ES8502612A1 - Procedimiento para la preparacion de 13a-alquilgonanos - Google Patents

Procedimiento para la preparacion de 13a-alquilgonanos

Info

Publication number
ES8502612A1
ES8502612A1 ES533260A ES533260A ES8502612A1 ES 8502612 A1 ES8502612 A1 ES 8502612A1 ES 533260 A ES533260 A ES 533260A ES 533260 A ES533260 A ES 533260A ES 8502612 A1 ES8502612 A1 ES 8502612A1
Authority
ES
Spain
Prior art keywords
carbon atoms
alkyl
hydrogen
alpha
beta
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
ES533260A
Other languages
English (en)
Other versions
ES533260A0 (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.)
Bayer Pharma AG
Original Assignee
Schering 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
Priority claimed from DE3321826A external-priority patent/DE3321826A1/de
Priority claimed from DE19843413036 external-priority patent/DE3413036A1/de
Application filed by Schering AG filed Critical Schering AG
Publication of ES533260A0 publication Critical patent/ES533260A0/es
Publication of ES8502612A1 publication Critical patent/ES8502612A1/es
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal 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
    • C07J41/0083Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

PROCEDIMIENTO PARA LA PREPARACION DE 13 BAB-ALQUILGONANOS.CONSISTENTE EN SOMETER A LUZ ULTRAVIOLETA DE UNA LAMPARA DE MERCURIO A ALTA PRESION Y EN UN APARATO DE CRISTAL DE CUARZO A 25JC: 1) EL COMPUESTO DE FORMULA (II), DONDE R1 ES RI-N-RII, CON RI Y RII COMO H, ALQUILO 1-4C O RI-N-RII ES UN ANILLO SATURADO DE 5-6 MIEMBROS, PUDIENDO LLEVAR ADEMAS DE N HETEROATOMO DE O, N O S Y OTROS; RII ES H, METILO O ETILO; R5 ES H, ALQUILO EN POSICION BAB O BBB DE C 1 A 4, Z ES ETILENO O 2-2 DIMETILPROPILENO; O 2) EL COMPUESTO DE FORMULA (II) SE TRANSFORMA POR REACCION DE ADICION NUCLEOFILA CON LA 17-CETONA, DESDOBLAMIENTO DE LA PROTECCION POR 3-CETAL Y SEPARACION DE AGUA DE POSICION 4,5 DE FORMULA (I) PARA OBTENER: A) 13 BAB-ALQUILGONANOS DE FORMULA (I) Y R3 ES -(CH2)N-CH3, CON N F 0-4 U OTROS Y R4 ES HIDROXI, ALQUILOXI U OTROS.
ES533260A 1983-06-15 1984-06-08 Procedimiento para la preparacion de 13a-alquilgonanos Expired ES8502612A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3321826A DE3321826A1 (de) 1983-06-15 1983-06-15 13(alpha)-alkylgonane, deren herstellung und diese enthaltende pharmazeutische praeparate
DE19843413036 DE3413036A1 (de) 1984-04-04 1984-04-04 13(alpha)-alkylgonane, deren herstellung und diese enthaltende pharmazeutische praeparate

Publications (2)

Publication Number Publication Date
ES533260A0 ES533260A0 (es) 1985-02-01
ES8502612A1 true ES8502612A1 (es) 1985-02-01

Family

ID=25811539

Family Applications (1)

Application Number Title Priority Date Filing Date
ES533260A Expired ES8502612A1 (es) 1983-06-15 1984-06-08 Procedimiento para la preparacion de 13a-alquilgonanos

Country Status (16)

