CN104334562A - 用于制备软海绵素b的大环c1-酮类似物的合成方法及其中有用的中间体 - Google Patents

用于制备软海绵素b的大环c1-酮类似物的合成方法及其中有用的中间体 Download PDF

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Publication number
CN104334562A
CN104334562A CN201380028907.2A CN201380028907A CN104334562A CN 104334562 A CN104334562 A CN 104334562A CN 201380028907 A CN201380028907 A CN 201380028907A CN 104334562 A CN104334562 A CN 104334562A
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compound
alcohol protecting
formula
protecting group
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Chinese (zh)
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F·E·S·索扎
A·鲁道夫
M·潘
B·戈林
T·K·魏
J·A·贝克思鲁德
R·奥普来西奥
H·兰格瓦拉
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A Fangla Studies Limited-Liability Co
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A Fangla Studies Limited-Liability Co
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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • 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
    • C07D407/14—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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
CN201380028907.2A 2012-03-30 2013-03-28 用于制备软海绵素b的大环c1-酮类似物的合成方法及其中有用的中间体 Pending CN104334562A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261618004P 2012-03-30 2012-03-30
US61/618,004 2012-03-30
US201261647127P 2012-05-15 2012-05-15
US61/647,127 2012-05-15
PCT/CA2013/050254 WO2013142999A1 (en) 2012-03-30 2013-03-28 Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein

Publications (1)

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CN104334562A true CN104334562A (zh) 2015-02-04

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CN201380028907.2A Pending CN104334562A (zh) 2012-03-30 2013-03-28 用于制备软海绵素b的大环c1-酮类似物的合成方法及其中有用的中间体

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US (2) US9278979B2 (enExample)
EP (1) EP2831082B1 (enExample)
JP (1) JP6531911B2 (enExample)
CN (1) CN104334562A (enExample)
AU (1) AU2013239290B2 (enExample)
CA (1) CA2868627C (enExample)
IN (1) IN2014MN02106A (enExample)
WO (1) WO2013142999A1 (enExample)

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CN107849057A (zh) * 2015-05-07 2018-03-27 卫材R&D管理有限公司 用于合成软海绵素大环内酯的大环化反应及中间体和其他片段
CN108658956A (zh) * 2017-03-28 2018-10-16 上海时莱生物技术有限公司 艾日布林中间体及其制备方法
WO2018210297A1 (zh) * 2017-05-17 2018-11-22 上海时莱生物技术有限公司 一种艾日布林中间体及其制备方法
CN111868044A (zh) * 2018-01-03 2020-10-30 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
US11136335B2 (en) 2016-06-30 2021-10-05 Eisai R&D Management Co., Ltd. Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof
WO2024153123A1 (zh) * 2023-01-17 2024-07-25 成都百利多特生物药业有限责任公司 一种艾日布林类药物的偶联物

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CN101899026B (zh) 2004-06-03 2016-08-03 卫材R&D管理有限公司 用于制备软海绵素b的类似物的中间体
BRPI0817909B1 (pt) 2007-10-03 2022-06-21 Eisai R&D Management Co., Ltd Métodos de obtenção e de preparação de uma composição diastereomericamente pura, compostos, e método para produzir os referidos compostos
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
EP2785687B1 (en) 2011-11-30 2019-02-20 Sandoz AG Process for preparation of (3r)-2,4-di-leaving group-3-methylbut-1-ene
EP2791123B1 (en) 2011-12-16 2018-07-18 Sandoz AG Process for preparation of 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl) propanol derivatives and intermediates useful thereof
AU2012363334B2 (en) 2011-12-29 2017-02-02 Alphora Research Inc. 2-((2s,3s,4r,5r)-5-((s)-3-amino-2-hydroxyprop-1-yl)-4-methoxy-3-(phenylsulfonylmethyl) tetrahydrofuran-2-yl)acetaldehyde derivatives and process for their preparation
AU2014286880B2 (en) * 2013-07-03 2017-12-14 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
CN103483352A (zh) * 2013-10-18 2014-01-01 李友香 抗肿瘤的药用原料药
HUE049387T2 (hu) * 2013-11-04 2020-09-28 Eisai R&D Man Co Ltd A halichondrin B analógjainak szintézisében hasznos makrociklizációs reakciók és köztitermékek
SG10201805024YA (en) 2013-12-06 2018-07-30 Eisai R&D Man Co Ltd Methods useful in the synthesis of halichondrin b analogs
TW201617326A (zh) * 2014-03-06 2016-05-16 Ａｌｐｈｏｒａ研發股份有限公司 （ｓ）－１－（（２ｒ，３ｒ，４ｓ，５ｓ）－５－烯丙－３－甲氧－４－（對甲苯磺醯甲基）四氫呋喃－２－基）－３－氨基丙－２－醇之結晶衍生物
US10556910B2 (en) 2014-06-30 2020-02-11 President And Fellows Of Harvard College Synthesis of halichondrin analogs and uses thereof
CN105713031B (zh) * 2014-12-05 2021-05-07 正大天晴药业集团股份有限公司 一种用于制备艾日布林的中间体及其制备方法
US10344038B2 (en) 2015-04-30 2019-07-09 President And Fellows Of Harvard College Chromium-mediated coupling and application to the synthesis of halichondrins
US10676481B2 (en) 2016-02-12 2020-06-09 Eisai R&D Management Co., Ltd. Intermediates in the synthesis of eribulin and related methods of synthesis
JOP20170053B1 (ar) 2016-03-02 2021-08-17 Eisai Randd Man Co Ltd مترافقات جسم مضاد وعقار أساسها إيريبولين وطرق استخدامها
EP3464297B1 (en) * 2016-05-26 2023-10-25 Dr. Reddy's Laboratories Ltd. Process for preparation of eribulin and intermediates thereof
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
WO2018096478A2 (en) 2016-11-23 2018-05-31 Dr. Reddy’S Laboratories Limited Process for preparation of eribulin and intermediates thereof
US9938288B1 (en) 2017-04-05 2018-04-10 President And Fellows Of Harvard College Macrocyclic compound and uses thereof
JP7168580B2 (ja) 2017-04-05 2022-11-09 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 大環状化合物およびその使用
WO2018217894A1 (en) * 2017-05-24 2018-11-29 Eisai R&D Management Co., Ltd. Fluorine-labelled halichondrin derivatives and related methods of synthesis
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis
IL295588B2 (en) * 2017-07-06 2024-03-01 Harvard College Synthesis of halichondrins
ES2974243T3 (es) 2017-11-15 2024-06-26 Harvard College Compuestos macrocíclicos y usos de los mismos
IL279168B (en) 2020-12-02 2022-04-01 Finetech Pharmaceutical Ltd A process for the preparation of eribulin
CN114213429B (zh) * 2021-12-22 2023-06-20 苏州正济药业有限公司 一种甲磺酸艾立布林杂质的制备方法

