SG10201811715YA - Intermediates and methods for the synthesis of halichondrin b analogs - Google Patents
Intermediates and methods for the synthesis of halichondrin b analogsInfo
- Publication number
- SG10201811715YA SG10201811715YA SG10201811715YA SG10201811715YA SG10201811715YA SG 10201811715Y A SG10201811715Y A SG 10201811715YA SG 10201811715Y A SG10201811715Y A SG 10201811715YA SG 10201811715Y A SG10201811715Y A SG 10201811715YA SG 10201811715Y A SG10201811715Y A SG 10201811715YA
- Authority
- SG
- Singapore
- Prior art keywords
- halichondrin
- analogs
- synthesis
- methods
- intermediates
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- FXNFULJVOQMBCW-VZBLNRDYSA-N halichondrin b Chemical class O([C@@H]1[C@@H](C)[C@@H]2O[C@@H]3C[C@@]4(O[C@H]5[C@@H](C)C[C@@]6(C[C@@H]([C@@H]7O[C@@H](C[C@@H]7O6)[C@@H](O)C[C@@H](O)CO)C)O[C@H]5C4)O[C@@H]3C[C@@H]2O[C@H]1C[C@@H]1C(=C)[C@H](C)C[C@@H](O1)CC[C@H]1C(=C)C[C@@H](O1)CC1)C(=O)C[C@H](O2)CC[C@H]3[C@H]2[C@H](O2)[C@@H]4O[C@@H]5C[C@@]21O[C@@H]5[C@@H]4O3 FXNFULJVOQMBCW-VZBLNRDYSA-N 0.000 title abstract 3
- 239000000543 intermediate Substances 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 238000003786 synthesis reaction Methods 0.000 title abstract 3
- 230000002194 synthesizing effect Effects 0.000 abstract 1
Classifications
-
- 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
- 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
- C07D493/20—Spiro-condensed systems
-
- 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
- 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
-
- 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
- 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
- C07D307/30—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 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
- C07D307/32—Oxygen atoms
- C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/16—Heterocyclic compounds containing six-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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
- C07D493/08—Bridged 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
- C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
- C07D493/18—Bridged 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
-
- 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
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Furan Compounds (AREA)
- Silicates, Zeolites, And Molecular Sieves (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US99762507P | 2007-10-03 | 2007-10-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
SG10201811715YA true SG10201811715YA (en) | 2019-02-27 |
Family
ID=40019255
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG10201811715YA SG10201811715YA (en) | 2007-10-03 | 2008-10-03 | Intermediates and methods for the synthesis of halichondrin b analogs |
Country Status (11)
Country | Link |
---|---|
US (6) | US8093410B2 (fr) |
EP (2) | EP2578576B9 (fr) |
JP (1) | JP5735277B2 (fr) |
CN (3) | CN108948039B (fr) |
BR (1) | BRPI0817909B1 (fr) |
CA (1) | CA2701534C (fr) |
IL (1) | IL204791A (fr) |
MX (1) | MX2010003599A (fr) |
RU (1) | RU2489437C2 (fr) |
SG (1) | SG10201811715YA (fr) |
WO (1) | WO2009046308A1 (fr) |
Families Citing this family (39)
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HU227912B1 (en) * | 1998-06-17 | 2012-05-29 | Eisai R & D Man Co | Halichondrin analogs and methods of their use and preparation |
CA2567984C (fr) | 2004-06-03 | 2014-05-20 | Eisai Co., Ltd. | Intermediaires pour la preparation d'analogues d'halichondrine b |
EP2578576B9 (fr) | 2007-10-03 | 2016-09-14 | Eisai R&D Management Co., Ltd. | Intermédiaires pour la synthèse d'analogues d'halichondrine b |
BRPI0911269A2 (pt) | 2008-04-04 | 2015-09-29 | Eisai R&D Man Co Ltd | análogos de halicondrina b |
DE102009012660A1 (de) * | 2009-03-13 | 2010-09-16 | H.C. Starck Clevios Gmbh | Polymerbeschichtungen mit verbesserter Temperaturstabilität |
SI2415470T1 (sl) | 2009-03-30 | 2016-12-30 | Eisai R&D Management Co., Ltd. | Liposomski sestavek |
SG182612A1 (en) | 2010-01-26 | 2012-08-30 | Eisai R&D Man Co Ltd | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs |
CN102225921B (zh) * | 2011-04-26 | 2013-04-24 | 中国人民解放军第二军医大学 | 一种环戊烷聚酮类化合物simplextone A及其用途 |
WO2012147900A1 (fr) | 2011-04-28 | 2012-11-01 | Eisai R&D Management Co., Ltd. | Procédé en microréacteurs pour synthèse d'analogue d'halichondrine b |
MX2015007185A (es) | 2012-12-04 | 2017-09-05 | Eisai R&D Man Co Ltd | Uso de eribulina en el tratamiento de cancer de pecho. |
RU2672585C2 (ru) | 2013-06-26 | 2018-11-16 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Применение эрибулина и ленватиниба в качестве комбинированной терапии для лечения рака |
