DE102006018888A1 - Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil) - Google Patents

Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil) Download PDF

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Publication number
DE102006018888A1
DE102006018888A1 DE102006018888A DE102006018888A DE102006018888A1 DE 102006018888 A1 DE102006018888 A1 DE 102006018888A1 DE 102006018888 A DE102006018888 A DE 102006018888A DE 102006018888 A DE102006018888 A DE 102006018888A DE 102006018888 A1 DE102006018888 A1 DE 102006018888A1
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DE
Germany
Prior art keywords
asoprisnil
drying
solution
reaction
spray
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.)
Ceased
Application number
DE102006018888A
Other languages
German (de)
English (en)
Inventor
Detlef Grawe
Sabine Gliesing
Hagen Gerecke
Peter Hoesel
Uwe Mueller
Thomas Michel
Robert Eilers
Uwe Knabe
Bernd Erhart
Michael Mosebach
David Voigtlaender
Ulf Tilstam
Juergen Jacke
Klaus Bahl
Ulf Bohlmann
Dieter Wehmeier
Ernst Sander
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.)
Bayer Pharma AG
Original Assignee
Bayer Schering Pharma AG
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 Bayer Schering Pharma AG filed Critical Bayer Schering Pharma AG
Priority to DE102006018888A priority Critical patent/DE102006018888A1/de
Priority to MX2007000450A priority patent/MX2007000450A/es
Priority to MX2008013336A priority patent/MX2008013336A/es
Priority to CA2648537A priority patent/CA2648537C/fr
Priority to BRPI0710517-7A priority patent/BRPI0710517A2/pt
Priority to JP2009505800A priority patent/JP2009534345A/ja
Priority to RU2008145098/04A priority patent/RU2008145098A/ru
Priority to PCT/EP2007/003723 priority patent/WO2007118717A2/fr
Priority to EP07724653A priority patent/EP2010555A2/fr
Priority to CA2839228A priority patent/CA2839228A1/fr
Priority to AU2007237457A priority patent/AU2007237457A1/en
Priority to CNA2007800212624A priority patent/CN101466724A/zh
Priority to KR1020087025453A priority patent/KR20080110629A/ko
Publication of DE102006018888A1 publication Critical patent/DE102006018888A1/de
Priority to ZA200809787A priority patent/ZA200809787B/xx
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
DE102006018888A 2006-04-18 2006-04-18 Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil) Ceased DE102006018888A1 (de)

Priority Applications (14)

