CN108601760A - 艾日布林的合成中的中间体及相关的合成方法 - Google Patents

艾日布林的合成中的中间体及相关的合成方法 Download PDF

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Publication number
CN108601760A
CN108601760A CN201780010903.XA CN201780010903A CN108601760A CN 108601760 A CN108601760 A CN 108601760A CN 201780010903 A CN201780010903 A CN 201780010903A CN 108601760 A CN108601760 A CN 108601760A
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CN
China
Prior art keywords
formula
compound
salt
eribulin
aldehyde
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.)
Pending
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CN201780010903.XA
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English (en)
Chinese (zh)
Inventor
P.S.巴兰
C.E.蔡斯
F.G.方
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Sanitary Material R&d Management Co ltd
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Sanitary Material R&d Management Co ltd
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Publication of CN108601760A publication Critical patent/CN108601760A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/22—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Materials For Photolithography (AREA)
CN201780010903.XA 2016-02-12 2017-02-10 艾日布林的合成中的中间体及相关的合成方法 Pending CN108601760A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662294538P 2016-02-12 2016-02-12
US62/294538 2016-02-12
PCT/US2017/017501 WO2017139664A1 (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis

Publications (1)

Publication Number Publication Date
CN108601760A true CN108601760A (zh) 2018-09-28

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780010903.XA Pending CN108601760A (zh) 2016-02-12 2017-02-10 艾日布林的合成中的中间体及相关的合成方法

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Country Link
US (1) US10676481B2 (enExample)
EP (1) EP3413887B1 (enExample)
JP (1) JP6786610B2 (enExample)
KR (1) KR20180107243A (enExample)
CN (1) CN108601760A (enExample)
IL (1) IL260717B (enExample)
MX (1) MX377663B (enExample)
RU (1) RU2732575C2 (enExample)
SG (1) SG11201806133UA (enExample)
WO (1) WO2017139664A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110568121A (zh) * 2019-07-11 2019-12-13 山东省药学科学院 一种艾日布林及含艾日布林的制剂中有关物质的检测方法
CN115551866A (zh) * 2020-05-11 2022-12-30 研成精密化学株式会社 艾瑞布林的结晶盐

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7982060B2 (en) 2004-06-03 2011-07-19 Eisai R&D Management Co., Ltd. Intermediates for the preparation of analogs of Halichondrin B
WO2009046308A1 (en) 2007-10-03 2009-04-09 Eisai R & D Management Co., Ltd. Intermediates and methods for the synthesis of halichondrin b analogs
EP2528914B1 (en) 2010-01-26 2014-06-11 Eisai R&D Management Co., Ltd. Furo[3,2-b]pyrane derivatives useful in the synthesis of halichondrin b analogs
JP6625533B2 (ja) 2013-11-04 2019-12-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 ハリコンドリンｂの類縁体の合成において有用な大環化反応および中間体
CN105916861B (zh) 2013-12-06 2018-12-14 卫材R&D管理有限公司 可用于合成软海绵素b类似物的方法
RU2739034C2 (ru) 2015-05-07 2020-12-21 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Реакции макроциклизации и промежуточное соединение и другие фрагменты, полезные в синтезе макролидов галихондринов
CN114805322B (zh) 2016-06-30 2025-05-30 卫材R&D管理有限公司 可用于合成软海绵素大环内酯类及其类似物的普林斯反应和中间体
CN118894868A (zh) 2018-01-03 2024-11-05 卫材R&D管理有限公司 可用于合成软海绵素大环内酯及其类似物的普林斯反应和化合物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999065894A1 (en) * 1998-06-17 1999-12-23 Eisai Co., Ltd. Macrocyclic analogs and methods of their use and preparation
WO2012147900A1 (en) * 2011-04-28 2012-11-01 Eisai R&D Management Co., Ltd. Microreactor process for halichondrin b analog synthesis
WO2015066729A1 (en) * 2013-11-04 2015-05-07 Eisai R&D Management Co., Ltd. Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b
US20150158881A1 (en) * 2013-12-06 2015-06-11 Eisai R&D Management Co., Ltd. Methods useful in the synthesis of halichondrin b analogs

