CN110475784B - 用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基 - Google Patents

用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基 Download PDF

Info

Publication number
CN110475784B
CN110475784B CN201880022722.3A CN201880022722A CN110475784B CN 110475784 B CN110475784 B CN 110475784B CN 201880022722 A CN201880022722 A CN 201880022722A CN 110475784 B CN110475784 B CN 110475784B
Authority
CN
China
Prior art keywords
group
alkyl
aryl
amine
chiral auxiliary
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.)
Active
Application number
CN201880022722.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN110475784A (zh
Inventor
K·布莱谢尔
E·D·丰德
D·J·汉森
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.)
Roche Innovation Center Copenhagen AS
Original Assignee
Roche Innovation Center Copenhagen AS
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 Roche Innovation Center Copenhagen AS filed Critical Roche Innovation Center Copenhagen AS
Publication of CN110475784A publication Critical patent/CN110475784A/zh
Application granted granted Critical
Publication of CN110475784B publication Critical patent/CN110475784B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
    • 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
    • C07H21/04—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201880022722.3A 2017-03-29 2018-03-20 用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基 Active CN110475784B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17163506.3 2017-03-29
EP17163506 2017-03-29
PCT/EP2018/057069 WO2018177825A1 (en) 2017-03-29 2018-03-20 Orthogonal protecting groups for the preparation of stereodefined phosphorothioate oligonucleotides

Publications (2)

Publication Number Publication Date
CN110475784A CN110475784A (zh) 2019-11-19
CN110475784B true CN110475784B (zh) 2024-07-16

Family

ID=61899189

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880022722.3A Active CN110475784B (zh) 2017-03-29 2018-03-20 用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基

Country Status (6)

Country Link
US (1) US11591362B2 (https=)
EP (1) EP3601309A1 (https=)
JP (1) JP7164540B2 (https=)
KR (1) KR20190135494A (https=)
CN (1) CN110475784B (https=)
WO (1) WO2018177825A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019002237A1 (en) * 2017-06-28 2019-01-03 Roche Innovation Center Copenhagen A/S METHOD OF MULTIPLE COUPLING AND OXIDATION
PT3717646T (pt) 2017-12-01 2025-07-28 Texas A & M Univ Sys Tratamento antisense da síndrome de angelman
EP3883941A1 (en) * 2018-11-22 2021-09-29 Roche Innovation Center Copenhagen A/S Pyridinium salts as activators in the synthesis of stereodefined oligonucleotides
CN113748116A (zh) 2019-03-20 2021-12-03 波涛生命科学有限公司 可用于寡核苷酸制备的技术
CN113661168A (zh) * 2019-04-16 2021-11-16 罗氏创新中心哥本哈根有限公司 用于制备核苷酸p(v)单体的新方法
CN116867795A (zh) * 2021-02-01 2023-10-10 第一三共株式会社 抗体－免疫刺激剂偶联物的新型制造方法
TW202241454A (zh) * 2021-02-01 2022-11-01 日商第一三共股份有限公司 抗體－免疫賦活化劑共軛物之新穎製造方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104661664A (zh) * 2012-07-13 2015-05-27 威尔生命科学私人有限公司 手性控制