JP6625533B2 (ja) * | 2013-11-04 | 2019-12-25 | 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 |
RU2676486C1 (ru) | 2013-12-06 | 2018-12-29 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Способы, предназначенные для синтеза аналогов галихондрина b |
CN106413705A (zh) | 2014-05-28 | 2017-02-15 | 卫材R&D管理有限公司 | 艾日布林在治疗癌症中的用途 |
US10556910B2 (en) | 2014-06-30 | 2020-02-11 | President And Fellows Of Harvard College | Synthesis of halichondrin analogs and uses thereof |
EP3191479B1 (fr) | 2014-09-09 | 2020-04-08 | Cipla Limited | PROCÉDÉ DE PRÉPARATION D'ANALOGUES
DE CÉTONES MACROCYCLIQUES DE L'HALICHONDRINE B OU DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES ET D'INTERMEDIAIRES DE CEUX-CI |
WO2016140717A1 (fr) | 2015-03-04 | 2016-09-09 | Merck Sharp & Dohme Corp. | Association d'un antagoniste de pd-1 et d'un inhibiteur des tyrosines kinases vegfr/fgfr/ret pour traiter le cancer |
SG11201706872SA (en) | 2015-03-04 | 2017-09-28 | Merck Sharp & Dohme | Combination of a pd-1 antagonist and eribulin for treating cancer |
US10344038B2 (en) | 2015-04-30 | 2019-07-09 | President And Fellows Of Harvard College | Chromium-mediated coupling and application to the synthesis of halichondrins |
RU2020141025A (ru) | 2015-05-07 | 2020-12-28 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Реакции макроциклизации и промежуточные соединения и другие фрагменты, полезные в синтезе макролидов галихондринов |
SG11201806133UA (en) | 2016-02-12 | 2018-08-30 | Eisai R&D Man Co Ltd | Intermediates in the synthesis of eribulin and related methods of synthesis |
CN114191563A (zh) | 2016-03-02 | 2022-03-18 | 卫材研究发展管理有限公司 | 基于艾日布林的抗体-药物偶联物和使用方法 |
EP3449921B1 (fr) | 2016-04-28 | 2023-05-31 | Eisai R&D Management Co., Ltd. | Eribulin pour l' inhibition de croissance tumorale |
SG11201811671XA (en) * | 2016-06-30 | 2019-01-30 | Eisai R&D Man Co Ltd | Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof |
SG11201902974PA (en) | 2016-10-14 | 2019-05-30 | Merck Sharp & Dohme | Combination of a pd-1 antagonist and eribulin for treating urothelial cancer |
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 |
MX2019011982A (es) | 2017-04-05 | 2019-11-08 | Harvard College | Compuesto macrociclico y sus usos. |
MX2020000142A (es) | 2017-07-06 | 2020-07-22 | Harvard College | Sintesis de halicondrinas. |
US11498892B2 (en) | 2017-07-06 | 2022-11-15 | President And Fellows Of Harvard College | Fe/Cu-mediated ketone synthesis |
US20190046513A1 (en) | 2017-08-10 | 2019-02-14 | Huya Bioscience International, Llc | Combination therapies of hdac inhibitors and tubulin inhibitors |
US11407762B2 (en) | 2017-11-15 | 2022-08-09 | President And Fellows Of Harvard College | Macrocyclic compounds and uses thereof |
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EP2578576B9 (fr) | 2007-10-03 | 2016-09-14 | Eisai R&D Management Co., Ltd. | Intermédiaires pour la synthèse d'analogues d'halichondrine b |
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SG182612A1 (en) | 2010-01-26 | 2012-08-30 | Eisai R&D Man Co Ltd | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs |
WO2012147900A1 (fr) | 2011-04-28 | 2012-11-01 | Eisai R&D Management Co., Ltd. | Procédé en microréacteurs pour synthèse d'analogue d'halichondrine b |
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JP6625533B2 (ja) | 2013-11-04 | 2019-12-25 | 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 |
RU2676486C1 (ru) | 2013-12-06 | 2018-12-29 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Способы, предназначенные для синтеза аналогов галихондрина b |
EP3191479B1 (fr) | 2014-09-09 | 2020-04-08 | Cipla Limited | PROCÉDÉ DE PRÉPARATION D'ANALOGUES
DE CÉTONES MACROCYCLIQUES DE L'HALICHONDRINE B OU DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES ET D'INTERMEDIAIRES DE CEUX-CI |
RU2020141025A (ru) | 2015-05-07 | 2020-12-28 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Реакции макроциклизации и промежуточные соединения и другие фрагменты, полезные в синтезе макролидов галихондринов |
SG11201806133UA (en) | 2016-02-12 | 2018-08-30 | Eisai R&D Man Co Ltd | Intermediates in the synthesis of eribulin and related methods of synthesis |
SG11201811671XA (en) | 2016-06-30 | 2019-01-30 | Eisai R&D Man Co Ltd | Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof |
WO2018217894A1 (fr) | 2017-05-24 | 2018-11-29 | Eisai R&D Management Co., Ltd. | Dérivés d'halichondrine marqués au fluor et procédés de synthèse associés |
JP7469226B2 (ja) | 2018-01-03 | 2024-04-16 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ハリコンドリンマクロライドとそのアナログの合成に有用なプリンス反応及び化合物 |
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