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU652180A1 (ru) 1975-12-16 1979-03-15 Краснодарский политехнический институт 1(Фурил-2,)-2-(2-,, формилфурил-5,, ) этилен или его метильное производное как промежуточный продукт дл синтеза фуран-2,5-дикарбоновой кислоты и способ его получени
US5436238A (en) 1992-03-12 1995-07-25 President And Fellows Of Harvard College Halichondrins and related compounds
US5338865A (en) 1992-03-12 1994-08-16 President And Fellows Of Harvard College Synthesis of halichondrin B and norhalichondrin B
GB9206244D0 (en) 1992-03-23 1992-05-06 Pharma Mar Sa Cytotoxic compound from a marine sponge
TW255880B (enExample) 1992-09-09 1995-09-01 Hoechst Ag
AU4255697A (en) 1996-09-06 1998-03-26 Eli Lilly And Company Catalytic selective sulfonylation process
US6870058B2 (en) 1996-12-03 2005-03-22 The Trustees Of The University Of Pennsylvania Compounds which mimic the chemical and biological properties of discodermolide
US6653341B1 (en) 1998-06-17 2003-11-25 Eisai Co., Ltd. Methods and compositions for use in treating cancer
US8097648B2 (en) 1998-06-17 2012-01-17 Eisai R&D Management Co., Ltd. Methods and compositions for use in treating cancer
DE10106647A1 (de) 2001-02-12 2002-08-22 Univ Hannover Ratjadon-Derivate zum Hemmen des Zellwachstums
US7982060B2 (en) 2004-06-03 2011-07-19 Eisai R&D Management Co., Ltd. Intermediates for the preparation of analogs of Halichondrin B
US20060045846A1 (en) 2004-08-30 2006-03-02 Horstmann Thomas E Reagents and methods for labeling terminal olefins
US20060154312A1 (en) 2004-12-09 2006-07-13 Sergei Agoulnik Tubulin isotype screening in cancer therapy using halichondrin B analogs
US7915457B2 (en) 2005-09-26 2011-03-29 Symrise Gmbh & Co. Kg Intramolecular Prins reaction and catalysts suitable therefor
WO2008010776A1 (en) 2006-07-21 2008-01-24 Agency For Science, Technology And Research Aigialomycin d and derivatives thereof and their use in treating cancer or malaria or a microbial infection
US8119839B2 (en) 2007-07-20 2012-02-21 Yamada Apiculture Center, Inc. Carboxylic acid and antidepressant composition containing the same as active ingredient
WO2009046308A1 (en) 2007-10-03 2009-04-09 Eisai R & D Management Co., Ltd. Intermediates and methods for the synthesis of halichondrin b analogs
BRPI0820519A2 (pt) 2007-11-16 2017-05-23 Eisai R&D Man Co Ltd intermediário para a síntese do análogo de halicondrina b e reação de dessulfonilação usada para o intermediário
SG189739A1 (en) 2008-04-04 2013-05-31 Eisai R&D Man Co Ltd Halichondrin b analogs
JP5371091B2 (ja) 2009-01-23 2013-12-18 三菱レイヨン株式会社 モノスルホン酸エステルの製造方法
EP2528914B1 (en) 2010-01-26 2014-06-11 Eisai R&D Management Co., Ltd. Furo[3,2-b]pyrane derivatives useful in the synthesis of halichondrin b analogs
US9181152B2 (en) 2011-11-30 2015-11-10 Alphora Research Inc. Process for preparation of (3R)-2,4-di-leaving group-3-methylbut-1-ene
IN2014MN02106A (enExample) 2012-03-30 2015-09-11 Alphora Res Inc
US9850254B2 (en) 2013-07-03 2017-12-26 Sandoz Ag Synthetic process for preparation of macrocyclic C1-keto analogs of Halichondrin B and intermediates useful therein including intermediates containing-SO2-(p-tolyl) groups
US10208058B2 (en) 2014-09-09 2019-02-19 Cipla Limited Process for the preparation of macrocyclic ketone analogs of halichondrin B or pharmaceutically acceptable salts and intermediates thereof
RU2739034C2 (ru) 2015-05-07 2020-12-21 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Реакции макроциклизации и промежуточное соединение и другие фрагменты, полезные в синтезе макролидов галихондринов
CN114805322B (zh) 2016-06-30 2025-05-30 卫材R&D管理有限公司 可用于合成软海绵素大环内酯类及其类似物的普林斯反应和中间体
WO2018217894A1 (en) 2017-05-24 2018-11-29 Eisai R&D Management Co., Ltd. Fluorine-labelled halichondrin derivatives and related methods of synthesis
CN118894868A (zh) 2018-01-03 2024-11-05 卫材R&D管理有限公司 可用于合成软海绵素大环内酯及其类似物的普林斯反应和化合物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999065894A1 (en) * 1998-06-17 1999-12-23 Eisai Co., Ltd. Macrocyclic analogs and methods of their use and preparation
WO2012147900A1 (en) * 2011-04-28 2012-11-01 Eisai R&D Management Co., Ltd. Microreactor process for halichondrin b analog synthesis
WO2015066729A1 (en) * 2013-11-04 2015-05-07 Eisai R&D Management Co., Ltd. Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b
US20150158881A1 (en) * 2013-12-06 2015-06-11 Eisai R&D Management Co., Ltd. Methods useful in the synthesis of halichondrin b analogs

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
HIROAKI SASAI ET AL.: "Efficient Diastereoselective and Enantioselective Nitroaldol Reactions from Prochiral Starting Materials: Utilization of La-Li-6,6"-Disubstituted BINOL Complexes as Asymmetric Catalysts", 《J. ORG. CHEM.》 *
MELVIN J. YU，ET AL.: "Atom-based enumeration: New eribulin analogues with low susceptibility to", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
YEEMAN K. RAMTOHUL ET AL.: "Synthesis and Evaluation of Keto-Glutamine Analogues as Inhibitors of Hepatitis A Virus 3C Proteinase", 《J. ORG. CHEM.》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110568121A (zh) * 2019-07-11 2019-12-13 山东省药学科学院 一种艾日布林及含艾日布林的制剂中有关物质的检测方法
CN115551866A (zh) * 2020-05-11 2022-12-30 研成精密化学株式会社 艾瑞布林的结晶盐

Also Published As

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US10676481B2 (en) 2020-06-09
EP3413887B1 (en) 2021-04-07
US20190300542A1 (en) 2019-10-03
JP6786610B2 (ja) 2020-11-18
MX2018009794A (es) 2018-12-17
EP3413887A4 (en) 2019-08-14
IL260717B (en) 2020-10-29
JP2019504839A (ja) 2019-02-21
SG11201806133UA (en) 2018-08-30
MX377663B (es) 2025-03-11
WO2017139664A1 (en) 2017-08-17
RU2018132264A (ru) 2020-03-12
RU2732575C2 (ru) 2020-09-21
WO2017139664A8 (en) 2018-07-26
EP3413887A1 (en) 2018-12-19
RU2018132264A3 (enExample) 2020-04-15
KR20180107243A (ko) 2018-10-01

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