CN1032211C - 9α-羟基-17-亚甲基甾类的制备方法 - Google Patents

9α-羟基-17-亚甲基甾类的制备方法 Download PDF

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Publication number
CN1032211C
CN1032211C CN89102092A CN89102092A CN1032211C CN 1032211 C CN1032211 C CN 1032211C CN 89102092 A CN89102092 A CN 89102092A CN 89102092 A CN89102092 A CN 89102092A CN 1032211 C CN1032211 C CN 1032211C
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CN
China
Prior art keywords
hydroxyl
alpha
methyl
pregnant
formula
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
CN89102092A
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English (en)
Chinese (zh)
Other versions
CN1036774A (zh
Inventor
杰克巴斯·尼考拉斯·玛瑞·巴提斯特
阿瑟·夫瑞迪奇·马克斯
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.)
Russell Ukraf Co ltd
Aventis Pharma SA
Aventis Pharmaceuticals Inc
Original Assignee
Roussel Uclaf SA
Gist Brocades NV
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Filing date
Publication date
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Publication of CN1036774A publication Critical patent/CN1036774A/zh
Application granted granted Critical
Publication of CN1032211C publication Critical patent/CN1032211C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal 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
    • C07J5/0007—Normal 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 not substituted in position 17 alfa
    • C07J5/0023—Normal 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 not substituted in position 17 alfa substituted in position 16
    • C07J5/003—Normal 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 not substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group including 16-alkylidene substitutes
    • C07J5/0038—Normal 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 not substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group including 16-alkylidene substitutes by an alkyl group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • 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
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • 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
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal 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
    • C07J5/0007—Normal 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 not substituted in position 17 alfa
    • C07J5/0015—Normal 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 not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/009—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by only one oxygen atom doubly bound

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN89102092A 1988-04-08 1989-04-08 9α-羟基-17-亚甲基甾类的制备方法 Expired - Lifetime CN1032211C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
NL88200675.2 1988-04-08
EP88200675 1988-04-08

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CNB951202561A Division CN1187365C (zh) 1988-04-08 1989-04-08 9α－羟基－17－亚甲基甾类在制备皮质甾类中的用途

Publications (2)

Publication Number Publication Date
CN1036774A CN1036774A (zh) 1989-11-01
CN1032211C true CN1032211C (zh) 1996-07-03

Family

ID=8199778

Family Applications (2)

Application Number Title Priority Date Filing Date
CN89102092A Expired - Lifetime CN1032211C (zh) 1988-04-08 1989-04-08 9α-羟基-17-亚甲基甾类的制备方法
CNB951202561A Expired - Lifetime CN1187365C (zh) 1988-04-08 1989-04-08 9α－羟基－17－亚甲基甾类在制备皮质甾类中的用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CNB951202561A Expired - Lifetime CN1187365C (zh) 1988-04-08 1989-04-08 9α－羟基－17－亚甲基甾类在制备皮质甾类中的用途

Country Status (18)