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6465628B1 (en) 1999-02-04 2002-10-15 Isis Pharmaceuticals, Inc. Process for the synthesis of oligomeric compounds
US6492171B2 (en) 2000-05-16 2002-12-10 Isis Pharmaceuticals, Inc. Antisense modulation of TERT expression
WO2005092909A1 (ja) 2004-03-25 2005-10-06 Toudai Tlo, Ltd. 立体規則性の高いリボヌクレオチド類縁体及びデオキシリボヌクレオチド類縁体の製造法
JP5342881B2 (ja) 2006-01-27 2013-11-13 アイシス ファーマシューティカルズ， インコーポレーテッド ６−修飾された二環式核酸類似体
CA2648132C (en) 2006-04-03 2019-05-28 Santaris Pharma A/S Pharmaceutical composition comprising anti-mirna antisense oligonucleotides
EP2623599B1 (en) 2007-10-04 2019-01-02 Roche Innovation Center Copenhagen A/S Micromirs
DK2285819T3 (da) 2008-04-04 2013-12-02 Isis Pharmaceuticals Inc Oligomere forbindelser omfattende neutralt bundne, terminale bicykliske nukleosider
WO2010036698A1 (en) 2008-09-24 2010-04-01 Isis Pharmaceuticals, Inc. Substituted alpha-l-bicyclic nucleosides
RU2572826C2 (ru) * 2008-12-02 2016-01-20 Чиралджен, Лтд. Способ синтеза модифицированных по атому фосфора нуклеиновых кислот
CA2767253A1 (en) 2009-07-06 2011-01-13 Ontorii, Inc. Novel nucleic acid prodrugs and methods of use thereof
JP5868324B2 (ja) 2010-09-24 2016-02-24 株式会社Wave Life Sciences Japan 不斉補助基
WO2017157672A1 (en) 2016-03-18 2017-09-21 Roche Innovation Center Copenhagen A/S Acyl-protected l-lna-guanosine monomers
CN109311925B (zh) 2016-05-12 2022-06-03 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
US10882884B2 (en) * 2016-05-18 2021-01-05 Eth Zurich Stereoselective synthesis of phosphorothioate oligoribonucleotides

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104661664A (zh) * 2012-07-13 2015-05-27 威尔生命科学私人有限公司 手性控制

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Solid-Phase Synthesis of Stereoregular Oligodeoxyribonucleoside Phosphorothioates Using Bicyclic Oxazaphospholidine Derivatives as Monomer Units;Natsuhisa Oka, et al.;《Journal of the American Chemical Society》;20081231;第130卷(第47期);第16031-16037 *

Also Published As

Publication number Publication date
JP2020512360A (ja) 2020-04-23
CN110475784A (zh) 2019-11-19
US11591362B2 (en) 2023-02-28
KR20190135494A (ko) 2019-12-06
US20210179658A1 (en) 2021-06-17
EP3601309A1 (en) 2020-02-05
JP7164540B2 (ja) 2022-11-01
WO2018177825A1 (en) 2018-10-04

Similar Documents

Publication Publication Date Title
CN110475784B (zh) 用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基
JP7492829B2 (ja) 多重カップリングおよび酸化の方法
JP7097820B2 (ja) ヌクレオシドまたはオリゴヌクレオチドへの、立体的に規定されたオキサザホスホリジンホスホルアミダイト単量体のカップリングの増大法
JP7017517B2 (ja) アシル保護ｌ－ｌｎａ－グアノシンモノマー
WO2000020431A1 (en) Improved process for oligonucleotide synthesis
JP7198768B2 (ja) ＵｎｙＬｉｎｋｅｒ迅速切断方法
JP7759323B2 (ja) 核酸オリゴマーの製造方法
JP7698631B2 (ja) 核酸オリゴマーの製造方法
KR20250042734A (ko) 올리고뉴클레오티드의 제조 방법
HK40017810A (en) Orthogonal protecting groups for the preparation of stereodefined phosphorothioate oligonucleotides
HK40017810B (zh) 用於制备立体限定硫代磷酸酯寡核苷酸的正交保护基
HK40016121A (en) Unylinker rapid cleavage
HK40022416A (en) Multiple coupling & oxidation method
HK40022416B (zh) 多重偶联和氧化方法
HK40003927B (en) Enhanced coupling of stereodefined oxazaphospholidine phosphoramidite monomers to nucleoside or oligonucleotide
HK40003927A (en) Enhanced coupling of stereodefined oxazaphospholidine phosphoramidite monomers to nucleoside or oligonucleotide

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40017810

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
TG01 Patent term adjustment
TG01 Patent term adjustment