Country Link
EP (1) EP0129499B1 (es)
JP (1) JPH02167296A (es)
AU (1) AU572849B2 (es)
CA (1) CA1307784C (es)
DD (1) DD218624A5 (es)
DE (1) DE3468030D1 (es)
DK (1) DK166729B1 (es)
ES (1) ES8502612A1 (es)
FI (1) FI78709C (es)
GR (1) GR82210B (es)
HU (1) HU191131B (es)
IE (1) IE57620B1 (es)
IL (1) IL72085A (es)
NO (1) NO160521C (es)
NZ (1) NZ208441A (es)
PT (1) PT78732B (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3446661A1 (de) * 1984-12-18 1986-06-19 Schering AG, 1000 Berlin und 4709 Bergkamen Neue 13(alpha)-alkyl-17(beta)-(3-acyloxypropyl)-gonane
DE3506785A1 (de) * 1985-02-22 1986-08-28 Schering AG, Berlin und Bergkamen, 1000 Berlin 11ss-n,n-dimethylaminophenyl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate
DE3630030A1 (de) * 1986-09-01 1988-03-03 Schering Ag 13(alpha)-alkylgonan-(delta)(pfeil hoch)9(pfeil hoch)(pfeil hoch)((pfeil hoch)(pfeil hoch)1(pfeil hoch)1(pfeil hoch))(pfeil hoch)-5,10-epoxide
US4774236A (en) * 1986-09-17 1988-09-27 Research Triangle Institute 17α-(substituted-methyl)-17β-hydroxy/esterified hydroxy steroids and pharmaceutical compositions containing them
IE60780B1 (en) * 1987-01-23 1994-08-10 Akzo Nv New 11-aryl steroid derivatives
EP0310542B1 (de) * 1987-10-01 1994-06-08 Schering Aktiengesellschaft Antigestagen- und antiöstrogenwirksame Verbindungen zur Behandlung hormonabhängiger Tumoren
JP2785023B2 (ja) * 1987-12-30 1998-08-13 ルセル―ユクラフ 17α位置を置換された17β―OH―19―ノルステロイドの新誘導体、その製造方法、その薬剤としての使用及びそれを含有する製薬組成物
US4954490A (en) * 1988-06-23 1990-09-04 Research Triangle Institute 11 β-substituted progesterone analogs
DE3822770A1 (de) * 1988-07-01 1990-01-04 Schering Ag 13-alkyl-11ss-phenylgonane
DE3832303A1 (de) * 1988-09-20 1990-04-12 Schering Ag 11ss-phenyl-14ssh-steroide
US5372996A (en) * 1989-03-10 1994-12-13 Endorecherche, Inc. Method of treatment of androgen-related diseases
US5364847A (en) * 1989-03-10 1994-11-15 Endorecherche Inhibitors of sex steroid biosynthesis and methods for their production and use
KR0181264B1 (ko) * 1989-07-07 1999-03-20 라브리 페르낭 성스테로이드 활성 억제용 안드로겐 유도체
DK0595796T3 (da) * 1989-07-07 2003-05-05 Endorech Inc Fremgangsmåde til behandling af androgen-relaterede sygdomme
EP0411733B1 (de) * 1989-08-04 1998-10-21 Schering Aktiengesellschaft 11 Beta-Aryl-gona-4,9-dien-3-one
FR2654337B1 (fr) * 1989-11-15 1994-08-05 Roussel Uclaf Nouvelles microspheres injectables biodegradables procede de preparation et suspensions injectables les renfermant.
DE4008584A1 (de) * 1990-03-15 1991-09-26 Schering Ag Verfahren zur herstellung von zwischenprodukten fuer die antigestagensynthese (onapristonsynthese)
US5407928A (en) * 1990-08-15 1995-04-18 Schering Aktiengesellschaft 11β-aryl-gona-4,9-dien-3-ones
US5472854A (en) * 1990-08-18 1995-12-05 Schering Aktiengesellschaft Process for the production of 17-oxosteroids via the fermentative oxidation of 17β-hydroxysteroids by Mycobacterium
RU2082762C1 (ru) * 1990-08-18 1997-06-27 Шеринг АГ Берлин унд Бергкамен Способ получения 17-оксостероидов
US7704983B1 (en) 1992-03-02 2010-04-27 Eastern Virginia Medical School Antiprogestin method for reducing side effects associated with low dosage HRT and oral contraception
MX9301121A (es) 1992-03-02 1993-09-01 Schering Ag Metodo y equipo para la contracepcion oral y regulacion de la menstruacion con estrogeno/progestina/aniprogestina.
US5439913A (en) 1992-05-12 1995-08-08 Schering Aktiengesellschaft Contraception method using competitive progesterone antagonists and novel compounds useful therein
UA35589C2 (uk) * 1992-05-21 2001-04-16 Андорешерш Інк. ІНГІБІТОРИ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ІНГІБУВАННЯ АКТИВНОСТІ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ
DE4413185A1 (de) * 1994-04-12 1995-10-19 Schering Ag 11beta,19-überbrückte 13alpha-Alkylsteroide
DE4415590A1 (de) * 1994-04-28 1995-11-02 Schering Ag Verfahren zur stereoselektiven Einführung einer Alkinylseitenkette an 11ß-Aryl-substituierten 13alpha-Alkylgonan-17-onen
DE4434488A1 (de) * 1994-09-14 1996-03-21 Schering Ag Steroidester und -amide, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
ZA9510926B (en) 1994-12-23 1996-07-03 Schering Ag Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception
US6900193B1 (en) 1996-05-01 2005-05-31 The United States Of America As Represented By The Department Of Health And Human Services Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
ES2152671T3 (es) 1996-05-01 2001-02-01 Us Gov Health & Human Serv Derivados de progesterona sustituidos en posicion 21 como nuevos agentes antiprogestacionales.
CA2966753A1 (en) 2014-11-17 2016-05-26 Arno Therapeutics, Inc. Onapristone extended-release compositions and methods
CA2998924A1 (en) 2015-09-25 2017-03-30 Context Biopharma Inc. Methods of making onapristone intermediates
US10548905B2 (en) 2015-12-15 2020-02-04 Context Biopharma Inc. Amorphous onapristone compositions and methods of making the same
US20180148471A1 (en) 2016-11-30 2018-05-31 Arno Therapeutics, Inc. Methods for onapristone synthesis dehydration and deprotection