Country Link
US (1) US5194602A (enExample)
EP (1) EP0336521B1 (enExample)
JP (1) JP2812397B2 (enExample)
KR (1) KR0138777B1 (enExample)
CN (2) CN1032211C (enExample)
AU (1) AU618350B2 (enExample)
CA (1) CA1332409C (enExample)
DE (1) DE68901104D1 (enExample)
DK (1) DK175401B1 (enExample)
ES (1) ES2033516T3 (enExample)
FI (1) FI108436B (enExample)
GR (1) GR3004539T3 (enExample)
HU (1) HU208437B (enExample)
IE (1) IE62277B1 (enExample)
IL (1) IL89880A (enExample)
NO (1) NO300894B1 (enExample)
PT (1) PT90227B (enExample)
WO (1) WO1989009781A1 (enExample)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ236206A (en) * 1989-11-27 1993-03-26 Schering Corp Preparation of 2'-methyl-4'-methylenespiro(androstadiene-17,5'(4'h)-oxazol)-3-one derivatives from pregn-5-en-20-ylideneacetamide derivatives by treatment with vilsmeier reagent or acid
FR2677029B1 (fr) * 1991-05-23 1994-01-21 Roussel Uclaf Nouveaux derives sterouides de l'andostra-4,9(11),16-trien-3-one.
FR2677028B1 (fr) * 1991-05-23 1994-01-21 Roussel Uclaf Nouveaux derives sterouides du pregna-4,9(11),17(20)-trien-3-one.
FR2676740B1 (fr) * 1991-05-23 1993-11-05 Roussel Uclaf Nouveaux derives sterouides du pregna-4,9(11),17(20)-trie-3-one, leur preparation, leur application a la preparation de composes sterouides de type pregna-4,9(11),16-triene-3,20-dione et nouveaux intermediaires.
FR2681069B1 (fr) * 1991-09-06 1995-04-28 Roussel Uclaf Nouveau procede de preparation de l'hydrocortisone et nouveaux intermediaires.
FR2683530B1 (fr) * 1991-11-08 1994-01-21 Roussel Uclaf Nouveau procede de preparation de derives 20-oxo 17 alpha, 21-dihydroxyles du pregnane et nouveaux intermediaires.
EP0624162B1 (en) * 1992-01-28 1998-09-16 Schering Corporation Novel steroid intermediates and processes for their preparation
CN1061984C (zh) * 1996-04-18 2001-02-14 上海华联制药有限公司 甾体激素化合物中引入9-11双键的一种方法
WO1999061055A1 (en) 1998-05-22 1999-12-02 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
US6855836B2 (en) * 2000-10-26 2005-02-15 Jenapharm Gmbh & Co. Kg 17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds
DK1889198T3 (da) 2005-04-28 2015-02-09 Proteus Digital Health Inc Farma-informatiksystem
JP2009508494A (ja) 2005-09-16 2009-03-05 ラプトール ファーマシューティカル インコーポレイテッド Ｃｒを含むタンパク質に対して特異的な受容体−結合タンパク質（ｒａｐ）変異体を含む組成物およびその使用
US20080318870A1 (en) 2007-06-19 2008-12-25 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
TWI503327B (zh) * 2007-06-19 2015-10-11 Kythera Biopharmaceuticals Inc 合成膽汁酸組合物，方法及製備
US8242294B2 (en) 2007-06-19 2012-08-14 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
JOP20180077A1 (ar) 2007-06-19 2019-01-30 Kythera Biopharmaceuticals Inc تركيبات وطرق لحمض صفراوي تخليقي
WO2010095940A2 (en) 2009-02-20 2010-08-26 To-Bbb Holding B.V. Glutathione-based drug delivery system
TWI556839B (zh) 2009-05-06 2016-11-11 研究室護膚股份有限公司 包含活性劑－磷酸鈣粒子複合物之皮膚遞送組成物及其使用方法
GB2480632A (en) 2010-05-25 2011-11-30 Kythera Biopharmaceuticals Inc Preparation of 12-keto and 12-alpha-hydroxy steroids
WO2012021133A1 (en) 2010-08-12 2012-02-16 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
WO2013044119A1 (en) * 2011-09-22 2013-03-28 Kythera Biopharmaceuticals, Inc. Compositions and methods related to deoxycholic acid and its polymorphs

