JP6978758B2 - パラジウム媒介ケトール化 - Google Patents

パラジウム媒介ケトール化 Download PDF

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Publication number
JP6978758B2
JP6978758B2 JP2016221064A JP2016221064A JP6978758B2 JP 6978758 B2 JP6978758 B2 JP 6978758B2 JP 2016221064 A JP2016221064 A JP 2016221064A JP 2016221064 A JP2016221064 A JP 2016221064A JP 6978758 B2 JP6978758 B2 JP 6978758B2
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alkyl
alkynyl
optionally substituted
alkenyl
hydrogen
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JP2018108937A (ja
JP2018108937A5 (enExample
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イー，ジョンファ
義人 岸
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Harvard University
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Harvard University
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Priority to US16/459,120 priority patent/US10844073B2/en
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    • 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
    • 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
    • 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
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • C07D307/20—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • 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
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
JP2016221064A 2016-11-11 2016-11-11 パラジウム媒介ケトール化 Active JP6978758B2 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2016221064A JP6978758B2 (ja) 2016-11-11 2016-11-11 パラジウム媒介ケトール化
US15/809,845 US10392400B2 (en) 2016-11-11 2017-11-10 Palladium-mediated ketolization
US16/459,120 US10844073B2 (en) 2016-11-11 2019-07-01 Palladium-mediated ketolization

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2016221064A JP6978758B2 (ja) 2016-11-11 2016-11-11 パラジウム媒介ケトール化

Publications (3)

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JP2018108937A JP2018108937A (ja) 2018-07-12
JP2018108937A5 JP2018108937A5 (enExample) 2019-12-26
JP6978758B2 true JP6978758B2 (ja) 2021-12-08

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US (2) US10392400B2 (enExample)
JP (1) JP6978758B2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017520586A (ja) 2014-06-30 2017-07-27 プレジデント アンド フェローズ オブ ハーバード カレッジ ハリコンドリン類似体の合成およびその使用
WO2016176560A1 (en) 2015-04-30 2016-11-03 President And Fellows Of Harvard College Chromium-mediated coupling and application to the synthesis of halichondrins
JP6978758B2 (ja) 2016-11-11 2021-12-08 プレジデント アンド フェローズ オブ ハーバード カレッジ パラジウム媒介ケトール化
HRP20221385T1 (hr) 2017-04-05 2023-01-06 President And Fellows Of Harvard College Makrociklički spoj i njegova uporaba
US9938288B1 (en) 2017-04-05 2018-04-10 President And Fellows Of Harvard College Macrocyclic compound and uses thereof
US11548898B2 (en) 2017-07-06 2023-01-10 President And Fellows Of Harvard College Synthesis of halichondrins
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis
EP3710454B1 (en) 2017-11-15 2024-01-03 President And Fellows Of Harvard College Macrocyclic compounds and uses thereof

