ES2188222T3 - Sintesis enantioselectiva. - Google Patents

Sintesis enantioselectiva.

Info

Publication number
ES2188222T3
ES2188222T3 ES99940813T ES99940813T ES2188222T3 ES 2188222 T3 ES2188222 T3 ES 2188222T3 ES 99940813 T ES99940813 T ES 99940813T ES 99940813 T ES99940813 T ES 99940813T ES 2188222 T3 ES2188222 T3 ES 2188222T3
Authority
ES
Spain
Prior art keywords
enantioselective synthesis
xiv
formula
pharmaceutically acceptable
acceptable salt
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.)
Expired - Lifetime
Application number
ES99940813T
Other languages
English (en)
Inventor
Richard W Draper
Radha V Iyer
Yuelie Lu
Eugene J Vater
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.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Application granted granted Critical
Publication of ES2188222T3 publication Critical patent/ES2188222T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • C07D311/26—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • 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
    • C07D311/60—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with aryl radicals attached in position 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Endocrinology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyrane Compounds (AREA)
  • Catalysts (AREA)
  • Steroid Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Un procedimiento de hacer reaccionar el compuesto de fórmula IV con el compuesto representado por la fórmula VII para producir el compuesto de fórmula IX, caracterizado porque el compuesto de fórmula IV se hace reaccionar con el compuesto representado por la fórmula VII **(Fórmula)** en presencia de piperidina, una base de amina orgánica impedida y un alcanol de C3-C6 a temperatura y durante un tiempo suficiente para producir el compuesto de fórmula IX químicamente puro y libre del isómero cis del compuesto de fórmula IX y libre de las chalconas E y Z de fórmula VIII, en el que HPG es un grupo protector de hidroxilo fenólico lábil frente a ácidos: **(Fórmula)**
ES99940813T 1998-08-14 1999-08-12 Sintesis enantioselectiva. Expired - Lifetime ES2188222T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13421698A 1998-08-14 1998-08-14

Publications (1)

Publication Number Publication Date
ES2188222T3 true ES2188222T3 (es) 2003-06-16

Family

ID=22462296

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99940813T Expired - Lifetime ES2188222T3 (es) 1998-08-14 1999-08-12 Sintesis enantioselectiva.

Country Status (10)

Country Link
EP (1) EP1104414B1 (es)
JP (2) JP3684332B2 (es)
CN (1) CN1146554C (es)
AT (1) ATE232525T1 (es)
AU (1) AU5459399A (es)
CA (1) CA2340343C (es)
DE (1) DE69905376T2 (es)
ES (1) ES2188222T3 (es)
WO (1) WO2000009493A1 (es)
ZA (1) ZA200100875B (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112012031464A2 (pt) 2010-06-10 2020-08-04 Aragon Pharmaceuticals, Inc. moduladores do receptor de estrogênio e os seus usos
SG11201403002RA (en) 2011-12-14 2014-07-30 Seragon Pharmaceuticals Inc Fluorinated estrogen receptor modulators and uses thereof
EA201490897A1 (ru) 2011-12-16 2015-03-31 Олема Фармасьютикалс, Инк. Новые бензопирановые соединения, композиции и их применение

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
US5254568A (en) * 1990-08-09 1993-10-19 Council Of Scientific & Industrial Research Benzopyrans as antiestrogenic agents
US6060503A (en) * 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
US5407947A (en) * 1993-11-05 1995-04-18 Eli Lilly And Company Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans
AU8102398A (en) * 1997-07-09 1999-02-08 Central Drug Research Institute (dl)-2,3-diaryl-2h-1-benzopyrans
AU8102498A (en) * 1997-07-09 1999-02-08 Central Drug Research Institute Preparation of diaryl-benzopyrans
US6465445B1 (en) * 1998-06-11 2002-10-15 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

Also Published As

Publication number Publication date
JP3684332B2 (ja) 2005-08-17
DE69905376D1 (de) 2003-03-20
HK1036978A1 (en) 2002-01-25
CN1322200A (zh) 2001-11-14
AU5459399A (en) 2000-03-06
ATE232525T1 (de) 2003-02-15
JP2002522533A (ja) 2002-07-23
CA2340343A1 (en) 2000-02-24
DE69905376T2 (de) 2003-10-09
EP1104414A1 (en) 2001-06-06
JP4461048B2 (ja) 2010-05-12
EP1104414B1 (en) 2003-02-12
WO2000009493A1 (en) 2000-02-24
ZA200100875B (en) 2002-06-26
CA2340343C (en) 2007-04-24
CN1146554C (zh) 2004-04-21
JP2005206610A (ja) 2005-08-04

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