AR248410A1 - Procedimiento para la preparacion de esteroides con puente 2, 19-metilenoxi y 2, 19-metilentio utiles como inhibidores de aromatasa y 19-hidroxilasa. - Google Patents

Procedimiento para la preparacion de esteroides con puente 2, 19-metilenoxi y 2, 19-metilentio utiles como inhibidores de aromatasa y 19-hidroxilasa.

Info

Publication number
AR248410A1
AR248410A1 AR90318689A AR31868990A AR248410A1 AR 248410 A1 AR248410 A1 AR 248410A1 AR 90318689 A AR90318689 A AR 90318689A AR 31868990 A AR31868990 A AR 31868990A AR 248410 A1 AR248410 A1 AR 248410A1
Authority
AR
Argentina
Prior art keywords
acid
formula
methyleneoxy
aromatase
hydroxylase inhibitors
Prior art date
Application number
AR90318689A
Other languages
English (en)
Original Assignee
Merrell Dow Pharma
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 Merrell Dow Pharma filed Critical Merrell Dow Pharma
Application granted granted Critical
Publication of AR248410A1 publication Critical patent/AR248410A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0073—Sulfur-containing hetero ring
    • C07J71/0078—Sulfur-containing hetero ring containing only sulfur
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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

Abstract

PREPARACION DE ESTEROIDES CON PUENTE 2, 19-METILENOXI Y 2, 19-METILENTIO UTILES COMO INHIBIDORES DE AROMATASA Y 19-HIDROXILASA DE FORMULA (I), DONDE A ES O'S; R ES H, =CH2 U =O, R2 ES =O, X ES =O E Y ES -OH CON LA CONDICION QUE CUANDO Y ES -OH, R NO PUEDE SER =O, SIENDO ÑI UN ENLACE SENCILLO O DOBLE; QUE COMPRENDE LAS ETAPAS: A) SOMETER UN 19-HIDROXI COMPUESTO DE FORMULA (II) A UNA REACCION CON DIISOPROPILETILAMINA Y 1-CLORO-2, 5- DIOXAHEXANO OBTENIENDOSE (III) QUE POR TRATAMIENTO CON CLORURO DE TRIMETILSILILO EN DIISOPROPILAMINA Y N-BULI DA (IV) QUE ES TRATADO CON TICL4 PARA DAR EL COMPUESTO DE FORMULA (V) QUE SE TRATA CON ACIDO EN UN EXCESO DE ETILENGLICOL Y LUEGO SUCESIVAMENTE CON A)ACIDO PERCLORICO; B) METOXIACETATO DE METILO Y DIISOPROPILAMIDURO DE LITIO; C) HIDRURO; D) CON ACIDO METACLOROPERBENZOICO EN DICLOROMETANO; E) OXIDACION DE JONES, DESHIDRATACION CON ACIDO P-TOLUENSULFONICO PARA DAR (VI) QUE SE DESHIDROGENA CON CLORANIL T-BUTANOL; F) Y LUEGO SE HACE REACCIONAR CON UNÑ ACETAL DE FORMALDEHIDO OBTENIENDOSE (VII).
AR90318689A 1989-12-20 1990-12-20 Procedimiento para la preparacion de esteroides con puente 2, 19-metilenoxi y 2, 19-metilentio utiles como inhibidores de aromatasa y 19-hidroxilasa. AR248410A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US45344189A 1989-12-20 1989-12-20

Publications (1)

Publication Number Publication Date
AR248410A1 true AR248410A1 (es) 1995-08-18

Family

ID=23800602

Family Applications (1)

Application Number Title Priority Date Filing Date
AR90318689A AR248410A1 (es) 1989-12-20 1990-12-20 Procedimiento para la preparacion de esteroides con puente 2, 19-metilenoxi y 2, 19-metilentio utiles como inhibidores de aromatasa y 19-hidroxilasa.

Country Status (20)

Country Link
EP (1) EP0434020B1 (es)
JP (1) JP2922653B2 (es)
KR (1) KR100187781B1 (es)
CN (1) CN1035768C (es)
AR (1) AR248410A1 (es)
AT (1) ATE124417T1 (es)
AU (1) AU630008B2 (es)
CA (1) CA2032311C (es)
DE (1) DE69020520T2 (es)
DK (1) DK0434020T3 (es)
ES (1) ES2076286T3 (es)
FI (1) FI107925B (es)
GR (1) GR3017136T3 (es)
HU (1) HU208024B (es)
IE (1) IE67557B1 (es)
IL (1) IL96695A (es)
NO (1) NO177676C (es)
NZ (1) NZ236473A (es)
PT (1) PT96258B (es)
ZA (1) ZA9010082B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5491136A (en) * 1989-12-20 1996-02-13 Merrell Dow Pharmaceuticals Inc. 2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase, 19-hydroxylaser inhibitors and methods of their use in the treatment of estrogen mediated disorders
US5126488A (en) * 1990-11-30 1992-06-30 Merrell Dow Pharmaceuticals Inc. 2β,19-methyleneamino bridged steroids as aromatase inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3627756A (en) * 1970-04-23 1971-12-14 Searle & Co N-dialkylaminoalkyl-n-(2{62 ,19-epoxy-5{60 -androstan-17{62 -yl)amines/formamides and 3{60 -halo derivatives thereof
US3954980A (en) * 1971-10-19 1976-05-04 Derek Harold Richard Barton Chemical compounds
US4814324A (en) * 1987-03-06 1989-03-21 Merck & Co., Inc. Sterol inhibitors of testosterone 5α-reductase

Also Published As

Publication number Publication date
NO177676C (no) 1995-11-01
CA2032311C (en) 2002-08-27
ZA9010082B (en) 1991-10-30
KR910011888A (ko) 1991-08-07
HU908299D0 (en) 1991-06-28
IL96695A (en) 1996-08-04
FI906269A0 (fi) 1990-12-19
NO177676B (no) 1995-07-24
IE67557B1 (en) 1996-04-17
JPH04128297A (ja) 1992-04-28
HUT56380A (en) 1991-08-28
EP0434020A1 (en) 1991-06-26
AU6808390A (en) 1991-10-17
DE69020520D1 (de) 1995-08-03
NZ236473A (en) 1993-04-28
JP2922653B2 (ja) 1999-07-26
HU208024B (en) 1993-07-28
CA2032311A1 (en) 1991-06-21
ES2076286T3 (es) 1995-11-01
CN1035768C (zh) 1997-09-03
FI906269A (fi) 1991-06-21
CN1052678A (zh) 1991-07-03
GR3017136T3 (en) 1995-11-30
DK0434020T3 (da) 1995-08-28
PT96258B (pt) 1998-09-30
EP0434020B1 (en) 1995-06-28
NO905494L (no) 1991-06-21
KR100187781B1 (ko) 1999-06-01
ATE124417T1 (de) 1995-07-15
NO905494D0 (no) 1990-12-19
PT96258A (pt) 1991-09-30
AU630008B2 (en) 1992-10-15
FI107925B (fi) 2001-10-31
IL96695A0 (en) 1991-09-16
DE69020520T2 (de) 1995-11-30
IE904597A1 (en) 1991-07-03

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