ES8200120A1 - Un metodo para la preparacion de 17,21-diesteres de 6alfa- fluoro-prednisolona - Google Patents

Un metodo para la preparacion de 17,21-diesteres de 6alfa- fluoro-prednisolona

Info

Publication number
ES8200120A1
ES8200120A1 ES496839A ES496839A ES8200120A1 ES 8200120 A1 ES8200120 A1 ES 8200120A1 ES 496839 A ES496839 A ES 496839A ES 496839 A ES496839 A ES 496839A ES 8200120 A1 ES8200120 A1 ES 8200120A1
Authority
ES
Spain
Prior art keywords
methyl
formula
hydrogen
prednisolone
fluoro
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
Application number
ES496839A
Other languages
English (en)
Other versions
ES496839A0 (es
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.)
Sterosynt Ltd
Original Assignee
Sterosynt Ltd
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
Priority claimed from IT7927353A external-priority patent/IT1209140B/it
Priority claimed from IT49853/80A external-priority patent/IT1143039B/it
Application filed by Sterosynt Ltd filed Critical Sterosynt Ltd
Publication of ES8200120A1 publication Critical patent/ES8200120A1/es
Publication of ES496839A0 publication Critical patent/ES496839A0/es
Granted legal-status Critical Current

Links

Classifications

    • 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
    • C07J5/0046—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 substituted in position 17 alfa
    • C07J5/0061—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 substituted in position 17 alfa substituted in position 16
    • C07J5/0069—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 substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group
    • C07J5/0076—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 substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group by an alkyl group
    • 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
    • C07J5/0046—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 substituted in position 17 alfa
    • C07J5/0053—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 substituted in position 17 alfa not substituted in position 16
    • 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
    • C07J71/0015—Oxiranes at position 9(11)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

PROCEDIMIENTO DE PREPARACION DE 17,21-DIESTERES DE 6-ALFA-FLUORO-PREDNISOLONA, DE FORMULA (I), DONDE R1 Y R2 SON UN GRUPO ALQUILO DE 1-6 CARBONOS, O ARILO; Y ES HIDROGENO O BROMO, Y Z ES HIDROGENO CUANDO R1 O R2 NO SON METILO, O ES METIL. SE HACE REACCIONAR UNA SOLUCION DE UN COMPUESTO DE FORMULA (II) EN ACIDO ACETICO O TETRACLORURO DE CARBONO, A TEMPERATURA DE 0-5 C, CON BROMURO DE HIDROGENO EN ACIDO ACETICO GLACIAL. SE OBTIENE EL COMPUESTO DE FORMULA (I), SIENDO Y BROMO. TRATANDO ESTE PRODUCTO CON HIDRURO DE TRIBUTILESTAÑO EN TETRAHIDROFURANO ANHIDRO, A LA TEMPERATURA DE REFLUJO Y EN PRESENCIA DE UN INICIADOR DE REACCIONES DE RADICAL LIBRE, SE OBTIENE EL COMPUESTO DE FORMULA (I), SIENDO Y HIDROGENO. DE APLICACION COMO AGENTES ANTIINFLAMATORIOS.
ES496839A 1979-11-16 1980-11-14 Un metodo para la preparacion de 17,21-diesteres de 6alfa- fluoro-prednisolona Granted ES496839A0 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT7927353A IT1209140B (it) 1979-11-16 1979-11-16 6 alfa-fluoro-prednisolone 17,21-diesteri.
IT49853/80A IT1143039B (it) 1980-10-09 1980-10-09 6-alfa-fluoro-prednisolone 17,21-diesteri

Publications (2)

Publication Number Publication Date
ES8200120A1 true ES8200120A1 (es) 1981-10-16
ES496839A0 ES496839A0 (es) 1981-10-16

Family

ID=26328728

Family Applications (3)

Application Number Title Priority Date Filing Date
ES496841A Expired ES8200122A1 (es) 1979-11-16 1980-11-14 Un metodo para la preparacion de 17,21-diesteres de 6alfa- 9alfa-didluoro-16-metil-prednisolona
ES496840A Expired ES8200121A1 (es) 1979-11-16 1980-11-14 Un metodo para la preparacion de 17,21-diesteres de 6alfa- fluoro-9alfa-cloro-prednisolona
ES496839A Granted ES496839A0 (es) 1979-11-16 1980-11-14 Un metodo para la preparacion de 17,21-diesteres de 6alfa- fluoro-prednisolona

Family Applications Before (2)

Application Number Title Priority Date Filing Date
ES496841A Expired ES8200122A1 (es) 1979-11-16 1980-11-14 Un metodo para la preparacion de 17,21-diesteres de 6alfa- 9alfa-didluoro-16-metil-prednisolona
ES496840A Expired ES8200121A1 (es) 1979-11-16 1980-11-14 Un metodo para la preparacion de 17,21-diesteres de 6alfa- fluoro-9alfa-cloro-prednisolona

