JP2016536316A5 - - Google Patents

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JP2016536316A5
JP2016536316A5 JP2016527449A JP2016527449A JP2016536316A5 JP 2016536316 A5 JP2016536316 A5 JP 2016536316A5 JP 2016527449 A JP2016527449 A JP 2016527449A JP 2016527449 A JP2016527449 A JP 2016527449A JP 2016536316 A5 JP2016536316 A5 JP 2016536316A5
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protecting group
hydroxyl protecting
formula
compound
combined
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JP2016527449A
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JP2016536316A (ja
JP6625533B2 (ja
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Priority claimed from PCT/US2014/063960 external-priority patent/WO2015066729A1/en
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Priority to JP2019181798A priority Critical patent/JP6909840B2/ja
Priority to JP2019213906A priority patent/JP6889232B2/ja
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JP2016527449A 2013-11-04 2014-11-04 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 Active JP6625533B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2019181798A JP6909840B2 (ja) 2013-11-04 2019-10-02 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
JP2019213906A JP6889232B2 (ja) 2013-11-04 2019-11-27 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

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361899697P 2013-11-04 2013-11-04
US61/899,697 2013-11-04
PCT/US2014/063960 WO2015066729A1 (en) 2013-11-04 2014-11-04 Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b

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JP2019181798A Division JP6909840B2 (ja) 2013-11-04 2019-10-02 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
JP2019213906A Division JP6889232B2 (ja) 2013-11-04 2019-11-27 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

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JP2016536316A JP2016536316A (ja) 2016-11-24
JP2016536316A5 true JP2016536316A5 (https=) 2017-12-14
JP6625533B2 JP6625533B2 (ja) 2019-12-25

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JP2016527449A Active JP6625533B2 (ja) 2013-11-04 2014-11-04 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
JP2019181798A Expired - Fee Related JP6909840B2 (ja) 2013-11-04 2019-10-02 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
JP2019213906A Active JP6889232B2 (ja) 2013-11-04 2019-11-27 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

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JP2019181798A Expired - Fee Related JP6909840B2 (ja) 2013-11-04 2019-10-02 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
JP2019213906A Active JP6889232B2 (ja) 2013-11-04 2019-11-27 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

Country Status (12)

Country Link
US (5) US9783549B2 (https=)
EP (2) EP3689881B1 (https=)
JP (3) JP6625533B2 (https=)
CN (3) CN105683198B (https=)
BR (1) BR112016009452B1 (https=)
CA (1) CA2929084C (https=)
ES (1) ES2787603T3 (https=)
HU (1) HUE049387T2 (https=)
IL (4) IL244694B (https=)
RU (1) RU2710545C2 (https=)
SG (1) SG11201603490TA (https=)
WO (1) WO2015066729A1 (https=)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2522663T1 (sl) 2004-06-03 2015-08-31 Eisai R&D Management Co., Ltd. Vmesne spojine za pripravo halihondrina B
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
CA2720632C (en) 2008-04-04 2016-12-20 Eisai R&D Management Co., Ltd. Halichondrin b analogs
RU2579511C2 (ru) 2010-01-26 2016-04-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Производные фуро[3,2-в]пирана, применимые в синтезе аналогов
BR112016009452B1 (pt) 2013-11-04 2022-06-07 Eisai R&D Management Co., Ltd Métodos de preparar intermediários na síntese de eribulina, métodos de preparar eribulina e mesilato de eribulina, e compostos intermediários
EP3077399B1 (en) 2013-12-06 2019-02-20 Eisai R&D Management Co., Ltd. Methods useful in the synthesis of halichondrin b analogs
US10556910B2 (en) 2014-06-30 2020-02-11 President And Fellows Of Harvard College Synthesis of halichondrin analogs and uses thereof
US10344038B2 (en) 2015-04-30 2019-07-09 President And Fellows Of Harvard College Chromium-mediated coupling and application to the synthesis of halichondrins
MX392296B (es) 2015-05-07 2025-03-24 Eisai R&D Man Co Ltd Reacciones de macrociclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina.
WO2017064627A2 (en) * 2015-10-14 2017-04-20 Dr. Reddy's Laboratories Limited Process for preparation of eribulin and intermediates thereof
CN108601760A (zh) * 2016-02-12 2018-09-28 卫材R&D管理有限公司 艾日布林的合成中的中间体及相关的合成方法
PE20231050A1 (es) 2016-03-02 2023-07-11 Eisai Randd Man Co Ltd Conjugados de anticuerpo y farmaco basados en eribulina y metodos para su uso
KR102404629B1 (ko) * 2016-06-30 2022-06-02 에자이 알앤드디 매니지먼트 가부시키가이샤 할리콘드린 마크롤리드 및 그의 유사체의 합성에 유용한 프린스 반응 및 중간체
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
SMT202200455T1 (it) * 2017-04-05 2023-01-13 Harvard College Composto macrociclico e relativi usi
WO2018217894A1 (en) * 2017-05-24 2018-11-29 Eisai R&D Management Co., Ltd. Fluorine-labelled halichondrin derivatives and related methods of synthesis
WO2019010363A1 (en) 2017-07-06 2019-01-10 President And Fellows Of Harvard College HALICHONDRINES SYNTHESIS
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis
CN109694379B (zh) * 2017-10-24 2020-09-11 江苏恒瑞医药股份有限公司 用于制备艾日布林的中间体及其制备方法
US11142509B2 (en) * 2017-11-09 2021-10-12 Yonsung Fine Chemical Co., Ltd. Intermediate for preparing eribulin mesylate and process for preparing the same
WO2019099646A1 (en) 2017-11-15 2019-05-23 President And Fellows Of Harvard College Macrocyclic compounds and uses thereof
WO2019097073A1 (en) 2017-11-20 2019-05-23 Basilea Pharmaceutica International AG Pharmaceutical combinations for use in the treatment of neoplastic diseases
CN109970822B (zh) * 2017-12-27 2023-03-28 上海科胜药物研发有限公司 一种合成埃格列净中间体的制备方法
IL275729B2 (en) 2018-01-03 2023-09-01 Eisai R&D Man Co Ltd Prins reaction and compounds useful in the synthesis of helicondrin macrolides and their analogs
WO2019166019A1 (zh) * 2018-03-02 2019-09-06 北京天一绿甫医药科技有限公司 吡喃稠环类化合物、其制备方法和用途
WO2019211877A1 (en) * 2018-05-03 2019-11-07 Cipla Limited Process for the preparation of macrocyclic ketone analogs of halichondrin b
WO2020016847A2 (en) * 2018-07-20 2020-01-23 Dr. Reddy’S Laboratories Limited Purification process for preparation of eribulin and intermediates thereof
US11447499B2 (en) * 2019-06-14 2022-09-20 Rk Pharma Inc. Process for the preparation of eribulin mesylate intermediate
CN110684036B (zh) * 2019-11-22 2022-04-12 江苏慧聚药业股份有限公司 一条制备甲磺酸艾日布林的方法
WO2023144733A1 (en) * 2022-01-26 2023-08-03 Simon Fraser University Compounds and processes for the preparation of eribulin
CN119585437A (zh) * 2022-07-29 2025-03-07 上海皓元医药股份有限公司 一种艾日布林中间体的制备方法

