PE13899A1 - Sintesis de benzo [f] quinolinonas - Google Patents

Sintesis de benzo [f] quinolinonas

Info

Publication number
PE13899A1
PE13899A1 PE1997000959A PE00095997A PE13899A1 PE 13899 A1 PE13899 A1 PE 13899A1 PE 1997000959 A PE1997000959 A PE 1997000959A PE 00095997 A PE00095997 A PE 00095997A PE 13899 A1 PE13899 A1 PE 13899A1
Authority
PE
Peru
Prior art keywords
methyl
react
base
synthesis
reaction
Prior art date
Application number
PE1997000959A
Other languages
English (en)
Inventor
John Nmn Brennan
Christopher William Doecke
Perry Clark Heath
Uko Effiong Udodong
Leland Otto Weigel
Lawrence Edward Patterson
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE13899A1 publication Critical patent/PE13899A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
    • C07C319/20—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides by reactions not involving the formation of sulfide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/22—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Quinoline Compounds (AREA)

Abstract

SE REFIERE A LA SINTESIS DEL COMPUESTO (I), EN DONDE: R1 ES NO2-FENILO, CN-FENILO, ENTRE OTROS, DE PREFERENCIA (I) ES (+)-(4aR)-(10bR)-4-METIL-8-(4-ETIL-2-BENZOTIAZOLILTIO)-10b-METIL-1,2,3,4,4a,5,6,10b-OCTAHIDROBENZO[f]QUINOLIN-3-ONA, QUE COMPRENDE: HACER REACCIONAR UN ACETAL PROTEGIDO CON UN ALQUIL-Li Y UN REACTIVO DE TRANSFERENCIA DE AZUFRE; DESPROTEGER PARA OBTENER (II) Y HACERLO REACCIONAR CON (R)-(+)-FENETILAMINA; HACER REACCIONAR LO OBTENIDO CON UNA BASE DE Li; METILAR; HACER REACCIONAR LO OBTENIDO CON UN HALURO DE ACILO O UN ANHIDRIDO DEL ACIDO ACRILICO Y APAGAR LA REACCION CON UNA BASE PARA OBTENER (VI); COMBINAR (VI) CON UN SILANO Y CF3COOH EN AUSENCIA DE DISOLVENTE; LO OBTENIDO HACER REACCIONAR CON UN HALURO DE METILO EN UNA MEZCLA DE REACCION FORMADA POR UN DISOLVENTE Y UNA BASE FUERTE PARA OBTENER (VIII) Y OXIDARLO HASTA OBTENER SU SULFOXIDO, QUE SE HACE REACCIONAR CON UN AGENTE DE ACILACION; EL PRODUCTO DE TRANSPOSICION DE PUMMERER OBTENIDO SE HACE REACCINAR CON UN A-R1, EN DONDE A ES UN GRUPO SALIENTE, EN PRESENCIA DE UN CATALIZADOR DE TRANSFERENCIA DE FASE, UN REDUCTOR HIDRURO Y UNA BASE. TAMBIEN SE REFIERE A LOS COMPUESTOS INTERMEDIOS (II), (VI) Y (VIII) Y A LA SINTESIS DE (II) Y (VII). LOS COMPUESTOS (I) ACTUAN COMO INHIBIDORES DE LA 5O-REDUCTASA, SIENDO UTILES EN EL TRATAMIENTO DE LA CALVICIE MASCULINA
PE1997000959A 1996-10-30 1997-10-27 Sintesis de benzo [f] quinolinonas PE13899A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US2786896P 1996-10-30 1996-10-30

Publications (1)

Publication Number Publication Date
PE13899A1 true PE13899A1 (es) 1999-02-25

Family

ID=21840234

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000959A PE13899A1 (es) 1996-10-30 1997-10-27 Sintesis de benzo [f] quinolinonas

Country Status (20)

Country Link
EP (1) EP0839807A1 (es)
JP (1) JP2001504816A (es)
KR (1) KR20000052952A (es)
AR (1) AR011268A1 (es)
AU (1) AU735651B2 (es)
BR (1) BR9712711A (es)
CA (1) CA2270433A1 (es)
CO (1) CO4930266A1 (es)
EA (1) EA199900429A1 (es)
HU (1) HUP9904069A2 (es)
ID (1) ID21978A (es)
IL (1) IL129689A0 (es)
NO (1) NO992110D0 (es)
NZ (1) NZ335512A (es)
PE (1) PE13899A1 (es)
PL (1) PL333303A1 (es)
TR (1) TR199901543T2 (es)
TW (1) TW438752B (es)
WO (1) WO1998018757A1 (es)
ZA (1) ZA979612B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR200003746T2 (tr) * 1998-06-18 2002-03-21 Eli Lilly And Company Benzo [F] kinolinonlarìn sentezlenmesi
AU754604B2 (en) * 1998-07-29 2002-11-21 Merck & Co., Inc. Tricyclic compounds

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5239075A (en) * 1991-08-21 1993-08-24 Eli Lilly And Company Process for the preparation of benzo (f) quinolinones
US5574160A (en) * 1994-05-26 1996-11-12 Eli Lilly And Company Syntheis of benzoquinolinones
US5578724A (en) * 1994-09-20 1996-11-26 Eli Lilly And Company Process for preparation of benzo[f]quinolinones
TW450809B (en) * 1995-03-21 2001-08-21 Lilly Co Eli Pharmaceutical compositions for preventing or treating prostatic cancer comprising benzoquinolin-3-one derivatives
US5629007A (en) * 1995-03-21 1997-05-13 Eli Lilly And Company Method of preventing prostatic cancer development
US5635197A (en) * 1995-03-21 1997-06-03 Eli Lilly And Company Treatment and prevention of prostatic cancer metastasis
US5550134A (en) * 1995-05-10 1996-08-27 Eli Lilly And Company Methods for inhibiting bone loss

Also Published As

Publication number Publication date
NZ335512A (en) 2001-08-31
TR199901543T2 (xx) 1999-09-21
IL129689A0 (en) 2000-02-29
EP0839807A1 (en) 1998-05-06
NO992110L (no) 1999-04-30
CA2270433A1 (en) 1998-05-07
ID21978A (id) 1999-08-19
NO992110D0 (no) 1999-04-30
PL333303A1 (en) 1999-11-22
KR20000052952A (ko) 2000-08-25
CO4930266A1 (es) 2000-06-27
EA199900429A1 (ru) 1999-10-28
AR011268A1 (es) 2000-08-16
HUP9904069A2 (hu) 2000-04-28
ZA979612B (en) 1999-04-28
JP2001504816A (ja) 2001-04-10
AU735651B2 (en) 2001-07-12
BR9712711A (pt) 1999-10-26
WO1998018757A1 (en) 1998-05-07
TW438752B (en) 2001-06-07
AU4917297A (en) 1998-05-22

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FG Grant, registration
FD Application declared void or lapsed