FI77870B - Foerfarande foer framstaellning av antivirala difluorsubstituerade nukleosider och difluorkolhydrater anvaendbara som mellanprodukter vid foerfarandet. - Google Patents

Foerfarande foer framstaellning av antivirala difluorsubstituerade nukleosider och difluorkolhydrater anvaendbara som mellanprodukter vid foerfarandet. Download PDF

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Publication number
FI77870B
FI77870B FI840890A FI840890A FI77870B FI 77870 B FI77870 B FI 77870B FI 840890 A FI840890 A FI 840890A FI 840890 A FI840890 A FI 840890A FI 77870 B FI77870 B FI 77870B
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Prior art keywords
deoxy
formula
difluororibose
pyrimidin
bis
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FI840890A
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English (en)
Finnish (fi)
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FI840890A (fi
FI77870C (sv
FI840890A0 (fi
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Larry Wayne Hertel
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Lilly Co Eli
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Publication of FI77870C publication Critical patent/FI77870C/sv

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/32—Oxygen atoms
    • C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H11/00—Compounds containing saccharide radicals esterified by inorganic acids; Metal salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H5/00—Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium
    • C07H5/02—Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to halogen
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Furan Compounds (AREA)

Claims (18)

1 I 35 väri R* är som definierats i patentkravet 1. 38 7 7 8 7 0
1. Förfarande för framställning av antivirala nuk-leosider med formeln I 5 HOCH V°v8 --F
10 HO F eller farmaceutiskt godtagbara salter därav, i vilken form-el R är en basradikal med en av formlerna: ? NH2 R2 1*3 ^T"R Rl CH=CHR3
0 AJ AijJ o N O X N N ^ I i i 20 1 vilka R1 är väte, metyl, brom, fluor, klor eller jod; 2 R är hydroxi eller amino; 3
25 R är brom, klor eller jod, kännetecknat därav, att a) ett skyddat derivat av en bas som motsvarar den ovan definierade basradikalen R omsätts med en förening med formeln II
30 Y1OCH5 y°\ .F : : —-^ II ; ; 35 y2° F 12 . . väri Q är CHX, väri X är en avgäende grupp, och Y och Y oberoende av varandra är väte eller en skyddsgrupp för hydroxi, och skyddsgrupperna avlägsnas frän det erhällna 37 7 7 8 7 0 skyddade derivatet av en nukleofil med formeln I, eller b) en förening med formeln II' y1och2 5 \/0- ^ c=o F _/ II · Y20 F 10 1 2 väri Y och Y är som ovan definierats, eller ett skyddat derivat därav reduceras och den fria hydroxigruppen i den erhällna föreningen med formeln II"
15 Y1OCH- v°- ^ CHOH _/ II" 20 γ2° F utbyts mot en avgäende grupp X och de sä erhällna föreningen med formeln II behandlas säsom anförts i punkt a) .
2. Förfarande enligt patentkravet 1, k ä n n e -25 tecknat därav, att kolhydratdelen i nukleosiden med formeln I är 2-desoxi-2,2-difluoriribosyl.
3. Förfarande enligt patentkravet 1 eller 2, kännetecknat därav, att R är 0 nh2 .«V 1. eiier JL i
4. Förfarande enligt nägot av patentkraven 1 - 3, kännnetecknat därav, att R är NH_
5. Förfarande enligt nägot av patentkraven 1-3, kännetecknat därav, att man framställer 1—(5— metyl-2,4-dioxo-lH,3H-pyrimidin-l-yl)-1, 2-desoxi-2,2-di-fluorribos eller ett farmaceutiskt godtagbart sait därav. 15
6. Förfarande enligt nägot av patentkraven 1-4, kännetecknat därav, att man framställer l-(4-amino-2-oxo-lH-pyrimidin-l-yl)-2-desoxi-2,2-difluorribos eller ett farmaceutiskt godtagbart sait därav.
5 N^VRl i 10 och R* är som definierats i patentkravet 1.
7. Förfarande enligt n&got av patentkraven 1-4, 20 kännetecknat därav, att man framställer 1—(4— amino-5-jod-2-oxo-lH-pyrimidin-l-yl)-2-desoxi-2,2-difluor-ribos eller ett farmaceutiskt godtagbart sait därav.
8. Förfarande enligt nägot av patentkraven 1-3, kännetecknat därav, att man framställer 1-(2,4- 25 dioxo-5-fluor-lH,3H-pyrimidin-l-yl)-2-desoxi-2,2-difluor-ribos eller ett farmaceutiskt godtagbart sait därav.
9. Förfarande enligt patentkravet 1, punkt b), kännetecknat därav, att föreningen med formeln II" har samma konfiguration som ribos. 30
10. Förfarande enligt patentkravet 1 eller 9, kännetecknat därav, att föreningen med formeln II" är 2-desoxi-2,2-difluorribos eller ett skyddat derivat därav.
FI840890A 1983-03-10 1984-03-06 Förfarande för framställning av antivirala difluorsubstituerade nukleo sider och difluorkolhydrater användbara som mellanprodukter vid förfar andet. FI77870C (sv)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US47388383 1983-03-10
US06/473,883 US4526988A (en) 1983-03-10 1983-03-10 Difluoro antivirals and intermediate therefor