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4107206A (en) 1974-04-08 1978-08-15 Akzona Incorporated Benzo-bicyclononene- derivatives
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 (https=) 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
JP4454151B2 (ja) 1998-06-17 2010-04-21 エーザイ・アール・アンド・ディー・マネジメント株式会社 大環状類似体及びそれらの使用並びに調製方法
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
CA2822994C (en) * 2004-06-03 2016-09-27 Eisai R&D Management Co., Ltd. Intermediates for the preparation of analogs of halichondrin b
SI2522663T1 (sl) 2004-06-03 2015-08-31 Eisai R&D Management Co., Ltd. Vmesne spojine za pripravo halihondrina 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
JP2009510005A (ja) 2005-09-26 2009-03-12 シムライズ・ゲゼルシヤフト・ミツト・ベシユレンクテル・ハフツング・ウント・コンパニー・コマンジツト・ゲゼルシヤフト 分子内プリンス反応および該反応に適する触媒
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
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
CN101910180A (zh) 2007-11-16 2010-12-08 卫材R&D管理有限公司 用于软海绵素b类似物合成的新颖中间体和用于该中间体的新颖脱磺酰化反应
CA2720632C (en) 2008-04-04 2016-12-20 Eisai R&D Management 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
RU2579511C2 (ru) 2010-01-26 2016-04-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Производные фуро[3,2-в]пирана, применимые в синтезе аналогов
WO2012147900A1 (en) 2011-04-28 2012-11-01 Eisai R&D Management Co., Ltd. Microreactor process for halichondrin b analog synthesis
WO2013078559A1 (en) * 2011-11-30 2013-06-06 Alphora Research Inc. Process for preparation of (3r)-2,4-di-leaving group-3-methylbut-1-ene
US9278979B2 (en) 2012-03-30 2016-03-08 Alphora Research Inc. Synthetic process for preparation of macrocyclic C1-keto analogs of halichondrin B and intermediates useful therein
EP3016957A4 (en) 2013-07-03 2016-11-30 Alphora Res Inc SYNTHETIC METHOD FOR THE PRODUCTION OF CYCLIC C1-KETO ANALOGUE OF HALICHONDRIN B AND USEFUL INTERMEDIATE PRODUCTS, INCLUDING INTERMEDIATE PRODUCTS WITH -SO2- (P-TOLYL) GROUPS
BR112016009452B1 (pt) 2013-11-04 2022-06-07 Eisai R&D Management Co., Ltd Métodos de preparar intermediários na síntese de eribulina, métodos de preparar eribulina e mesilato de eribulina, e compostos intermediários
EP3077399B1 (en) * 2013-12-06 2019-02-20 Eisai R&D Management Co., Ltd. Methods useful in the synthesis of halichondrin b analogs
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
US10344038B2 (en) * 2015-04-30 2019-07-09 President And Fellows Of Harvard College Chromium-mediated coupling and application to the synthesis of halichondrins
MX392296B (es) * 2015-05-07 2025-03-24 Eisai R&D Man Co Ltd Reacciones de macrociclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina.
CN108601760A (zh) 2016-02-12 2018-09-28 卫材R&D管理有限公司 艾日布林的合成中的中间体及相关的合成方法
KR102404629B1 (ko) 2016-06-30 2022-06-02 에자이 알앤드디 매니지먼트 가부시키가이샤 할리콘드린 마크롤리드 및 그의 유사체의 합성에 유용한 프린스 반응 및 중간체
US20180009825A1 (en) * 2016-07-06 2018-01-11 Apicore Us Llc Methods of making eribulin mesylate
WO2018217894A1 (en) 2017-05-24 2018-11-29 Eisai R&D Management Co., Ltd. Fluorine-labelled halichondrin derivatives and related methods of synthesis
IL275729B2 (en) * 2018-01-03 2023-09-01 Eisai R&D Man Co Ltd Prins reaction and compounds useful in the synthesis of helicondrin macrolides and their analogs

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