Country Status (12)

Country Link
US (2) US4358445A (es)
EP (3) EP0029151B1 (es)
AU (3) AU530348B2 (es)
CA (3) CA1162532A (es)
DE (3) DE3069074D1 (es)
DK (3) DK487680A (es)
ES (3) ES8200122A1 (es)
FI (3) FI69474C (es)
IE (1) IE50829B1 (es)
NO (3) NO803452L (es)
PH (2) PH19406A (es)
YU (3) YU41747B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0095894A3 (en) * 1982-05-31 1985-01-02 Ohta Seiyaku Kabushiki Kaisha. 6 alpha-methylprednisolone derivatives
PT78973A (en) * 1984-07-25 1984-08-01 Joao Emerico Villax New preparation process of the 9alpha-fluoro 17,21-acylates or hidroxilades in 17 and 21 chloro-corticosteroid
US5110809A (en) * 1988-03-21 1992-05-05 Bristol-Myers Squibb Company Antifungal gel formulations
US6565885B1 (en) * 1997-09-29 2003-05-20 Inhale Therapeutic Systems, Inc. Methods of spray drying pharmaceutical compositions
US20060165606A1 (en) * 1997-09-29 2006-07-27 Nektar Therapeutics Pulmonary delivery particles comprising water insoluble or crystalline active agents
AUPQ899700A0 (en) 2000-07-25 2000-08-17 Borody, Thomas Julius Probiotic recolonisation therapy
AU2002359523A1 (en) * 2001-11-29 2003-06-17 Taro Pharmaceuticals U.S.A., Inc. Method for the preparation of 6-alpha-fluoro corticosteroids
CN101759760B (zh) * 2008-11-28 2013-02-13 天津金耀集团有限公司 一种含氟甾体激素的制备
CN101928318A (zh) * 2009-06-24 2010-12-29 天津金耀集团有限公司 一种含氟甾体激素的制备
WO2011151941A1 (ja) 2010-06-04 2011-12-08 国立大学法人東京大学 制御性ｔ細胞の増殖または集積を誘導する作用を有する組成物
ES2993669T3 (en) 2011-12-01 2025-01-03 Univ Tokyo Human-derived bacteria that induce proliferation or accumulation of regulatory t cells
WO2015006355A2 (en) * 2013-07-09 2015-01-15 Puretech Ventures, Llc Compositions containing combinations of bioactive molecules derived from microbiota for treatment of disease
CN108727458A (zh) * 2018-05-10 2018-11-02 浙江仙居仙乐药业有限公司 一种17-丙酸酯的合成方法
CN112851734B (zh) * 2019-11-27 2024-02-06 重庆华邦胜凯制药有限公司 一种二丙酸倍他米松的制备方法
CN111944002A (zh) * 2020-07-29 2020-11-17 河南利华制药有限公司 一种倍氯米松二丙酸酯中间体及制备方法

