ES485457A1 - Procedimiento de preparacion de 6-piperidino-2,4-diaminopi- rimidina-3-oxido - Google Patents

Procedimiento de preparacion de 6-piperidino-2,4-diaminopi- rimidina-3-oxido

Info

Publication number
ES485457A1
ES485457A1 ES485457A ES485457A ES485457A1 ES 485457 A1 ES485457 A1 ES 485457A1 ES 485457 A ES485457 A ES 485457A ES 485457 A ES485457 A ES 485457A ES 485457 A1 ES485457 A1 ES 485457A1
Authority
ES
Spain
Prior art keywords
general formula
defined above
image
hal
reacting
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
ES485457A
Other languages
English (en)
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.)
Egyt Gyogyszervegyeszeti Gyar
Original Assignee
Egyt Gyogyszervegyeszeti Gyar
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 Egyt Gyogyszervegyeszeti Gyar filed Critical Egyt Gyogyszervegyeszeti Gyar
Publication of ES485457A1 publication Critical patent/ES485457A1/es
Expired 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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • 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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50—Three nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms

Landscapes

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

Abstract

Esta invención se relaciona con un nuevo procedimiento de preparación de 6-piperidino-23,4- diaminopirimidina-3-óxido de fórmula (I) **fórmula** a partir de 6-hidroxi-2,4-diaminopirimidina de fórmula (II) **fórmula** el compuesto de fórmula (I) ejerce excelentes efectos hipotensivos. Se han elaborado varios métodos para la preparación del compuesto de fórmula (I) , sin embargo, ninguno de ello proporciona un medio económico de producción a gran escala del producto deseado. Se reacciona 2, 4-diamino-6-hidroxipirimidina con oxicloruro de fósforo para obtener 2,4- diamino-6-cloropiridina con un rendimiento del 60% , haciéndose reaccionar dicho compuesto con fenol 0 2-4-diclorofenol, al 2,4-diamino-6-fenoxipirimidina resultante obtenida con un rendimiento del 40% se oxida para obtener el N-óxido respectivo , con un rendimiento del 21% y finalmente el N-óxido se trata con piperidina para obtener el producto deseado. Esta última fase de la reacción tiene lugar con un rendimiento del 45% , así, elrendimiento total del proceso, calculado para la 2,4-diamino-6-hidroxipirimidina inicial, es sólo del 2% al 2,3%
ES485457A 1978-10-27 1979-10-26 Procedimiento de preparacion de 6-piperidino-2,4-diaminopi- rimidina-3-oxido Expired ES485457A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
HU78EE2594A HU177601B (en) 1978-10-27 1978-10-27 New process for preparing 6-piperidino-2,4-diamino-pyrimidine-3-oxide

Publications (1)

Publication Number Publication Date
ES485457A1 true ES485457A1 (es) 1980-10-01

Family

ID=10995794

Family Applications (1)

Application Number Title Priority Date Filing Date
ES485457A Expired ES485457A1 (es) 1978-10-27 1979-10-26 Procedimiento de preparacion de 6-piperidino-2,4-diaminopi- rimidina-3-oxido

Country Status (14)

Country Link
JP (1) JPS5559172A (es)
AT (1) AT373246B (es)
CH (1) CH642365A5 (es)
CS (1) CS213398B2 (es)
DE (1) DE2943161A1 (es)
DK (1) DK454579A (es)
ES (1) ES485457A1 (es)
FI (1) FI793307A (es)
GB (1) GB2032434B (es)
HU (1) HU177601B (es)
PL (1) PL119712B1 (es)
SE (1) SE432596B (es)
SU (1) SU913942A3 (es)
YU (1) YU262579A (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1179344A (en) * 1981-07-15 1984-12-11 Jean-Claude Muller Process for the preparation of 6-¬3,6-dihydro-1(2h)- pyridyl| pyrimidine-3-oxides
CH649291A5 (de) * 1982-03-16 1985-05-15 Hoffmann La Roche Dicarbamate.
HU196067B (en) * 1986-07-10 1988-09-28 Richter Gedeon Vegyeszet Process for production of 6-amin-1,2-dihydro-1-hydroxi-2-imino-4-piperidin-piramidin
HU196061B (en) * 1986-07-10 1988-09-28 Richter Gedeon Vegyeszet Process for production of pirimidine-derivatives
FI864046A (fi) * 1986-10-07 1988-04-08 Farmos Oy Foerfarande foer framstaellning av en terapeutiskt aktiv foerening.
LU86960A1 (fr) * 1987-07-31 1989-03-08 Oreal Procede de preparation de piperidino-6 diamino-2,4 pyrimidine oxyde-3 et composes nouveaux
LU86958A1 (fr) * 1987-07-31 1989-03-08 Oreal Sels d'acide thiamorpholinone carboxylique et de derives de diamino-2,4 pyrimidine,leur utilisation en cosmetique et pharmacie
US4959475A (en) * 1989-01-04 1990-09-25 Lonza Ltd. Process for the production of 2,4-diamino-6-piperidinyl-pyrimidine-3-N-oxide

Also Published As

Publication number Publication date
FI793307A (fi) 1980-04-28
GB2032434B (en) 1982-11-17
DE2943161A1 (de) 1980-05-08
AT373246B (de) 1983-12-27
ATA689879A (de) 1983-05-15
HU177601B (en) 1981-11-28
SE432596B (sv) 1984-04-09
GB2032434A (en) 1980-05-08
JPS5559172A (en) 1980-05-02
YU262579A (en) 1983-01-21
SU913942A3 (en) 1982-03-15
PL219242A1 (es) 1980-06-16
DK454579A (da) 1980-04-28
CS213398B2 (en) 1982-04-09
CH642365A5 (de) 1984-04-13
PL119712B1 (en) 1982-01-30
SE7908629L (sv) 1980-04-28

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