Application Number Priority Date Filing Date Title
DE102006018888A DE102006018888A1 (de) 2006-04-18 2006-04-18 Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil)
MX2007000450A MX2007000450A (es) 2006-04-18 2007-01-12 PROCEDIMIENTO PARA LA PREPARACION DE LA (E)-OXIMA DE 4-[17ß-METOXI-A-METOXIMETIL-3-OXO-ESTRA-4,9-DIEN-11ß-IL]-BENZALDE HIDO(ASOPRISNIL).
PCT/EP2007/003723 WO2007118717A2 (fr) 2006-04-18 2007-04-17 MÉTHODE DE PRÉPARATION DE 4-[17β-METHOXY-17α-MÉTHOXYMÉTHYL-3-OXOESTRA-4,9-DIEN-11β-YL]BENZALDÉHYDE (E)-OXIME (ASOPRISNIL)
CA2839228A CA2839228A1 (fr) 2006-04-18 2007-04-17 Methode de preparation de 4-[17.beta.-methoxy-17.alpha.-methoxymethyl-3-oxoestra-4,9-dien-11.beta.-yl]benzaldehyde (e)-oxime (asoprisnil)
BRPI0710517-7A BRPI0710517A2 (pt) 2006-04-18 2007-04-17 método para preparar 4-[17 beta-metóxi-17alfa-metoximetil-3-oxoestra-4,9-diean- 11beta-il]benzaldeìdo (e)-oxima (asoprisnil)
JP2009505800A JP2009534345A (ja) 2006-04-18 2007-04-17 ４−［１７β−メトキシ−１７α−メトキシメチル−３−オキソエストラ−４，９−ジエン−１１β−イル］ベンズアルデヒド（Ｅ）−オキシム（アソプリスニル）の調製方法
RU2008145098/04A RU2008145098A (ru) 2006-04-18 2007-04-17 Способ получения 4-[17[бэта]-метокси-17[альфа]-метоксиметил-3-оксоэстра-4,9-диен-11[бэта]-ил]бензальдегид(е)-оксима (азоприснила)
MX2008013336A MX2008013336A (es) 2006-04-18 2007-04-17 METODO PARA PREPARAR (E)-OXIMA DE 4-[17ß-METOXI-17A-METOXIMETIL-3- OXOESTRA-4,9-DIEN-11ß-IL]BENZALDEHIDO (ASOPRISNIL).
EP07724653A EP2010555A2 (fr) 2006-04-18 2007-04-17 Méthode de préparation de 4-[17 beta -methoxy-17 alpha -méthoxyméthyl-3-oxoestra-4,9-dien-11beta -yl]benzaldéhyde (e)-oxime (asoprisnil)
CA2648537A CA2648537C (fr) 2006-04-18 2007-04-17 Methode de preparation de 4-[17.beta.-methoxy-17.alpha.-methoxymethyl-3-oxoestra-4,9-dien-11.beta.-yl]benzaldehyde (e)-oxime (asoprisnil)
AU2007237457A AU2007237457A1 (en) 2006-04-18 2007-04-17 Method for preparing 4-[17beta-methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyde (E)-oxime (asoprisnil)
CNA2007800212624A CN101466724A (zh) 2006-04-18 2007-04-17 制备4-[17β-甲氧基-17α-甲氧基甲基-3-氧代雌-4,9-二烯-11β-基]苯甲醛(E)-肟(asoprisnil)的方法
KR1020087025453A KR20080110629A (ko) 2006-04-18 2007-04-17 4-[17β-메톡시-17α-메톡시메틸-3-옥소에스트라-4,9-디엔-11β-일]벤즈알데히드 (Ｅ)-옥심 (아소프리스닐)의 제조 방법
ZA200809787A ZA200809787B (en) 2006-04-18 2008-11-17 Method for preparing 4-[17ß-methoxy-17+--methoxymethyl-3-oxoestra-4,9-dien-11ß-yl]benzaldehyde (E)-oxime (asoprisnil)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102006018888A DE102006018888A1 (de) 2006-04-18 2006-04-18 Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil)

Publications (1)

Publication Number Publication Date
DE102006018888A1 true DE102006018888A1 (de) 2007-10-25

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ID=38536818

Family Applications (1)

Application Number Title Priority Date Filing Date
DE102006018888A Ceased DE102006018888A1 (de) 2006-04-18 2006-04-18 Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil)

Country Status (12)

Country Link
EP (1) EP2010555A2 (fr)
JP (1) JP2009534345A (fr)
KR (1) KR20080110629A (fr)
CN (1) CN101466724A (fr)
AU (1) AU2007237457A1 (fr)
BR (1) BRPI0710517A2 (fr)
CA (2) CA2839228A1 (fr)
DE (1) DE102006018888A1 (fr)
MX (2) MX2007000450A (fr)
RU (1) RU2008145098A (fr)
WO (1) WO2007118717A2 (fr)
ZA (1) ZA200809787B (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108003210A (zh) * 2018-01-24 2018-05-08 四川理工学院 一种雌甾-4,9-二烯-3,17-二酮的制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0057115A2 (fr) * 1981-01-09 1982-08-04 Roussel-Uclaf Nouveaux dérivés stéroides substitués en 11beta, procédé de préparation, leur application comme médicament et les compositions les renfermant
DE4332283A1 (de) * 1993-09-20 1995-04-13 Jenapharm Gmbh Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
DE10056675A1 (de) * 2000-11-10 2002-05-16 Jenapharm Gmbh Verfahren zur Herstellung von 4-(17alpha-Methylsubstituierten 3-Oxoestra-4,9-dien-11ß-yl)-benzaldehyd-(1E oder 1Z)-oximen
DE10056676A1 (de) * 2000-11-10 2002-05-16 Jenapharm Gmbh Verfahren zur Herstellung von 4-/17alpha-substituierten-3-oxoestra-4,9-dien-11beta-yl)benzaldehyd-(1E oder 1Z)-oximen
EP1292607A2 (fr) * 2000-05-23 2003-03-19 Schering AG Nouvelles formes solides de mesoprogestine 11beta- 4e-(hydroxyiminomethyl)-phenyle]-17alpha-methoxymethyle-17beta-methoxy-estra-4,9-diene-3-one

