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AR014944A1 - Proceso para la sintesis de azaesteroides e intermediarios y compuestos intermediarios - Google Patents

Proceso para la sintesis de azaesteroides e intermediarios y compuestos intermediarios

Info

Publication number
AR014944A1
AR014944A1 ARP980106605A ARP980106605A AR014944A1 AR 014944 A1 AR014944 A1 AR 014944A1 AR P980106605 A ARP980106605 A AR P980106605A AR P980106605 A ARP980106605 A AR P980106605A AR 014944 A1 AR014944 A1 AR 014944A1
Authority
AR
Argentina
Prior art keywords
ring
azaesteroids
synthesis
intermediaries
heteroaromatic ring
Prior art date
Application number
ARP980106605A
Other languages
English (en)
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR014944A1 publication Critical patent/AR014944A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/185—Saturated compounds having only one carboxyl group and containing keto groups
    • C07C59/205—Saturated compounds having only one carboxyl group and containing keto groups containing rings
    • 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
    • A61P5/28—Antiandrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Un proceso para la síntesis de azaesteroides e intermediarios de formula estructural (11) en donde: Ar es fenilo no sustituido o mono- o di-sustituido,naftilo, o anillo heteroaromático de 5, 6 o 7 miembros que contiene por lo menos un miembro seleccionado entre el grupo que consiste en: un átomo de oxígeno enel anillo, un átomo de azufre en el anillo, 1-4 átomos de nitrogeno en el anillo, o combinaciones de los mismos; en donde el anillo heteroaromático tambiénpuede ser fusionado con un anillo benzo o heteroaromático; que comprende tratar un compuesto de formula estructural (10) con t-butoxido de potasio y aislandoel producto resultante (11) y un compuesto de acuerdo con la reinvindicacion 1 a 14, que es seleccionado entre formulas (1) a (10).
ARP980106605A 1997-12-23 1998-12-22 Proceso para la sintesis de azaesteroides e intermediarios y compuestos intermediarios AR014944A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US6853697P 1997-12-23 1997-12-23

Publications (1)

Publication Number Publication Date
AR014944A1 true AR014944A1 (es) 2001-04-11

Family

ID=22083194

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980106605A AR014944A1 (es) 1997-12-23 1998-12-22 Proceso para la sintesis de azaesteroides e intermediarios y compuestos intermediarios

Country Status (10)

Country Link
US (1) US6187925B1 (es)
EP (1) EP1042356A2 (es)
AR (1) AR014944A1 (es)
AU (1) AU2306799A (es)
EA (1) EA002333B1 (es)
EE (1) EE200000357A (es)
IS (1) IS5507A (es)
TR (1) TR200001969T2 (es)
TW (1) TW548276B (es)
WO (1) WO1999032507A2 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR016257A1 (es) * 1998-05-14 2001-06-20 Merck & Co Inc Proceso para la sintesis estereoselectiva de ariloxi-4-aza-5alfa-androstan-3-onas, 16 alfa y 16 beta-sustituidas e insustituidas, e intermediariosobtenidos en dicho proceso.
NO20031736D0 (no) * 2003-04-15 2003-04-15 Amersham Health As Forbindelser

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2759952A (en) 1955-08-01 1956-08-21 Lasdon Foundation Inc Cyclopentano-phenanthrene compounds
GB813845A (en) 1955-08-01 1959-05-27 Lasdon Foundation Inc Improvements in cyclopentanophenanthrene compounds
US4377584A (en) 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
US4760071A (en) 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
DK0474666T3 (da) 1989-05-30 1995-02-06 Upjohn Co Oxidativ fremstilling af A-nor-17-beta-carboxy-3,5-seco-androstan-5-on-syre
US5021575A (en) 1989-11-13 1991-06-04 Merck & Co., Inc. Method for introducing a 1,2 double bond into azasteroids
US5091534A (en) 1990-08-27 1992-02-25 Merck & Co., Inc. Trialkylsilyl trifluoromethanesulfonate mediated α-methylenic carbon functionalization of 4-AZA-5α-androstan-3-one steroids
US5120847A (en) 1990-08-27 1992-06-09 Merck & Co., Inc. Process for iodinating or brominating the α-methylenic carbon of a secondary amide
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
US5237064A (en) 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
CN1058499C (zh) * 1993-10-21 2000-11-15 麦克公司 １６－取代－４－氮杂－雄甾烷－５α－还原酶同工酶１抑制剂
SK282278B6 (sk) 1994-05-19 2002-01-07 Merck & Co., Inc. Spôsob oxidácie delta-5-steroidného alkénu
US5470976A (en) 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
DE69713285T2 (de) 1996-02-14 2003-01-02 Aventis Pharmaceuticals Inc., Bridgewater 17-beta-cyclopropyl(amino/oxy)4-aza steroide als testosterone 5-alpha-rectase und c17-20-lyase hemmende verbindungen

Also Published As

Publication number Publication date
TR200001969T2 (tr) 2000-12-21
EP1042356A2 (en) 2000-10-11
EA002333B1 (ru) 2002-04-25
US6187925B1 (en) 2001-02-13
WO1999032507A3 (en) 1999-09-10
IS5507A (is) 2000-05-23
WO1999032507A2 (en) 1999-07-01
AU2306799A (en) 1999-07-12
TW548276B (en) 2003-08-21
EE200000357A (et) 2001-12-17
EA200000705A1 (ru) 2000-12-25

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