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EP2785687B1 (en) 2011-11-30 2019-02-20 Sandoz AG Process for preparation of (3r)-2,4-di-leaving group-3-methylbut-1-ene
EP2791123B1 (en) 2011-12-16 2018-07-18 Sandoz AG Process for preparation of 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl) propanol derivatives and intermediates useful thereof
AU2012363334B2 (en) * 2011-12-29 2017-02-02 Alphora Research Inc. 2-((2s,3s,4r,5r)-5-((s)-3-amino-2-hydroxyprop-1-yl)-4-methoxy-3-(phenylsulfonylmethyl) tetrahydrofuran-2-yl)acetaldehyde derivatives and process for their preparation
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Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107849057A (zh) * 2015-05-07 2018-03-27 卫材R&D管理有限公司 用于合成软海绵素大环内酯的大环化反应及中间体和其他片段
CN107849057B (zh) * 2015-05-07 2020-11-10 卫材R&D管理有限公司 用于合成软海绵素大环内酯的大环化反应及中间体和其他片段
US10913749B2 (en) 2015-05-07 2021-02-09 Eisai R&D Management Co., Ltd. Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides
CN117024469A (zh) * 2015-05-07 2023-11-10 卫材R&D管理有限公司 可用于合成软海绵素大环内酯的大环化反应以及中间体和其他片段
US11136335B2 (en) 2016-06-30 2021-10-05 Eisai R&D Management Co., Ltd. Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof
CN108658956A (zh) * 2017-03-28 2018-10-16 上海时莱生物技术有限公司 艾日布林中间体及其制备方法
CN108658956B (zh) * 2017-03-28 2021-02-02 上海时莱生物技术有限公司 艾日布林中间体及其制备方法
WO2018210297A1 (zh) * 2017-05-17 2018-11-22 上海时莱生物技术有限公司 一种艾日布林中间体及其制备方法
US11186570B2 (en) 2017-05-17 2021-11-30 Selection Bioscience Llc Intermediate of eribulin and preparation method therefor
CN111868044A (zh) * 2018-01-03 2020-10-30 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
WO2024153123A1 (zh) * 2023-01-17 2024-07-25 成都百利多特生物药业有限责任公司 一种艾日布林类药物的偶联物

Also Published As

Publication number Publication date
EP2831082B1 (en) 2019-02-20
CA2868627A1 (en) 2013-10-03
US9278979B2 (en) 2016-03-08
US20150065733A1 (en) 2015-03-05
US20160152631A1 (en) 2016-06-02
JP6531911B2 (ja) 2019-06-19
CA2868627C (en) 2021-02-16
WO2013142999A1 (en) 2013-10-03
EP2831082A4 (en) 2016-01-06
AU2013239290A1 (en) 2014-10-30
JP2015512897A (ja) 2015-04-30
AU2013239290B2 (en) 2017-08-03
US9695187B2 (en) 2017-07-04
IN2014MN02106A (enExample) 2015-09-11
EP2831082A1 (en) 2015-02-04

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