IL244694B - Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs - Google Patents
Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogsInfo
- Publication number
- IL244694B IL244694B IL244694A IL24469416A IL244694B IL 244694 B IL244694 B IL 244694B IL 244694 A IL244694 A IL 244694A IL 24469416 A IL24469416 A IL 24469416A IL 244694 B IL244694 B IL 244694B
- Authority
- IL
- Israel
- Prior art keywords
- halichondrin
- analogs
- synthesis
- intermediates useful
- macrocyclization reactions
- Prior art date
Links
Classifications
-
- 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
- C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D307/28—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring 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
- C07D407/02—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
- C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
- C07D493/14—Ortho-condensed systems
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrane Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Saccharide Compounds (AREA)
- Steroid Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361899697P | 2013-11-04 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL244694A0 IL244694A0 (en) | 2016-04-21 |
| IL244694B true IL244694B (en) | 2019-07-31 |
Family
ID=53005318
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL244694A IL244694B (en) | 2013-11-04 | 2016-03-21 | Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs |
| IL267936A IL267936B (en) | 2013-11-04 | 2019-07-09 | Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs |
| IL275240A IL275240B (en) | 2013-11-04 | 2020-06-09 | Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs |
| IL288468A IL288468B2 (en) | 2013-11-04 | 2021-11-28 | Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL267936A IL267936B (en) | 2013-11-04 | 2019-07-09 | Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs |
| IL275240A IL275240B (en) | 2013-11-04 | 2020-06-09 | Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs |
| IL288468A IL288468B2 (en) | 2013-11-04 | 2021-11-28 | Microcyclization reactions and useful intermediates in the synthesis of helichondrin b analogs |
Country Status (12)
| Country | Link |
|---|---|
| US (5) | US9783549B2 (enExample) |
| EP (2) | EP3689881B1 (enExample) |
| JP (3) | JP6625533B2 (enExample) |
| CN (3) | CN114716453A (enExample) |
| BR (1) | BR112016009452B1 (enExample) |
| CA (1) | CA2929084C (enExample) |
| ES (1) | ES2787603T3 (enExample) |
| HU (1) | HUE049387T2 (enExample) |
| IL (4) | IL244694B (enExample) |
| RU (1) | RU2710545C2 (enExample) |
| SG (1) | SG11201603490TA (enExample) |
| WO (1) | WO2015066729A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| SG10201811715YA (en) | 2007-10-03 | 2019-02-27 | Eisai R&D Man Co Ltd | Intermediates and methods for the synthesis of halichondrin b analogs |
| CA2720632C (en) | 2008-04-04 | 2016-12-20 | Eisai R&D Management Co., Ltd. | Halichondrin b analogs |
| MX2012008510A (es) | 2010-01-26 | 2012-11-21 | Eisai R&D Man Co Ltd | Derivados de furo [3, 2-b] pirano utiles en la sintesis de analogos de halicondrina b. |
| CN114716453A (zh) | 2013-11-04 | 2022-07-08 | 卫材R&D管理有限公司 | 软海绵素b的类似物合成中有用的大环化反应和中间体 |
| BR112016012237B1 (pt) | 2013-12-06 | 2023-02-07 | Eisai R&D Management Co., Ltd | Métodos úteis na síntese de análogos de halicondrina b |
| 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 |
| US10344038B2 (en) | 2015-04-30 | 2019-07-09 | President And Fellows Of Harvard College | Chromium-mediated coupling and application to the synthesis of halichondrins |
| 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 |
| WO2017064627A2 (en) * | 2015-10-14 | 2017-04-20 | Dr. Reddy's Laboratories Limited | Process for preparation of eribulin and intermediates thereof |
| MX377663B (es) * | 2016-02-12 | 2025-03-11 | Eisai R&D Man Co Ltd | Intermediarios en la sintesis de eribulina y metodos de sintesis relacionados. |
| RU2754369C2 (ru) | 2016-03-02 | 2021-09-01 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конъюгаты антитело-лекарственное средство на основе эрибулина и способы применения |
| 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 |
| PL3606928T3 (pl) * | 2017-04-05 | 2023-02-06 | President And Fellows Of Harvard College | Związek makrocykliczny i jego zastosowania |
| US9938288B1 (en) | 2017-04-05 | 2018-04-10 | President And Fellows Of Harvard College | Macrocyclic compound and uses thereof |
| 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 |
| CN111433211B (zh) | 2017-07-06 | 2024-05-07 | 哈佛大学的校长及成员们 | 软海绵素的合成 |
| 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 |
| KR102177992B1 (ko) * | 2017-11-09 | 2020-11-12 | 연성정밀화학(주) | 에리불린 메실산염의 제조 중간체 및 그의 제조방법 |
| US11407762B2 (en) | 2017-11-15 | 2022-08-09 | President And Fellows Of Harvard College | Macrocyclic compounds and uses thereof |