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL103170C (enExample) * 1958-11-14
DE1568506A1 (de) * 1966-03-23 1970-07-16 Hoechst Ag Verfahren zur Herstellung von delta?-Pregnen-3,21-diol-20-on-21-acylaten
US3445907A (en) * 1967-02-16 1969-05-27 Ind Tectonics Inc Roller retaining method for roller bearing separators
US4255344A (en) * 1978-11-08 1981-03-10 Mitsubishi Chemical Industries, Limited 9-α-Hydroxy steroids
FR2462445A1 (fr) * 1979-07-31 1981-02-13 Roussel Uclaf Nouveaux derives 17-/(hydroxymethyl) (formamido) methylene/steroides, leur procede de preparation et leur application a l'introduction de la chaine laterale hydroxyacetyle
FR2486947A1 (fr) * 1980-07-15 1982-01-22 Roussel Uclaf Nouveaux derives steroides 20-isonitriles 17(20) insatures, leur procede de preparation et leur application a la preparation des steroides 17a-hydroxy 20-ceto
DE3136917A1 (de) * 1980-09-27 1982-05-19 Barmag Barmer Maschinenfabrik Ag, 5630 Remscheid "kraftstoffoerderpumpe"
FR2493324B1 (enExample) * 1980-11-05 1983-01-21 Roussel Uclaf
FR2521567A1 (fr) * 1982-02-18 1983-08-19 Roussel Uclaf Nouveaux derives steroides 17(20)nitro, leur procede de preparation et leur application a la preparation de corticosteroides
EP0123734A1 (en) * 1983-04-29 1984-11-07 Gist-Brocades N.V. 17-(Isocyano-sulfonylmethylene)-steroids, 17-(formamido-sulfonylmethylene)-steroids and their preparation

Also Published As

Publication number Publication date
DK240890A (da) 1990-10-05
DE68901104D1 (de) 1992-05-07
PT90227B (pt) 1994-06-30
ES2033516T3 (es) 1993-03-16
EP0336521A1 (en) 1989-10-11
JP2812397B2 (ja) 1998-10-22
HUT55411A (en) 1991-05-28
NO904333D0 (no) 1990-10-05
CA1332409C (en) 1994-10-11
HU208437B (en) 1993-10-28
HU892602D0 (en) 1991-03-28
KR0138777B1 (ko) 1998-04-30
IE62277B1 (en) 1995-01-25
CN1036774A (zh) 1989-11-01
AU618350B2 (en) 1991-12-19
US5194602A (en) 1993-03-16
PT90227A (pt) 1989-11-10
DK240890D0 (da) 1990-10-05
CN1187365C (zh) 2005-02-02
FI108436B (fi) 2002-01-31
IL89880A (en) 1994-06-24
FI904877A0 (fi) 1990-10-03
AU3431389A (en) 1989-11-03
IL89880A0 (en) 1989-12-15
KR900700499A (ko) 1990-08-13
DK175401B1 (da) 2004-09-27
CN1141301A (zh) 1997-01-29
WO1989009781A1 (en) 1989-10-19
NO904333L (no) 1990-12-03
NO300894B1 (no) 1997-08-11
JPH03503645A (ja) 1991-08-15
GR3004539T3 (enExample) 1993-04-28
IE891134L (en) 1989-10-08
EP0336521B1 (en) 1992-04-01

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C06 Publication
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Address after: Paris France

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Address before: Holland V Woolf.

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COR Change of bibliographic data

Free format text: CORRECT: APPLICANT; FROM: GIST-BROCADES S. A. TO: LU SAIER UCLAF LTD.

C53 Correction of patent of invention or patent application
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Free format text: CORRECT: APPLICANT; FROM: GIST-BROCADES S. A. TO: ROUSSEL·WURLKURF CO., LTD.

C14 Grant of patent or utility model
GR01 Patent grant
C15 Extension of patent right duration from 15 to 20 years for appl. with date before 31.12.1992 and still valid on 11.12.2001 (patent law change 1993)
OR01 Other related matters
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Owner name: ROUSSEL·WURLKURF CO., LTD.

Free format text: FORMER NAME OR ADDRESS: ROUSSEL UCLAF

Owner name: AVENTIS PHARMA S.A.

Free format text: FORMER NAME OR ADDRESS: HOECHST MARION ROUSSEL, INC.

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Patentee before: HOECHST MARION ROUSSEL, Inc.

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C17 Cessation of patent right
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