CN115667279A - 3’n核苷通过肟中间体的合成以及相关化合物 - Google Patents

3’n核苷通过肟中间体的合成以及相关化合物 Download PDF

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Publication number
CN115667279A
CN115667279A CN202180036016.6A CN202180036016A CN115667279A CN 115667279 A CN115667279 A CN 115667279A CN 202180036016 A CN202180036016 A CN 202180036016A CN 115667279 A CN115667279 A CN 115667279A
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S·格里亚兹诺夫
V·K·拉杰万希
I·N·侯皮斯
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Jensen Biopharmaceutical Co ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
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    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/167Purine radicals with ribosyl as the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/067Pyrimidine radicals with ribosyl as the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/20Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
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    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/111General methods applicable to biologically active non-coding nucleic acids
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/10Type of nucleic acid
    • C12N2310/11Antisense
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/10Type of nucleic acid
    • C12N2310/14Type of nucleic acid interfering nucleic acids [NA]
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2330/00Production
    • C12N2330/30Production chemically synthesised

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Saccharide Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN202180036016.6A 2020-03-16 2021-03-15 3’n核苷通过肟中间体的合成以及相关化合物 Pending CN115667279A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062990361P 2020-03-16 2020-03-16
US62/990361 2020-03-16
PCT/IB2021/052141 WO2021186328A1 (en) 2020-03-16 2021-03-15 Synthesis of 3'n nucleosides through oxime intermediates and related compounds

Publications (1)

Publication Number Publication Date
CN115667279A true CN115667279A (zh) 2023-01-31

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CN202180036016.6A Pending CN115667279A (zh) 2020-03-16 2021-03-15 3’n核苷通过肟中间体的合成以及相关化合物

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US (1) US20230203078A1 (https=)
EP (1) EP4121435A1 (https=)
JP (1) JP2023517735A (https=)
KR (1) KR20220154788A (https=)
CN (1) CN115667279A (https=)
AU (1) AU2021237843A1 (https=)
CA (1) CA3176112A1 (https=)
IL (1) IL296530A (https=)
MX (1) MX2022011552A (https=)
WO (1) WO2021186328A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117343111A (zh) * 2023-12-04 2024-01-05 康羽生命科学技术(苏州)有限公司 核苷修饰物n2-异丁酰-2'-甲氧基鸟苷的制备方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115851855A (zh) 2022-08-24 2023-03-28 凯莱英医药集团(天津)股份有限公司 酶催化合成嘌呤核苷的方法及组合物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1436082A (zh) * 2000-04-13 2003-08-13 法玛塞特有限公司 用于治疗肝炎病毒感染的3′-或2′-羟甲基取代的核苷衍生物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1436082A (zh) * 2000-04-13 2003-08-13 法玛塞特有限公司 用于治疗肝炎病毒感染的3′-或2′-羟甲基取代的核苷衍生物

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
AHMED KHALIL ET AL.: ""Synthesis of 2’, 3’-Dideoxy-2’-fluoro-3’-(hydroxyimino)-, -3’-(methoxyimino)- and -3’-(hydroxyamino)pyrimidine Nucleosides"", 《EUR. J. ORG. CHEM.》, vol. 2012, no. 16, 1 June 2012 (2012-06-01), pages 3172 - 3179, XP055817673, DOI: 10.1002/ejoc.201200119 *
AKIRA OGAWA ET AL.: ""Nucleosides and Nucleotides. 180. Synthesis and Antitumor Activity of Nucleosides That Have a Hydroxylamino Group Instead of a Hydroxyl Group at the 2’- or 3’-Position of the Sugar Moiety"", 《J. MED. CHEM.》, vol. 41, 6 November 1998 (1998-11-06), pages 5094 - 5107, XP055817659, DOI: 10.1021/jm980466g *
N. HOSSAIN ET AL.: ""Synthesis of 2′, 3′-Dideoxy-3′-nitro-2′, 3′-didehydrothymidine. Its Use as a General Intermediate for the Preparation of Various 2′, 3′-Substituted Nucleosides"", 《NUCLEOSIDES & NUCLEOTIDES》, vol. 12, no. 5, 1 June 1993 (1993-06-01), pages 499 - 528, XP055817796, DOI: 10.1080/07328319308021219 *
NAOSHI KOJIMA ET AL.: ""Synthesis of ribonucleic guanidine: replacement of the negative phosphodiester linkages of RNA with positive guanidinium linkages"", 《TETRAHEDRON》, vol. 58, 31 December 2002 (2002-12-31), pages 867 - 879, XP004332709, DOI: 10.1016/S0040-4020(01)01185-1 *
SONGQING WANG ET AL.: ""Synthesis of Potentially Antiviral 2, 3-Dideoxy-2-fluoro-3 -(hydroxyamino)nucleosides"", 《HELVETICA CHIMICA ACTA》, vol. 87, no. 2, 1 February 2004 (2004-02-01), pages 327 - 339, XP055817791, DOI: 10.1002/hlca.200490030 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117343111A (zh) * 2023-12-04 2024-01-05 康羽生命科学技术(苏州)有限公司 核苷修饰物n2-异丁酰-2'-甲氧基鸟苷的制备方法
CN117343111B (zh) * 2023-12-04 2024-02-06 康羽生命科学技术(苏州)有限公司 核苷修饰物n2-异丁酰-2'-甲氧基鸟苷的制备方法

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AU2021237843A1 (en) 2022-10-20
CA3176112A1 (en) 2021-09-23
IL296530A (en) 2022-11-01
KR20220154788A (ko) 2022-11-22
WO2021186328A1 (en) 2021-09-23
US20230203078A1 (en) 2023-06-29
EP4121435A1 (en) 2023-01-25
JP2023517735A (ja) 2023-04-26
MX2022011552A (es) 2023-01-04

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