AU2001270906B2 - Oxidation process for preparing the intermediate 6.alpha.,9.alpha.-difluoro-11.beta.,17.alpha.-dihydroxy-16.a lpha.-methyl-androst-1,4-dien-3-one 17.beta.-carboxylic acid - Google Patents

Oxidation process for preparing the intermediate 6.alpha.,9.alpha.-difluoro-11.beta.,17.alpha.-dihydroxy-16.a lpha.-methyl-androst-1,4-dien-3-one 17.beta.-carboxylic acid Download PDF

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Publication number
AU2001270906B2
AU2001270906B2 AU2001270906A AU2001270906A AU2001270906B2 AU 2001270906 B2 AU2001270906 B2 AU 2001270906B2 AU 2001270906 A AU2001270906 A AU 2001270906A AU 2001270906 A AU2001270906 A AU 2001270906A AU 2001270906 B2 AU2001270906 B2 AU 2001270906B2
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AU
Australia
Prior art keywords
process according
formula
compound
water
alpha
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Ceased
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AU2001270906A
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AU2001270906A1 (en
Inventor
Frederick David Albinson
Steven John Coote
John Malcolm Robinson
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Glaxo Group Ltd
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Glaxo Group Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
AU2001270906A 2000-07-21 2001-07-20 Oxidation process for preparing the intermediate 6.alpha.,9.alpha.-difluoro-11.beta.,17.alpha.-dihydroxy-16.a lpha.-methyl-androst-1,4-dien-3-one 17.beta.-carboxylic acid Ceased AU2001270906B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0017988.7A GB0017988D0 (en) 2000-07-21 2000-07-21 Novel process
GB0017988.7 2000-07-21
PCT/GB2001/003289 WO2002008243A1 (en) 2000-07-21 2001-07-20 Oxidation process for preparing the intermediate 6.alpha.,9.alpha.-difluoro-11.beta.,17.alpha.-dihydroxy-16.alpha.-methyl-androst-1,4-dien-3-one 17.beta.-carboxylic acid

Publications (2)

Publication Number Publication Date
AU2001270906A1 AU2001270906A1 (en) 2002-05-02
AU2001270906B2 true AU2001270906B2 (en) 2005-10-13

Family

ID=9896132

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2001270906A Ceased AU2001270906B2 (en) 2000-07-21 2001-07-20 Oxidation process for preparing the intermediate 6.alpha.,9.alpha.-difluoro-11.beta.,17.alpha.-dihydroxy-16.a lpha.-methyl-androst-1,4-dien-3-one 17.beta.-carboxylic acid
AU7090601A Pending AU7090601A (en) 2000-07-21 2001-07-20 Oxidation process for preparing the intermediate 6.alpha.,9.alpha.-difluoro-11.beta.,17.alpha.-dihydroxy-16.alpha.-methyl-androst-1,4-dien-3-one 17.beta.-carboxylic acid

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU7090601A Pending AU7090601A (en) 2000-07-21 2001-07-20 Oxidation process for preparing the intermediate 6.alpha.,9.alpha.-difluoro-11.beta.,17.alpha.-dihydroxy-16.alpha.-methyl-androst-1,4-dien-3-one 17.beta.-carboxylic acid

Country Status (26)

Country Link
US (1) US20040043974A1 (enExample)
EP (1) EP1301526B1 (enExample)
JP (1) JP2004504403A (enExample)
KR (1) KR100787293B1 (enExample)
CN (1) CN1315864C (enExample)
AT (1) ATE398628T1 (enExample)
AU (2) AU2001270906B2 (enExample)
BR (1) BR0110430A (enExample)
CA (1) CA2406963A1 (enExample)
CY (1) CY1108553T1 (enExample)
CZ (1) CZ302592B6 (enExample)
DE (1) DE60134472D1 (enExample)
DK (1) DK1301526T3 (enExample)
ES (1) ES2307628T3 (enExample)
GB (1) GB0017988D0 (enExample)
HK (1) HK1056179B (enExample)
HU (1) HUP0301108A3 (enExample)
IL (2) IL152348A0 (enExample)
MX (1) MXPA02010967A (enExample)
NO (1) NO324836B1 (enExample)
NZ (1) NZ522083A (enExample)
PL (1) PL206652B1 (enExample)
PT (1) PT1301526E (enExample)
SI (1) SI1301526T1 (enExample)
WO (1) WO2002008243A1 (enExample)
ZA (1) ZA200208372B (enExample)

