SG11201603490TA - Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b - Google Patents
Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin bInfo
- Publication number
- SG11201603490TA SG11201603490TA SG11201603490TA SG11201603490TA SG11201603490TA SG 11201603490T A SG11201603490T A SG 11201603490TA SG 11201603490T A SG11201603490T A SG 11201603490TA SG 11201603490T A SG11201603490T A SG 11201603490TA SG 11201603490T A SG11201603490T A SG 11201603490TA
- Authority
- SG
- Singapore
- 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 System
- 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 System
- 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 System
- 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
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 (1)
Publication Number | Publication Date |
---|---|
SG11201603490TA true SG11201603490TA (en) | 2016-05-30 |
Family
ID=53005318
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG11201603490TA SG11201603490TA (en) | 2013-11-04 | 2014-11-04 | Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b |
Country Status (12)
Country | Link |
---|---|
US (5) | US9783549B2 (en) |
EP (2) | EP3066102B1 (en) |
JP (3) | JP6625533B2 (en) |
CN (3) | CN114716453A (en) |
BR (1) | BR112016009452B1 (en) |
CA (1) | CA2929084C (en) |
ES (1) | ES2787603T3 (en) |
HU (1) | HUE049387T2 (en) |
IL (4) | IL244694B (en) |
RU (1) | RU2710545C2 (en) |
SG (1) | SG11201603490TA (en) |
WO (1) | WO2015066729A1 (en) |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
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USRE45324E1 (en) | 2004-06-03 | 2015-01-06 | Eisai R&D Management Co., Ltd. | Intermediates for the preparation of analogs of halichondrin B |
BRPI0817909B1 (en) | 2007-10-03 | 2022-06-21 | Eisai R&D Management Co., Ltd | Methods of obtaining and preparing a diastereomerically pure composition, compounds, and method of producing said compounds |
RU2517167C2 (en) | 2008-04-04 | 2014-05-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Halichondrin b analogues |
MX2012008510A (en) | 2010-01-26 | 2012-11-21 | Eisai R&D Man Co Ltd | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs. |
EP3066102B1 (en) | 2013-11-04 | 2020-02-26 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b |
CA2931788C (en) | 2013-12-06 | 2022-05-24 | Eisai R&D Management Co., Ltd. | Methods useful in the synthesis of halichondrin b analogs |
EP3160970A4 (en) | 2014-06-30 | 2017-12-27 | 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 |
MX2021002629A (en) | 2015-05-07 | 2022-05-13 | Eisai R&D Man Co Ltd | Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides. |
WO2017064627A2 (en) * | 2015-10-14 | 2017-04-20 | Dr. Reddy's Laboratories Limited | Process for preparation of eribulin and intermediates thereof |
RU2732575C2 (en) * | 2016-02-12 | 2020-09-21 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Intermediate products in synthesis of eribulin and corresponding methods of synthesis |
KR102445255B1 (en) | 2016-03-02 | 2022-09-22 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | Eribulin-Based Antibody-Drug Conjugates and Methods of Use |
KR102404629B1 (en) * | 2016-06-30 | 2022-06-02 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | Prince Reaction and Intermediates Useful for Synthesis of Halicondine Macrolides and Analogs thereof |
JP6978758B2 (en) | 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 | Palladium-mediated ketolization |
HRP20221385T1 (en) | 2017-04-05 | 2023-01-06 | President And Fellows Of Harvard College | Macrocyclic compound and uses thereof |
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 |
IL271660B (en) | 2017-07-06 | 2022-09-01 | Harvard College | Synthesis of halichondrins |
US11498892B2 (en) | 2017-07-06 | 2022-11-15 | President And Fellows Of Harvard College | Fe/Cu-mediated ketone synthesis |
CN109694379B (en) * | 2017-10-24 | 2020-09-11 | 江苏恒瑞医药股份有限公司 | Intermediate for preparing eribulin and preparation method thereof |
WO2019093776A1 (en) * | 2017-11-09 | 2019-05-16 | 연성정밀화학(주) | Intermediate for preparing eribulin mesylate and method for preparing same |
CN111566113B (en) | 2017-11-15 | 2024-01-09 | 哈佛大学的校长及成员们 | 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 (en) * | 2017-12-27 | 2023-03-28 | 上海科胜药物研发有限公司 | Preparation method for synthesizing emamectin benzoate intermediate |
MX2020006945A (en) | 2018-01-03 | 2020-11-09 | Eisai R&D Man Co Ltd | Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof. |
US11396515B2 (en) * | 2018-03-02 | 2022-07-26 | Beijing Tienyi Lufu Pharmatech Co. Ltd. | Pyran fused ring compound, preparation method therefor and use thereof |
WO2019211877A1 (en) * | 2018-05-03 | 2019-11-07 | Cipla Limited | Process for the preparation of macrocyclic ketone analogs of halichondrin b |
CN112437775A (en) * | 2018-07-20 | 2021-03-02 | 雷迪博士实验室有限公司 | Purification method for preparing eribulin and intermediates thereof |
