo contiene y metodo detr

Info

Publication number
AR016818A1
AR016818A1 ARP980104034A ARP980104034A AR016818A1 AR 016818 A1 AR016818 A1 AR 016818A1 AR P980104034 A ARP980104034 A AR P980104034A AR P980104034 A ARP980104034 A AR P980104034A AR 016818 A1 AR016818 A1 AR 016818A1
Authority
AR
Argentina
Prior art keywords
compound
formula
composite
contacting
stage
Prior art date
Application number
ARP980104034A
Other languages
English (en)
Original Assignee
Du Pont Pharm Co
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 Du Pont Pharm Co filed Critical Du Pont Pharm Co
Publication of AR016818A1 publication Critical patent/AR016818A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61—Halogen atoms or nitro radicals
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/26—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Un proceso para preparar un compuesto polimorfo estable de 10,10-bis ((2-fluor 4-piridinil)metil)-9(10h)-antracenona cristalina, de formula (I) quecomprende las etapas de: (1) poner en contacto por un tiempo suficiente a una temperatura adecuada un compuesto de la formula (II) en acetonitrilo conalrededor de un equivalente de un agente de halogenacion adecuado en presencia de un radical iniciador adecuado, para formar una mezcla de compuestos de lasformulas (II), (III) y (IV) donde Z es un cloroo bromo. (2) poner en contacto la mezcla de los compuestos (II), (III) y (IV) de la Etapa (1) con agua quecontenga, por lo menos, un equivalente de una base adecuada para formar un compuesto de la formula (V); (3) extraer la solucion de la Etapa 2 con un solventede extraccion adecuado para eliminar los compuestos de las formulas (II) y (IV); (4) extraer la solucion acuosa resultante de la Etapa (3) con un solventeorgánica polar para eliminar el compuesto (V); (5) poner en contacto un compuestode la formula (V) con un agente de sulfonilacion adecuado en presencia de undepurador de ácidos adecuados para obtener el compuesto de la formula (VI) donde -OA es un éster de sulfonato; (6) poner en contacto un compuesto de formula(VI) con una sal de iodo adecuada en un solvente de reaccion adecuado para obtener un compuesto de la formula (VII); y (7) poner en contacto un compuesto de laformula (VIII) en presencia de una base fuerte adecuada con un compuesto de la formula (VII) para obtener uncompuesto de la formula (I). La enfermedad deAlzheimer se manifiesta por una significativa destruccion de la memoria y una creciente confusion mental a medida que se pierden las células nerviosas delcerebro. El envejecimiento general de la poblacionen los proximos anos aumentará la frecuencia de la enfermedad y resulta imperioso dar respuesta a esteproblema antes de que se convierta en una epidemia. La investigacion ha llevado a examinar una gran variedad de estrategias de medicacion con poco éxito. Lasprimeras estrategias terapéuticas incluyen aquellas que se basan en el incremento del flujo sanguíneo cerebral o poseen efectos psicoestimulantes. Entre ellas
ARP980104034A 1997-08-14 1998-08-14 Proceso para preparar un compuesto polimorfo estable de 10,10-bis((2-fluor 4-piridinil)metil)-9(10h)-antracenona cristalina, y la mezcla de compuestosiniciales de la etapa (1) y el compuesto de la etapa (2); dicho compuesto polimorfo de forma 2, composicion farmaceutica que lo contiene y metodo detr AR016818A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8022397P 1997-08-14 1997-08-14
US7739598P 1998-03-10 1998-03-10

Publications (1)

Publication Number Publication Date
AR016818A1 true AR016818A1 (es) 2001-08-01

Family

ID=26759225

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980104034A AR016818A1 (es) 1997-08-14 1998-08-14 Proceso para preparar un compuesto polimorfo estable de 10,10-bis((2-fluor 4-piridinil)metil)-9(10h)-antracenona cristalina, y la mezcla de compuestosiniciales de la etapa (1) y el compuesto de la etapa (2); dicho compuesto polimorfo de forma 2, composicion farmaceutica que lo contiene y metodo detr

Country Status (16)

Country Link
US (1) US6214847B1 (es)
EP (1) EP1003722A1 (es)
JP (1) JP2001515067A (es)
KR (1) KR20010022834A (es)
CN (1) CN1268121A (es)
AR (1) AR016818A1 (es)
AU (1) AU8777498A (es)
CA (1) CA2301074A1 (es)
EE (1) EE200000071A (es)
HR (1) HRP980429A2 (es)
HU (1) HUP0003433A2 (es)
IL (1) IL133953A0 (es)
NO (1) NO20000676L (es)
PL (1) PL338706A1 (es)
SK (1) SK1582000A3 (es)
WO (1) WO1999009010A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100509740C (zh) * 2006-06-06 2009-07-08 中国科学院广州化学研究所 10,10-二苄基蒽酮及其衍生物和合成方法
CN105343021A (zh) * 2015-11-10 2016-02-24 石家庄市华新药业有限责任公司 一种瑞格列奈片剂及其制备方法
CN105254592A (zh) * 2015-11-10 2016-01-20 石家庄市华新药业有限责任公司 一种瑞格列奈化合物及其制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2823414B2 (ja) 1992-02-26 1998-11-11 セントラル硝子株式会社 ２−クロロ−メチルピリジン類の側鎖塩素化法
US5296478A (en) 1992-10-07 1994-03-22 The Dupont Merck Pharmaceutical Co. 1-substituted oxindoles as cognition enhancers
US5594001A (en) * 1993-04-08 1997-01-14 The Dupont Merck Pharmaceutical Company Polycyclic systems, and derivatives thereof, as neurotransmitter release enhancers useful in the treatment of cognitive disorders
CA2184812C (en) * 1994-03-09 1999-12-28 Ronald L. Ream Method and apparatus for forming miniature size confectionery products

Also Published As

Publication number Publication date
NO20000676L (no) 2000-03-28
CN1268121A (zh) 2000-09-27
AU8777498A (en) 1999-03-08
US6214847B1 (en) 2001-04-10
EP1003722A1 (en) 2000-05-31
JP2001515067A (ja) 2001-09-18
SK1582000A3 (en) 2000-09-12
NO20000676D0 (no) 2000-02-10
WO1999009010A1 (en) 1999-02-25
CA2301074A1 (en) 1999-02-25
KR20010022834A (ko) 2001-03-26
PL338706A1 (en) 2000-11-20
IL133953A0 (en) 2001-04-30
HRP980429A2 (en) 1999-06-30
EE200000071A (et) 2000-10-16
HUP0003433A2 (hu) 2001-01-29

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