Families Citing this family (20)

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Publication number Priority date Publication date Assignee Title
US6858596B2 (en) 2000-08-05 2005-02-22 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivative
US6787532B2 (en) 2000-08-05 2004-09-07 Smithkline Beecham Corporation Formulation containing anti-inflammatory androstane derivatives
US6858593B2 (en) 2000-08-05 2005-02-22 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US6759398B2 (en) 2000-08-05 2004-07-06 Smithkline Beecham Corporation Anti-inflammatory androstane derivative
US6777400B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
CO5310534A1 (es) 2000-08-05 2003-08-29 Glaxo Group Ltd Nuevos derivados de androstano anti-inflamatorios
US6777399B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
GB0019172D0 (en) 2000-08-05 2000-09-27 Glaxo Group Ltd Novel compounds
US6750210B2 (en) 2000-08-05 2004-06-15 Smithkline Beecham Corporation Formulation containing novel anti-inflammatory androstane derivative
UA77656C2 (en) 2001-04-07 2007-01-15 Glaxo Group Ltd S-fluoromethyl ester of 6-alpha, 9-alpha-difluoro-17-alpha-[(2-furanylcarbonyl)oxy]-11-beta-hydroxy-16- alpha-methyl-3-oxoandrosta-1,4-dien-17-beta-carbothioacid as anti-inflammatory agent
ES2314052T3 (es) 2001-04-30 2009-03-16 Glaxo Group Limited Derivados de ester de 17beta-carbotioato de androstano con un grupo ester ciclico en la posicion 17alfa.
GB2389530B (en) 2002-06-14 2007-01-10 Cipla Ltd Pharmaceutical compositions
IL150654A (en) 2002-07-09 2006-12-10 Ori Lerman Method for acid isolation 6α, 9α - difluoro - ß, 17α11 - dihydroxy - 16α - methylfargana - 3 - oxo - 1, 4 - diene - 17ß - carboxylate
JP2006522028A (ja) * 2003-04-04 2006-09-28 アルファーマ エーピーエス ステロイド性カルボチオ酸誘導体の製造方法および中間体
EP1466920A1 (en) * 2003-04-04 2004-10-13 Alpharma APS Process for the preparation of steroidal 17 beta-carbothioates
EP1526139A1 (en) * 2003-10-24 2005-04-27 S.N.I.F.F. Italia S.P.A. A process for preparing highly pure androstane 17-beta-carboxylic acids and androstane 17-beta-carbothioic acid fluoromethyl esters
GB0612027D0 (en) 2006-06-16 2006-07-26 Glaxo Group Ltd Novel process
NO331891B1 (no) 2007-03-20 2012-04-30 Clavis Pharma Asa Kjemiske forbindelser, et farmasoytisk preparat inneholdende slike forbindelser, samt anvendelse derav for behandling av kreft, inflammasjon og KOLS
PT105139B (pt) * 2010-06-01 2013-01-29 Hovione Farmaciencia S A Método para a monofluorometilação de substratos orgânicos para preparação de compostos orgânicos biologicamente activos
WO2012029077A2 (en) 2010-09-01 2012-03-08 Cadila Healthcare Limited Process for preparing fluticasone propionate/furoate

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1964356A1 (de) * 1968-12-23 1970-07-02 Ciba Geigy Verfahren zur Herstellung von Estern von Steroid-17-carbonsaeuren
GB2018256A (en) * 1978-04-05 1979-10-17 Syntex Inc Thio atianic acid derivatives
US4198336A (en) * 1978-04-05 1980-04-15 Syntex (U.S.A.) Inc. Chemical process for preparing androsta-4-ene 17α-carboxylic acids
GB2088877A (en) * 1980-02-15 1982-06-16 Glaxo Group Ltd Androstane 17 beta carbothioates
WO1995018621A1 (en) * 1994-01-04 1995-07-13 Duke University Methods of inhibiting angiogenesis and tumor growth, and treating ophthalmologic conditions with angiostatic and therapeutic steroids