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US5338865A (en) 1992-03-12 1994-08-16 President And Fellows Of Harvard College Synthesis of halichondrin B and norhalichondrin B
US5436238A (en) 1992-03-12 1995-07-25 President And Fellows Of Harvard College Halichondrins and related compounds
GB9206244D0 (en) 1992-03-23 1992-05-06 Pharma Mar Sa Cytotoxic compound from a marine sponge
US5426194A (en) 1993-01-19 1995-06-20 Arizona Board Of Regents, A Body Corporate Acting On Behalf Of Arizona State University Isolation and structure of Halistatin 1
US5352804A (en) 1993-01-19 1994-10-04 Arizona Board Of Regents, A Body Corporate, Acting On Behalf Of Arizona State University Isolation and structure of Halistatin 2
IL139960A0 (en) 1998-06-17 2002-02-10 Eisai Co Ltd Macrocylic analogs and methods of their use and preparation
US8097648B2 (en) 1998-06-17 2012-01-17 Eisai R&D Management Co., Ltd. Methods and compositions for use in treating cancer
US6653341B1 (en) 1998-06-17 2003-11-25 Eisai Co., Ltd. Methods and compositions for use in treating cancer
JP2001305734A (ja) * 2000-04-20 2001-11-02 Fuji Photo Film Co Ltd 光重合性組成物
JP2003261447A (ja) 2002-03-07 2003-09-16 Kyosei Seiyaku Kk 抗腫瘍剤
PL2522663T3 (pl) 2004-06-03 2015-08-31 Eisai R&D Man Co Ltd Produkty pośrednie do otrzymywania halichondryny B
WO2006076100A2 (en) 2004-12-09 2006-07-20 Eisai Co. Ltd. Tubulin isotype screening in cancer therapy using halichondrin b analogs
JP2009184924A (ja) 2006-05-31 2009-08-20 Eisai R & D Management Co Ltd 生物学的試薬用化合物
WO2008112137A1 (en) 2007-03-07 2008-09-18 Interdigital Technology Corporation Method and apparatus for generating and processing a mac-ehs protocol data unit
JP2010530437A (ja) 2007-06-18 2010-09-09 メディミューン，エルエルシー ＥｐｈＡ２およびＥｒｂＢ２を発現する細胞の相乗的治療
EP2578576B9 (en) 2007-10-03 2016-09-14 Eisai R&D Management Co., Ltd. Intermediates for the synthesis of halichondrin B analogs
CA2705383A1 (en) 2007-11-16 2009-05-22 Eisai R&D Management Co., Ltd. Novel intermediate for halichondrin b analog synthesis and novel desulfonylation reaction used for the intermediate
US8598373B2 (en) 2008-04-04 2013-12-03 Eisai R&D Management Co., Ltd. Halichondrin B analogs
SG182612A1 (en) 2010-01-26 2012-08-30 Eisai R&D Man Co Ltd Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs
CA2824154A1 (en) 2011-01-10 2012-07-19 President And Fellows Of Harvard College Method for delivering agents into cells using bacterial toxins
WO2012147900A1 (en) 2011-04-28 2012-11-01 Eisai R&D Management Co., Ltd. Microreactor process for halichondrin b analog synthesis
JP2015501818A (ja) 2011-12-16 2015-01-19 アルフォラ リサーチ インコーポレイテッドＡｌｐｈｏｒａ Ｒｅｓｅａｒｃｈ Ｉｎｃ． ３−（（２ｓ，５ｓ）−４−メチレン−５−（３−オキソプロピル）テトラヒドロフラン−２−イル）プロパノール誘導体およびそれらの有用な中間体を調製する方法
IN2014MN01521A (enExample) 2011-12-29 2015-05-01 Alphora Res Inc
WO2013142999A1 (en) 2012-03-30 2013-10-03 Alphora Research Inc. Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein
JP6511613B2 (ja) 2013-07-03 2019-05-15 サンド・アクチエンゲゼルシヤフト ハリコンドリンＢの大環状Ｃ１−ケト類似体の製造のための合成方法及び該方法に有用な中間体、例えば−ＳＯ２−（ｐ−トリル）基を含有する中間体
HUE049387T2 (hu) 2013-11-04 2020-09-28 Eisai R&D Man Co Ltd A halichondrin B analógjainak szintézisében hasznos makrociklizációs reakciók és köztitermékek
SG11201604545XA (en) 2013-12-06 2016-07-28 Eisai R&D Man Co Ltd Methods useful in the synthesis of halichondrin b analogs
JP2017520586A (ja) 2014-06-30 2017-07-27 プレジデント アンド フェローズ オブ ハーバード カレッジ ハリコンドリン類似体の合成およびその使用
WO2016038624A1 (en) 2014-09-09 2016-03-17 Cipla Limited "process for the preparation of macrocyclic ketone analogs of halichondrin b or pharmaceutically acceptable salts and intermediates thereof"
WO2016176560A1 (en) * 2015-04-30 2016-11-03 President And Fellows Of Harvard College Chromium-mediated coupling and application to the synthesis of halichondrins
KR102743950B1 (ko) 2015-05-07 2024-12-18 에자이 알앤드디 매니지먼트 가부시키가이샤 할리콘드린 마크롤라이드의 합성에 유용한 마크로고리화 반응 및 중간체 및 기타 단편
JP6978758B2 (ja) 2016-11-11 2021-12-08 プレジデント アンド フェローズ オブ ハーバード カレッジ パラジウム媒介ケトール化
HRP20221385T1 (hr) 2017-04-05 2023-01-06 President And Fellows Of Harvard College Makrociklički spoj i njegova uporaba
US9938288B1 (en) 2017-04-05 2018-04-10 President And Fellows Of Harvard College Macrocyclic compound and uses thereof
US11548898B2 (en) 2017-07-06 2023-01-10 President And Fellows Of Harvard College Synthesis of halichondrins
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis

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JP2018108937A (ja) 2018-07-12
US10844073B2 (en) 2020-11-24
US20200002352A1 (en) 2020-01-02
US10392400B2 (en) 2019-08-27
US20180155361A1 (en) 2018-06-07

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