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB924931A (es) * 1958-07-09
US3499016A (en) * 1958-08-04 1970-03-03 Upjohn Co 6alpha-fluoro-16alpha-methyl derivatives of the pregnane series
GB933859A (es) * 1958-09-06 1963-08-14 Syntex S.A.
US3007923A (en) * 1959-01-22 1961-11-07 Lab Francais Chimiotherapie Process for the fluorination of 9beta, 11beta-epoxy and 5alpha, 6alpha-epoxy steroids
DE1081153B (de) * 1959-01-23 1960-05-05 Telefunken Gmbh Verfahren zur Bepastung der Emissionsschichttraeger von Flachkathoden mit Emissionsmaterial und Vorrichtung zur Durchfuehrung des Verfahrens
US3714353A (en) * 1959-08-11 1973-01-30 Upjohn Co THERAPEUTIC COMPOSITIONS COMPRISING A 6 alpha ; 9 alpha -DIFLUORO-11 beta ,17 alpha ,21-TRIHYDROXY-16 alpha -METHYL-1,4-PREGNADIENE-3,20-DIONE AND 21-ACYLATES
US3626063A (en) * 1959-08-11 1971-12-07 Upjohn Co Therapeutic compositions comprising 6-fluoro-16-methyl prednisolone, the 21 acylates and salts thereof
CH429716A (de) * 1961-06-24 1967-02-15 Vismara Francesco Spa Verfahren zur Herstellung von 17a-Acyloxy-21-hydroxy-Steroiden
GB1047518A (en) * 1963-06-11 1966-11-02 Glaxo Lab Ltd 17ª‡-monoesters of 11,17,21-trihydroxy steroid compounds
US3463852A (en) * 1966-01-14 1969-08-26 Schering Corp Treating allergies with steroids of the pregnane series
US3422193A (en) * 1966-08-11 1969-01-14 Schering Corp 17-mono esters of corticoids
IT1061787B (it) * 1967-03-01 1983-04-30 Vismara Francesco Spa Miglioramenti relativi alla preparazione di 17 benzoato di betametazone
US3784692A (en) * 1967-06-16 1974-01-08 Warner Lambert Co 17-propionate,21-ester derivatives of 6alpha,9alpha-difluoroprednisolone,compositions and use
US3780177A (en) * 1967-06-16 1973-12-18 Warner Lambert Co 17-butyrate,21-ester derivatives of 6alpha,9alpha-difluoroprednisolone,compositions and use
SE339685B (es) * 1967-06-16 1971-10-18 Warner Lambert Pharmaceutical
IT1034011B (it) * 1969-06-26 1979-09-10 Vister Vismara Terapeutici S P Processo per la prapratzione di 17 monoesteri di 17 a 21 diossisteroidi per idrolisi die corpispondenti 17 21 ortoesteri ciclici a ph control lato
DE2011559B2 (de) * 1970-03-07 1973-03-08 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur herstellung von 9alpha-chlor-11beta-hydroxysteroiden
US3691214A (en) * 1970-06-08 1972-09-12 Warner Lambert Pharmaceutical 17-valerate ester of 6alpha,9alpha-difluoroprednisolone,its compositions and use as an anti-inflammatory agent
US3857941A (en) * 1970-06-22 1974-12-31 Warner Lambert Co Pharmaceutical compositions and use of prednisolone 17-benzoate
DE2144405A1 (de) * 1971-09-04 1973-03-08 Merck Patent Gmbh Verfahren zur herstellung von estern der pregnanreihe
DE2365992C3 (de) 1972-03-09 1982-05-19 The Upjohn Co., 49001 Kalamazoo, Mich. 6α-Fluor-17,21-dihydroxy-16β-methylpregna-4,9(11)-dien-3,20-dion-17,21-diacetat und Verfahren zu dessen Herstellung
US3980778A (en) * 1973-10-25 1976-09-14 The Upjohn Company Anti-inflammatory steroid
SE418294B (sv) * 1974-03-27 1981-05-18 Plurichemie Anstalt Sett att framstella en 16alfa- eller 16beta-9alfa-klor eller -fluorsteroidester
US4018918A (en) * 1975-05-20 1977-04-19 The Upjohn Company Topical clindamycin preparations
CH611631A5 (en) 1975-07-23 1979-06-15 Ciba Geigy Ag Process for the preparation of 11,12-unsaturated 9alpha-fluorosteroids
US4036831A (en) * 1975-10-28 1977-07-19 Steroid Development Company Establishment Trimethyl siloxane steroid intermediates
LU75809A1 (es) * 1976-09-16 1978-05-12
US4261984A (en) * 1978-04-05 1981-04-14 Syntex (U.S.A.) Inc. 17β-thiocarboxylic acid esters of 3-oxo-4-halo-16β-methylandrost-4-enes
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.

Also Published As

Publication number Publication date
AU530802B2 (en) 1983-07-28
YU291180A (en) 1983-02-28
ES496840A0 (es) 1981-10-16
PH19406A (en) 1986-04-10
EP0029924B1 (en) 1984-08-15
FI803577A7 (fi) 1981-05-17
DE3069074D1 (en) 1984-10-04
CA1162533A (en) 1984-02-21
NO803452L (no) 1981-05-18
FI69474B (fi) 1985-10-31
YU291380A (en) 1983-02-28
FI803579A7 (fi) 1981-05-17
DK487480A (da) 1981-05-17
ES496841A0 (es) 1981-10-16
DK487580A (da) 1981-05-17
DE3071122D1 (en) 1985-10-31
EP0029151A3 (en) 1981-08-26
IE50829B1 (en) 1986-07-23
EP0029151A2 (en) 1981-05-27
FI803577L (fi) 1981-05-17
EP0029151B1 (en) 1985-09-25
AU6439080A (en) 1981-05-21
ES8200121A1 (es) 1981-10-16
CA1162532A (en) 1984-02-21
FI803579L (fi) 1981-05-17
US4576936A (en) 1986-03-18
US4358445A (en) 1982-11-09
FI803578L (fi) 1981-05-17
IE802379L (en) 1981-05-16
YU291280A (en) 1983-02-28
AU6438880A (en) 1981-05-21
ES496839A0 (es) 1981-10-16
ES8200122A1 (es) 1981-10-16
EP0029924A1 (en) 1981-06-10
DE3068965D1 (en) 1984-09-20
AU531292B2 (en) 1983-08-18
EP0030615A1 (en) 1981-06-24
EP0030615B1 (en) 1984-08-29
NO803450L (no) 1981-05-18
DK487680A (da) 1981-05-17
CA1162921A (en) 1984-02-28
PH17696A (en) 1984-11-08
AU6438980A (en) 1981-05-21
NO154268C (no) 1986-08-20
YU41747B (en) 1987-12-31
NO803451L (no) 1981-05-18
NO154268B (no) 1986-05-12
AU530348B2 (en) 1983-07-14
FI69474C (fi) 1986-02-10

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