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL187577C (nl) * 1978-04-05 1991-11-18 Sibla Srl 3-acetoxy-9beta,11beta-epoxy-pregna-1,3,5-trienen, werkwijze voor de bereiding daarvan en werkwijze voor de bereiding van 6alfa-halogeen-pregna-1,4-dieen-3-onen.
US4263289A (en) * 1978-04-05 1981-04-21 Syntex (U.S.A.) Inc. Thio etianic acid derivatives
US6197761B1 (en) * 1995-12-29 2001-03-06 Glaxo Wellcome Inc. 17β-2-oxo-tetrahydrofuranyl)-carbothioic acid ester, -carboxylic acid ester and -carboxylic acid amide androstane derivatives
US20020133032A1 (en) * 2000-02-25 2002-09-19 Jufang Barkalow Method for the preparation of fluticasone and related 17beta-carbothioic esters using a novel carbothioic acid synthesis and novel purification methods
MXPA02009814A (es) * 2000-04-04 2003-03-27 Celanese Int Corp Composiciones de revestimiento receptivas de tinta que contienen alcohol polivinilico injertado con grupos funcionales amina.
US6777400B2 (en) * 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1964356A1 (de) * 1968-12-23 1970-07-02 Ciba Geigy Verfahren zur Herstellung von Estern von Steroid-17-carbonsaeuren
GB2018256A (en) * 1978-04-05 1979-10-17 Syntex Inc Thio atianic acid derivatives
US4198336A (en) * 1978-04-05 1980-04-15 Syntex (U.S.A.) Inc. Chemical process for preparing androsta-4-ene 17α-carboxylic acids
GB2088877A (en) * 1980-02-15 1982-06-16 Glaxo Group Ltd Androstane 17 beta carbothioates
WO1995018621A1 (en) * 1994-01-04 1995-07-13 Duke University Methods of inhibiting angiogenesis and tumor growth, and treating ophthalmologic conditions with angiostatic and therapeutic steroids

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J Org Chem (1986) 51, 2315 *

Also Published As

Publication number Publication date
CN1437610A (zh) 2003-08-20
ATE398628T1 (de) 2008-07-15
ES2307628T3 (es) 2008-12-01
CA2406963A1 (en) 2002-01-31
PT1301526E (pt) 2008-09-09
IL152348A (en) 2008-08-07
NO324836B1 (no) 2007-12-17
US20040043974A1 (en) 2004-03-04
EP1301526B1 (en) 2008-06-18
HUP0301108A3 (en) 2008-04-28
PL359462A1 (en) 2004-08-23
PL206652B1 (pl) 2010-09-30
NZ522083A (en) 2004-06-25
NO20025054D0 (no) 2002-10-21
GB0017988D0 (en) 2000-09-13
KR100787293B1 (ko) 2007-12-20
NO20025054L (no) 2002-11-05
IL152348A0 (en) 2003-05-29
HK1056179A1 (en) 2004-02-06
MXPA02010967A (es) 2003-03-27
ZA200208372B (en) 2004-02-11
HUP0301108A2 (hu) 2003-08-28
JP2004504403A (ja) 2004-02-12
CN1315864C (zh) 2007-05-16
DE60134472D1 (de) 2008-07-31
DK1301526T3 (da) 2008-10-06
AU7090601A (en) 2002-02-05
CZ20023472A3 (cs) 2003-04-16
BR0110430A (pt) 2003-07-08
WO2002008243A1 (en) 2002-01-31
EP1301526A1 (en) 2003-04-16
SI1301526T1 (sl) 2008-10-31
CY1108553T1 (el) 2014-04-09
HK1056179B (en) 2009-07-17
KR20030028736A (ko) 2003-04-10
CZ302592B6 (cs) 2011-07-27

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired