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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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 (cg-RX-API-DMAC7.html
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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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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)

Publication Number Publication Date
JP2018108937A JP2018108937A (ja) 2018-07-12
JP2018108937A5 JP2018108937A5 (cg-RX-API-DMAC7.html) 2019-12-26
JP6978758B2 true JP6978758B2 (ja) 2021-12-08

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JP (1) JP6978758B2 (cg-RX-API-DMAC7.html)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10556910B2 (en) 2014-06-30 2020-02-11 President And Fellows Of Harvard College Synthesis of halichondrin analogs and uses 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
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
US9938288B1 (en) 2017-04-05 2018-04-10 President And Fellows Of Harvard College Macrocyclic compound and uses thereof
ES2931533T3 (es) 2017-04-05 2022-12-30 Harvard College Compuesto macrocíclico y usos del mismo
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis
BR112020000141A2 (pt) 2017-07-06 2020-07-14 President And Fellows Of Harvard College síntese de halicondrinas
EP3710454B1 (en) 2017-11-15 2024-01-03 President And Fellows Of Harvard College Macrocyclic compounds and uses thereof

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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
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
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
US8097648B2 (en) 1998-06-17 2012-01-17 Eisai R&D Management Co., Ltd. Methods and compositions for use in treating cancer
AU762998B2 (en) 1998-06-17 2003-07-10 Eisai R&D Management Co., Ltd. Macrocyclic analogs and methods of their use and preparation
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
JP5226304B2 (ja) 2004-06-03 2013-07-03 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類似体の調製用中間体
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
KR101251715B1 (ko) 2007-03-07 2013-04-05 인터디지탈 테크날러지 코포레이션 ＭＡＣ-ｅｈｓ 프로토콜 데이터 유닛을 생성하고 프로세싱하기 위한 방법 및 장치
CN101918844A (zh) 2007-06-18 2010-12-15 米迪缪尼有限公司 表达epha2和erbb2的细胞的协同治疗
SG10201811715YA (en) 2007-10-03 2019-02-27 Eisai R&D Man Co Ltd Intermediates and methods for the synthesis of halichondrin b analogs
US20090203771A1 (en) 2007-11-16 2009-08-13 Eisai R&D Management Co., Ltd. Novel intermediate for halichondrin b analog synthesis and novel desulfonylation reaction used for the intermediate
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BR112012018232B8 (pt) 2010-01-26 2023-01-10 Eisai R&D Man Co Ltd Compostos derivados de furo [3,2-b] pirano úteis na síntese de análogos de halicondrina b e métodos de sintetização de er-80402 e de eribulina
WO2012096926A2 (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
US9174956B2 (en) 2011-12-16 2015-11-03 Alphora Research Inc. Process for preparation of 3-((2S,5S)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivatives and intermediates useful thereof
JP6300030B2 (ja) 2011-12-29 2018-03-28 サンド アクツィエンゲゼルシャフト ２−（（２ｓ，３ｓ，４ｒ，５ｒ）−５−（（ｓ）−３−アミノ−２−ヒドロキシプロプ−１−イル）−４−メトキシ−３−（フェニルスルホニルメチル）テトラヒドロフラン−２−イル）アセトアルデヒド誘導体およびこれらを調製するためのプロセス
EP2831082B1 (en) 2012-03-30 2019-02-20 Sandoz AG 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
EP3689881B1 (en) 2013-11-04 2022-01-12 Eisai R&D Management Co., Ltd. Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b
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
US10556910B2 (en) 2014-06-30 2020-02-11 President And Fellows Of Harvard College Synthesis of halichondrin analogs and uses thereof
EP3191479B1 (en) 2014-09-09 2020-04-08 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
EP3292130B1 (en) 2015-05-07 2020-09-30 Eisai R&D Management Co., Ltd. Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides
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
ES2931533T3 (es) 2017-04-05 2022-12-30 Harvard College Compuesto macrocíclico y usos del mismo
US9938288B1 (en) 2017-04-05 2018-04-10 President And Fellows Of Harvard College Macrocyclic compound and uses thereof
BR112020000141A2 (pt) 2017-07-06 2020-07-14 President And Fellows Of Harvard College síntese de halicondrinas
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis

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

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