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2377418A1 (fr) * 1977-01-13 1978-08-11 Roussel Uclaf Nouveaux derives steroides 4,9-dieniques 11b-substitues, leur procede de preparation et leur application comme medicaments
ZA8231B (en) * 1981-01-09 1982-11-24 Roussel Uclaf New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained
DE3347126A1 (de) * 1983-12-22 1985-07-11 Schering AG, 1000 Berlin und 4709 Bergkamen 11ss-aryl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate
CA1304916C (en) * 1984-10-18 1992-07-14 Wilhelm Bannwarth Apparatus for the parallel performance of a plurality of chemical reaction sequences

Also Published As

Publication number Publication date
JPH0369919B2 (es) 1991-11-05
IE841484L (en) 1984-12-15
ES533260A0 (es) 1985-02-01
DK166729B1 (da) 1993-07-05
DD218624A5 (de) 1985-02-13
HU191131B (en) 1987-01-28
NO842394L (no) 1984-12-17
DK288184D0 (da) 1984-06-12
FI78709C (fi) 1989-09-11
EP0129499A2 (de) 1984-12-27
PT78732A (pt) 1985-01-01
DE3468030D1 (en) 1988-01-21
PT78732B (de) 1986-06-03
NO160521C (no) 1989-04-26
EP0129499A3 (en) 1985-10-09
GR82210B (es) 1984-12-13
DK288184A (da) 1984-12-16
NZ208441A (en) 1988-01-08
EP0129499B1 (de) 1987-12-09
HUT36139A (en) 1985-08-28
AU572849B2 (en) 1988-05-19
IE57620B1 (en) 1993-02-10
FI842395A (fi) 1984-12-16
FI78709B (fi) 1989-05-31
JPH02167296A (ja) 1990-06-27
AU2936184A (en) 1984-12-20
IL72085A0 (en) 1984-10-31
FI842395A0 (fi) 1984-06-13
IL72085A (en) 1987-09-16
NO160521B (no) 1989-01-16
CA1307784C (en) 1992-09-22

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