| US11419856B2 (en) | 2017-11-20 | 2022-08-23 | 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 |
| WO2019136145A1 (en) | 2018-01-03 | 2019-07-11 | Eisai R&D Management Co., Ltd. | Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof |
| 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 |
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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 |
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| 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 |
| EP2272840B1 (en) | 1998-06-17 | 2012-08-22 | Eisai R&D Management Co., Ltd. | Intermediate compound for the preparation of halichondrin analogs |
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| CN1993342A (zh) * | 2004-06-03 | 2007-07-04 | 卫材株式会社 | 用于制备软海绵素b的中间体 |
| 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 |
| US20060045846A1 (en) * | 2004-08-30 | 2006-03-02 | Horstmann Thomas E | Reagents and methods for labeling terminal olefins |
| JP2008522623A (ja) | 2004-12-09 | 2008-07-03 | エーザイ株式会社 | ハリコンドリンｂアナログを使用した癌治療でのチューブリンアイソタイプのスクリーニング |
| 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 |
| JPWO2009014105A1 (ja) | 2007-07-20 | 2010-10-07 | 株式会社山田養蜂場本社 | 新規カルボン酸およびそれを有効成分とする抗うつ用組成物 |
| SG10201811715YA (en) | 2007-10-03 | 2019-02-27 | Eisai R&D Man Co Ltd | Intermediates and methods for the synthesis of halichondrin b analogs |
| EP2220094A1 (en) | 2007-11-16 | 2010-08-25 | Eisai R&D Management Co., Ltd. | Novel intermediate for halichondrin b analog synthesis and novel desulfonylation reaction used for the intermediate |
| 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 |
| MX2012008510A (es) | 2010-01-26 | 2012-11-21 | Eisai R&D Man Co Ltd | Derivados de furo [3, 2-b] pirano utiles en la sintesis de analogos de halicondrina b. |
| WO2012147900A1 (en) | 2011-04-28 | 2012-11-01 | Eisai R&D Management Co., Ltd. | Microreactor process for halichondrin b analog synthesis |
| JP2015500210A (ja) * | 2011-11-30 | 2015-01-05 | アルフォラ リサーチ インコーポレイテッドＡｌｐｈｏｒａ Ｒｅｓｅａｒｃｈ Ｉｎｃ． | （３ｒ）−２，４−ジ−脱離基−３−メチルブタ−１−エンの調製方法 |
| CN104334562A (zh) | 2012-03-30 | 2015-02-04 | 阿方拉研究股份有限公司 | 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 |
| 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 |
| CN114716453A (zh) | 2013-11-04 | 2022-07-08 | 卫材R&D管理有限公司 | 软海绵素b的类似物合成中有用的大环化反应和中间体 |
| BR112016012237B1 (pt) | 2013-12-06 | 2023-02-07 | Eisai R&D Management Co., Ltd | Métodos úteis na síntese de análogos de halicondrina b |
| 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" |
| US10344038B2 (en) * | 2015-04-30 | 2019-07-09 | President And Fellows Of Harvard College | Chromium-mediated coupling and application to the synthesis of halichondrins |
| 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 |
| MX377663B (es) | 2016-02-12 | 2025-03-11 | Eisai R&D Man Co Ltd | Intermediarios en la sintesis de eribulina y metodos de sintesis relacionados. |
| 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 |
| WO2019136145A1 (en) * | 2018-01-03 | 2019-07-11 | Eisai R&D Management Co., Ltd. | Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof |
-
2014
- 2014-11-04 CN CN202210377346.8A patent/CN114716453A/zh active Pending
- 2014-11-04 EP EP20156829.2A patent/EP3689881B1/en active Active
- 2014-11-04 US US15/033,970 patent/US9783549B2/en active Active
- 2014-11-04 WO PCT/US2014/063960 patent/WO2015066729A1/en not_active Ceased
- 2014-11-04 JP JP2016527449A patent/JP6625533B2/ja active Active
- 2014-11-04 ES ES14858240T patent/ES2787603T3/es active Active
- 2014-11-04 RU RU2016121648A patent/RU2710545C2/ru active
- 2014-11-04 CA CA2929084A patent/CA2929084C/en active Active
- 2014-11-04 EP EP14858240.6A patent/EP3066102B1/en active Active
- 2014-11-04 HU HUE14858240A patent/HUE049387T2/hu unknown
- 2014-11-04 CN CN201480059909.2A patent/CN105683198B/zh active Active
- 2014-11-04 CN CN201910122043.XA patent/CN109942560B/zh active Active
- 2014-11-04 BR BR112016009452-2A patent/BR112016009452B1/pt active IP Right Grant
- 2014-11-04 SG SG11201603490TA patent/SG11201603490TA/en unknown
-
2016
- 2016-03-21 IL IL244694A patent/IL244694B/en active IP Right Grant
-
2017
- 2017-09-18 US US15/707,412 patent/US10221189B2/en active Active
-
2019
- 2019-01-14 US US16/246,999 patent/US10611773B2/en active Active
- 2019-07-09 IL IL267936A patent/IL267936B/en active IP Right Grant
- 2019-10-02 JP JP2019181798A patent/JP6909840B2/ja active Active
- 2019-11-27 JP JP2019213906A patent/JP6889232B2/ja active Active
-
2020
- 2020-03-30 US US16/833,923 patent/US10934307B2/en active Active
- 2020-06-09 IL IL275240A patent/IL275240B/en unknown
-
2021
- 2021-03-01 US US17/188,819 patent/US11643418B2/en active Active
- 2021-11-28 IL IL288468A patent/IL288468B2/en unknown
Also Published As
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