CN114555617B - 亚磷酰胺活化剂 - Google Patents

亚磷酰胺活化剂 Download PDF

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Publication number
CN114555617B
CN114555617B CN202080072331.XA CN202080072331A CN114555617B CN 114555617 B CN114555617 B CN 114555617B CN 202080072331 A CN202080072331 A CN 202080072331A CN 114555617 B CN114555617 B CN 114555617B
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phosphoramidite
molar concentration
activator
group
synthesis
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Chinese (zh)
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CN114555617A (zh
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菊池正峰
佐野君彦
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Fujifilm Wako Pure Chemical Corp
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Fujifilm Wako Pure Chemical Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6524—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/02—Phosphorylation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/16—Esters of thiophosphoric acids or thiophosphorous acids
    • C07F9/165—Esters of thiophosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Saccharide Compounds (AREA)
CN202080072331.XA 2019-10-18 2020-10-13 亚磷酰胺活化剂 Active CN114555617B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2019190698 2019-10-18
JP2019-190698 2019-10-18
PCT/JP2020/038612 WO2021075423A1 (ja) 2019-10-18 2020-10-13 ホスホロアミダイト活性化剤

Publications (2)

Publication Number Publication Date
CN114555617A CN114555617A (zh) 2022-05-27
CN114555617B true CN114555617B (zh) 2024-03-08

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CN202080072331.XA Active CN114555617B (zh) 2019-10-18 2020-10-13 亚磷酰胺活化剂

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US (1) US12202848B2 (https=)
EP (1) EP4047004B1 (https=)
JP (1) JP7452549B2 (https=)
KR (1) KR102834624B1 (https=)
CN (1) CN114555617B (https=)
WO (1) WO2021075423A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116413359B (zh) * 2023-03-08 2025-09-16 杭州诺泰诺和生物医药科技有限公司 一种亚磷酰胺单体液相色谱快速分析方法
CN117233281B (zh) * 2023-09-14 2024-11-05 上海奥锐特生物科技有限公司 2-氰乙基-n,n,n’,n’-四异丙基亚磷酰二胺的检测方法
CN117233282B (zh) * 2023-09-14 2024-12-20 上海奥锐特生物科技有限公司 2-氰乙基-n,n,n’,n’-四异丙基亚磷酰二胺的检测方法

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5218088A (en) * 1989-11-02 1993-06-08 Purdue Research Foundation Process for preparing dithiophosphate oligonucleotide analogs via nucleoside thiophosphoramidite intermediates
CN1723216A (zh) * 2002-12-09 2006-01-18 三井化学株式会社 亚磷酰胺的制造方法
CA2642693A1 (en) * 2006-02-27 2007-08-30 Nippon Shinyaku Co., Ltd. Method for removal of nucleic acid-protecting group
CN101048423A (zh) * 2004-08-26 2007-10-03 日本新药株式会社 亚磷酰胺化合物及低聚核糖核酸的制备方法
JP2007531794A (ja) * 2004-04-05 2007-11-08 アルニラム ファーマスーティカルズ インコーポレイテッド オリゴヌクレオチドの合成および精製に使用する方法および反応試薬
CN101155821A (zh) * 2005-02-08 2008-04-02 霍尼韦尔国际公司 用于寡核苷酸合成的亚磷酰胺活化剂
CN108635367A (zh) * 2011-08-30 2018-10-12 阿斯泰克斯制药公司 地西他滨衍生物制剂
CN109311925A (zh) * 2016-05-12 2019-02-05 罗氏创新中心哥本哈根有限公司 立体限定的氧杂氮杂磷杂环戊烷亚磷酰胺单体与核苷或寡核苷酸的增强的偶联

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003269239A1 (en) * 2002-10-15 2004-05-04 Avecia Biotechnology Inc. Phosphitylation process
IL185439A0 (en) * 2005-03-04 2008-01-06 Girindus Ag Synthesis of oligonucleotides
WO2006116476A1 (en) * 2005-04-27 2006-11-02 Sigma-Aldrich Co. Activators for oligonucleotide and phosphoramidite synthesis
CA2671873C (en) * 2006-12-12 2018-10-09 Brian Stephen Sproat Oligonucleotides containing high concentrations of guanine monomers
US7723528B2 (en) * 2008-06-05 2010-05-25 Am Chemicals Llc Sulfur transfer reagents for oligonucleotide synthesis
NO2718257T3 (https=) * 2014-05-30 2018-04-14
AU2016287585B2 (en) * 2015-07-02 2020-12-17 Otsuka Pharmaceutical Co., Ltd. Lyophilized pharmaceutical compositions

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5218088A (en) * 1989-11-02 1993-06-08 Purdue Research Foundation Process for preparing dithiophosphate oligonucleotide analogs via nucleoside thiophosphoramidite intermediates
CN1723216A (zh) * 2002-12-09 2006-01-18 三井化学株式会社 亚磷酰胺的制造方法
JP2007531794A (ja) * 2004-04-05 2007-11-08 アルニラム ファーマスーティカルズ インコーポレイテッド オリゴヌクレオチドの合成および精製に使用する方法および反応試薬
CN101048423A (zh) * 2004-08-26 2007-10-03 日本新药株式会社 亚磷酰胺化合物及低聚核糖核酸的制备方法
CN101155821A (zh) * 2005-02-08 2008-04-02 霍尼韦尔国际公司 用于寡核苷酸合成的亚磷酰胺活化剂
CA2642693A1 (en) * 2006-02-27 2007-08-30 Nippon Shinyaku Co., Ltd. Method for removal of nucleic acid-protecting group
CN108635367A (zh) * 2011-08-30 2018-10-12 阿斯泰克斯制药公司 地西他滨衍生物制剂
CN109311925A (zh) * 2016-05-12 2019-02-05 罗氏创新中心哥本哈根有限公司 立体限定的氧杂氮杂磷杂环戊烷亚磷酰胺单体与核苷或寡核苷酸的增强的偶联

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Wolfgang K.-D. Brill et al..Synthesis of Deoxydinucleoside Phosphorodithioates.《J. Am. Chem. SOC.》.1991,第113卷(第10期),第3972-3980页. *
Yogesh S. Sanghvi et al..Improved Process for the Preparation of Nucleosidic Phosphoramidites Using a Safer and Cheaper Activator.《Organic Process Research & Development》.2000,第4卷第175-181页. *
文思远,王升启.寡核苷酸自动合成试剂的研究进展.《化学试剂》.2000,第22卷(第05期),第285-288,284页. *

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Publication number Publication date
EP4047004B1 (en) 2024-03-06
US20240166674A1 (en) 2024-05-23
JPWO2021075423A1 (https=) 2021-04-22
KR20220083704A (ko) 2022-06-20
CN114555617A (zh) 2022-05-27
EP4047004A1 (en) 2022-08-24
WO2021075423A1 (ja) 2021-04-22
US12202848B2 (en) 2025-01-21
EP4047004A4 (en) 2023-06-14
JP7452549B2 (ja) 2024-03-19
KR102834624B1 (ko) 2025-07-15

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