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR5183M (fr) * 1966-03-04 1967-06-19
DD296931A5 (de) * 1987-08-28 1991-12-19 Jenapharm Gmbh Jena,De Verfahren zur herstellung von 13 beta-alkyl-5(10),9(11)-gonadienderivaten
US4910191A (en) * 1988-06-28 1990-03-20 Merrell Dow Pharmaceuticals Inc. 19-substituted progesterone derivatives useful as 19-hydroxylase inhibitors
JP4197890B2 (ja) * 2001-05-24 2008-12-17 興和創薬株式会社 第一級アリルアルコール類の酸化方法
DE10311092A1 (de) * 2003-03-07 2004-10-07 Schering Ag Verfahren zur Oxidation der 17-Hydroxylfunktion in Steroiden und die Verwendung von Trifluoressigsäure und Cyclohexanon zur Herstellung von steroidalen 17-Ketonen mittels Oppenauer Oxidation
DE102004021060A1 (de) * 2004-04-29 2005-11-24 Schering Ag Wiederfindung von Arzneistoffen im ppm-Bereich in Produktionsanlagen

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0057115A2 (fr) * 1981-01-09 1982-08-04 Roussel-Uclaf Nouveaux dérivés stéroides substitués en 11beta, procédé de préparation, leur application comme médicament et les compositions les renfermant
DE4332283A1 (de) * 1993-09-20 1995-04-13 Jenapharm Gmbh Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
EP1292607A2 (fr) * 2000-05-23 2003-03-19 Schering AG Nouvelles formes solides de mesoprogestine 11beta- 4e-(hydroxyiminomethyl)-phenyle]-17alpha-methoxymethyle-17beta-methoxy-estra-4,9-diene-3-one
DE10056675A1 (de) * 2000-11-10 2002-05-16 Jenapharm Gmbh Verfahren zur Herstellung von 4-(17alpha-Methylsubstituierten 3-Oxoestra-4,9-dien-11ß-yl)-benzaldehyd-(1E oder 1Z)-oximen
DE10056676A1 (de) * 2000-11-10 2002-05-16 Jenapharm Gmbh Verfahren zur Herstellung von 4-/17alpha-substituierten-3-oxoestra-4,9-dien-11beta-yl)benzaldehyd-(1E oder 1Z)-oximen

Also Published As

Publication number Publication date
JP2009534345A (ja) 2009-09-24
EP2010555A2 (fr) 2009-01-07
RU2008145098A (ru) 2010-05-27
CN101466724A (zh) 2009-06-24
CA2648537A1 (fr) 2007-10-25
KR20080110629A (ko) 2008-12-18
MX2008013336A (es) 2008-10-31
WO2007118717A2 (fr) 2007-10-25
CA2648537C (fr) 2014-09-23
MX2007000450A (es) 2009-02-11
BRPI0710517A2 (pt) 2011-08-16
CA2839228A1 (fr) 2007-10-25
ZA200809787B (en) 2010-01-27
WO2007118717A3 (fr) 2008-04-24
AU2007237457A1 (en) 2007-10-25

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Owner name: BAYER SCHERING PHARMA AKIENGESELLSCHAFT, 13353, DE

8131 Rejection