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ES2042552T3 - Derivados de indenopirimidina. - Google Patents

Derivados de indenopirimidina.

Info

Publication number
ES2042552T3
ES2042552T3 ES87302661T ES87302661T ES2042552T3 ES 2042552 T3 ES2042552 T3 ES 2042552T3 ES 87302661 T ES87302661 T ES 87302661T ES 87302661 T ES87302661 T ES 87302661T ES 2042552 T3 ES2042552 T3 ES 2042552T3
Authority
ES
Spain
Prior art keywords
formula
compound
produce
hydrogen
hydroxy
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 - Lifetime
Application number
ES87302661T
Other languages
English (en)
Inventor
Kenneth Steven Hirsch
Charles David Jones
Eriks Victor Krumkalns
Donald Grant Saunders
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of ES2042552T3 publication Critical patent/ES2042552T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un procedimiento para preparar un compuesto de fórmula I: **fórmula** donde Y es hidrógeno, metilo, hidroxi, metoxi, cloro, uoro, o -NHCOCH3; R1 es hidrógeno, cloro, fluoro, metoxi, o tri uorometilo; y R2 y R3 son, cada uno de ellos independientemente, hidrógeno, cloro, fluoro, o trifluorometilo, que comprende: a) la deshidratación de un alfa,alfa-difenil-5 -pirimidinametanol de fórmula II **fórmula** donde R1, R2 y R3 son los definidos arriba, para producir un compuesto de fórmula I donde Y es hidrógeno; o b) la oxidación de un compuesto de fórmula I, donde Y es hidrógeno, para producir el correspondiente compuesto de fórmula I, donde Y es hidroxi; o c) la reacción de un compuesto de fórmula I, donde Y es hidroxi, con acetonitrilo y ácido metanosulfónico, para producir el correspondiente compuesto de fórmula I, donde Y es -NHCOCH3; o d) la reacción de un compuesto de fórmula I, donde Y es hidroxi, con cloruro de tionilo para producir el correspondiente compuesto de fórmula I, donde Y es cloro; o e) la reacción de un compuesto de fórmula I, donde Y es hidroxi, con trifluoruro de dietilaminoazufre para producir el correspondiente compuesto de fórmula I, donde Y es fluoro; o f ) la reacción de un compuesto de fórmula I, donde Y es cloro, con una fuente de iones metoxido para producir el correspondiente compuesto de fórmula I, donde Y es metoxi; o g) la reacción de un compuesto de fórmula I, donde Y es hidrógeno, con un agente de metilación en presencia de una base fuerte para producir el correspondiente compuesto de fórmula I donde Y es metilo.
ES87302661T 1986-03-31 1987-03-27 Derivados de indenopirimidina. Expired - Lifetime ES2042552T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US06/846,541 US4769378A (en) 1986-03-31 1986-03-31 Indenopyrimidine aromatase inhibitors

Publications (1)

Publication Number Publication Date
ES2042552T3 true ES2042552T3 (es) 1993-12-16

Family

ID=25298228

Family Applications (1)

Application Number Title Priority Date Filing Date
ES87302661T Expired - Lifetime ES2042552T3 (es) 1986-03-31 1987-03-27 Derivados de indenopirimidina.

Country Status (21)

Country Link
US (1) US4769378A (es)
EP (1) EP0240263B1 (es)
JP (1) JPH0751568B2 (es)
KR (1) KR890003838B1 (es)
CN (1) CN1013673B (es)
AR (1) AR245109A1 (es)
AT (1) ATE78251T1 (es)
AU (1) AU581809B2 (es)
CA (1) CA1265140A (es)
DE (1) DE3780338T2 (es)
DK (1) DK165245C (es)
ES (1) ES2042552T3 (es)
GR (1) GR3005204T3 (es)
HU (1) HU196379B (es)
IE (1) IE59762B1 (es)
IL (1) IL81978A (es)
NZ (1) NZ219748A (es)
PH (1) PH23398A (es)
PT (1) PT84553B (es)
SU (1) SU1470185A3 (es)
ZA (1) ZA872162B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5780465A (en) * 1997-04-03 1998-07-14 Dow Agrosciences Llc 4-substituted 5-polycyclylpyrimidine herbicides
SE0401790D0 (sv) * 2004-07-07 2004-07-07 Forskarpatent I Syd Ab Tamoxifen response in pre- and postmenopausal breast cancer patients
US7960400B2 (en) 2007-08-27 2011-06-14 Duquesne University Of The Holy Ghost Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
US7982035B2 (en) 2007-08-27 2011-07-19 Duquesne University Of The Holy Spirit Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof
WO2009125299A2 (en) * 2008-03-05 2009-10-15 Lewis James D Quick-change fishing lure system and method of using
EP2927225B1 (en) 2012-11-30 2018-10-03 LG Chem, Ltd. Novel compound and organic electronic element using same

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133922A (en) * 1964-05-19 Z-cyano-
GB956269A (en) * 1960-04-01 1964-04-22 Manuf Prod Pharma Substituted indeno-pyrimidines
US3177216A (en) * 1961-12-28 1965-04-06 Searle & Co 4-trifluoromethyl-2-thio-5h-alka[d]-pyrimidines and congeners
US3763178A (en) * 1968-09-05 1973-10-02 American Home Prod Imidazolinyl phenyl carbonyl acid addition salts and related compounds
BE795636A (fr) * 1972-02-19 1973-08-20 Schering Ag Nitroimidazolylpyrimidines, et leur procede de preparation
US3925384A (en) * 1974-10-21 1975-12-09 Squibb & Sons Inc 2-Amino-4,5-dihydro-4-arylindeno pyrimidines
US4235893A (en) * 1978-05-08 1980-11-25 Brodie Angela M Ester derivatives of 4-hydroxy-4-androstene-3,17-dione and a method for inhibiting estrogen biosynthesis
ZA84652B (en) * 1983-02-02 1985-09-25 Lilly Co Eli Aromatase inhibiting pyrimidine derivatives

Also Published As

Publication number Publication date
IL81978A (en) 1991-03-10
CA1265140A (en) 1990-01-30
ATE78251T1 (de) 1992-08-15
JPS62238275A (ja) 1987-10-19
IL81978A0 (en) 1987-10-20
CN1013673B (zh) 1991-08-28
IE59762B1 (en) 1994-03-23
NZ219748A (en) 1989-05-29
DK161187D0 (da) 1987-03-30
HUT43834A (en) 1987-12-28
DK165245C (da) 1993-03-22
EP0240263B1 (en) 1992-07-15
KR890003838B1 (ko) 1989-10-05
PH23398A (en) 1989-07-26
ZA872162B (en) 1988-10-26
DE3780338T2 (de) 1993-03-04
DE3780338D1 (de) 1992-08-20
CN87102424A (zh) 1987-10-07
IE870812L (en) 1987-09-30
KR870008857A (ko) 1987-10-21
AR245109A1 (es) 1993-12-30
DK161187A (da) 1987-10-01
GR3005204T3 (es) 1993-05-24
SU1470185A3 (ru) 1989-03-30
PT84553B (pt) 1989-11-10
EP0240263A2 (en) 1987-10-07
DK165245B (da) 1992-10-26
EP0240263A3 (en) 1988-09-28
US4769378A (en) 1988-09-06
AU581809B2 (en) 1989-03-02
PT84553A (en) 1987-04-01
AU7075287A (en) 1987-10-08
HU196379B (en) 1988-11-28
JPH0751568B2 (ja) 1995-06-05

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