Publications (4)

Publication Number Publication Date
FI840890A0 FI840890A0 (fi) 1984-03-06
FI840890A FI840890A (fi) 1984-09-11
FI77870B true FI77870B (fi) 1989-01-31
FI77870C FI77870C (sv) 1989-05-10

Family

ID=23881409

Family Applications (1)

Application Number Title Priority Date Filing Date
FI840890A FI77870C (sv) 1983-03-10 1984-03-06 Förfarande för framställning av antivirala difluorsubstituerade nukleo sider och difluorkolhydrater användbara som mellanprodukter vid förfar andet.

Country Status (36)

Country Link
US (5) US4526988A (sv)
EP (1) EP0122707B1 (sv)
JP (2) JPS59175498A (sv)
KR (1) KR860001283B1 (sv)
AR (1) AR243533A1 (sv)
AT (1) ATE29726T1 (sv)
AU (1) AU565856B2 (sv)
BG (1) BG40814A3 (sv)
CA (2) CA1218647A (sv)
CS (1) CS246075B2 (sv)
CY (1) CY1489A (sv)
DD (1) DD216468A5 (sv)
DE (2) DE3466224D1 (sv)
DK (2) DK162529C (sv)
ES (1) ES530364A0 (sv)
FI (1) FI77870C (sv)
GB (2) GB2136425B (sv)
GR (1) GR81845B (sv)
HK (1) HK44989A (sv)
HU (1) HU193893B (sv)
IE (1) IE57071B1 (sv)
IL (2) IL80463A (sv)
KE (1) KE3874A (sv)
LU (1) LU88791I2 (sv)
MX (1) MX9203246A (sv)
MY (1) MY102025A (sv)
NL (1) NL950018I2 (sv)
NZ (1) NZ207358A (sv)
PH (2) PH23240A (sv)
PL (1) PL142437B1 (sv)
PT (1) PT78181B (sv)
RO (1) RO89963A (sv)
SG (1) SG21889G (sv)
SU (1) SU1442076A3 (sv)
UA (1) UA5955A1 (sv)
ZA (1) ZA841605B (sv)

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JPH06102655B2 (ja) 1994-12-14
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DK170647B1 (da) 1995-11-20
IL71143A (en) 1988-07-31
SU1442076A3 (ru) 1988-11-30
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PT78181B (en) 1986-08-05
US4808614A (en) 1989-02-28
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GR81845B (sv) 1984-12-12
PH23593A (en) 1989-09-11
FI77870C (sv) 1989-05-10
ES530364A0 (es) 1985-12-01
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NL950018I1 (sv) 1995-11-01
UA5955A1 (uk) 1994-12-29
DK190590A (da) 1990-08-10
BG40814A3 (en) 1987-02-16
PH23240A (en) 1989-06-06
US4692434A (en) 1987-09-08
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DD216468A5 (de) 1984-12-12
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US5118820A (en) 1992-06-02
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DK114484A (da) 1984-09-11
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DE19675003I2 (de) 2003-05-22
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US5015743A (en) 1991-05-14
US4526988A (en) 1985-07-02
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