US11447499B2 (en) * | 2019-06-14 | 2022-09-20 | Rk Pharma Inc. | Process for the preparation of eribulin mesylate intermediate |
CN110684036B (en) * | 2019-11-22 | 2022-04-12 | 江苏慧聚药业股份有限公司 | Method for preparing eribulin mesylate |
WO2023144733A1 (en) * | 2022-01-26 | 2023-08-03 | Simon Fraser University | Compounds and processes for the preparation of eribulin |
WO2024021261A1 (en) * | 2022-07-29 | 2024-02-01 | 上海皓元医药股份有限公司 | Method for preparing eribulin intermediate |
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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 |
GB9206244D0 (en) | 1992-03-23 | 1992-05-06 | Pharma Mar Sa | Cytotoxic compound from a marine sponge |
TW255880B (en) | 1992-09-09 | 1995-09-01 | Hoechst Ag | |
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CN1993342A (en) * | 2004-06-03 | 2007-07-04 | 卫材株式会社 | Intermediates for the preparation of halichondrin b |
USRE45324E1 (en) * | 2004-06-03 | 2015-01-06 | Eisai R&D Management Co., Ltd. | Intermediates for the preparation of analogs of halichondrin 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 (en) | 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 | Intramolecular Prince reaction and catalyst suitable for the reaction |
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 |
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BRPI0817909B1 (en) | 2007-10-03 | 2022-06-21 | Eisai R&D Management Co., Ltd | Methods of obtaining and preparing a diastereomerically pure composition, compounds, and method of producing said compounds |
RU2010118063A (en) | 2007-11-16 | 2011-12-27 | ЭЙСАЙ Ар энд Ди МЕНЕДЖМЕНТ КО., ЛТД. (JP) | A NEW INTERMEDIATE COMPOUND FOR SYNTHESIS OF ANALOG OF HALICHONDRIN B AND A NEW DESULPHONILATION REACTION USED FOR OBTAINING AN INTERMEDIATE COMPOUND |
RU2517167C2 (en) | 2008-04-04 | 2014-05-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Halichondrin b analogues |
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MX2012008510A (en) * | 2010-01-26 | 2012-11-21 | Eisai R&D Man Co Ltd | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs. |
WO2012147900A1 (en) | 2011-04-28 | 2012-11-01 | Eisai R&D Management Co., Ltd. | Microreactor process for halichondrin b analog synthesis |
CA2857385A1 (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 |
WO2015000070A1 (en) | 2013-07-03 | 2015-01-08 | Alphora Research Inc. | Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein including intermediates containing -so2-(p-tolyl) groups |
EP3066102B1 (en) * | 2013-11-04 | 2020-02-26 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b |
CA2931788C (en) | 2013-12-06 | 2022-05-24 | Eisai R&D Management Co., Ltd. | Methods useful in the synthesis of halichondrin b analogs |
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 |
MX2021002629A (en) | 2015-05-07 | 2022-05-13 | Eisai R&D Man Co Ltd | Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides. |
RU2732575C2 (en) | 2016-02-12 | 2020-09-21 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Intermediate products in synthesis of eribulin and corresponding methods of synthesis |
KR102404629B1 (en) | 2016-06-30 | 2022-06-02 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | Prince Reaction and Intermediates Useful for Synthesis of Halicondine Macrolides and Analogs thereof |
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 |
MX2020006945A (en) | 2018-01-03 | 2020-11-09 | Eisai R&D Man Co Ltd | Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof. |
-
2014
- 2014-11-04 EP EP14858240.6A patent/EP3066102B1/en active Active
- 2014-11-04 CN CN202210377346.8A patent/CN114716453A/en active Pending
- 2014-11-04 SG SG11201603490TA patent/SG11201603490TA/en unknown
- 2014-11-04 CN CN201480059909.2A patent/CN105683198B/en active Active
- 2014-11-04 CA CA2929084A patent/CA2929084C/en active Active
- 2014-11-04 BR BR112016009452-2A patent/BR112016009452B1/en active IP Right Grant
- 2014-11-04 JP JP2016527449A patent/JP6625533B2/en active Active
- 2014-11-04 RU RU2016121648A patent/RU2710545C2/en active
- 2014-11-04 US US15/033,970 patent/US9783549B2/en active Active
- 2014-11-04 CN CN201910122043.XA patent/CN109942560B/en active Active
- 2014-11-04 HU HUE14858240A patent/HUE049387T2/en unknown
- 2014-11-04 WO PCT/US2014/063960 patent/WO2015066729A1/en active Application Filing
- 2014-11-04 ES ES14858240T patent/ES2787603T3/en active Active
- 2014-11-04 EP EP20156829.2A patent/EP3689881B1/en active Active
-
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/en active Active
- 2019-11-27 JP JP2019213906A patent/JP6889232B2/en active Active
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2020
- 2020-03-30 US US16/833,923 patent/US10934307B2/en active Active
- 2020-06-09 IL IL275240A patent/IL275240B/en unknown
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2021
- 2021-03-01 US US17/188,819 patent/US11643418B2/en active Active
- 2021-11-28 IL IL288468A patent/IL288468B2/en unknown
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