SG11201811671XA - Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof - Google Patents
Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereofInfo
- Publication number
- SG11201811671XA SG11201811671XA SG11201811671XA SG11201811671XA SG11201811671XA SG 11201811671X A SG11201811671X A SG 11201811671XA SG 11201811671X A SG11201811671X A SG 11201811671XA SG 11201811671X A SG11201811671X A SG 11201811671XA SG 11201811671X A SG11201811671X A SG 11201811671XA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- analogs
- synthesis
- andover
- pct
- Prior art date
Links
- 239000003120 macrolide antibiotic agent Substances 0.000 title abstract 5
- 229930195695 Halichondrin Natural products 0.000 title abstract 4
- 230000015572 biosynthetic process Effects 0.000 title abstract 4
- 239000000543 intermediate Substances 0.000 title abstract 4
- 229940041033 macrolides Drugs 0.000 title abstract 4
- 238000003786 synthesis reaction Methods 0.000 title abstract 4
- 238000010478 Prins reaction Methods 0.000 title abstract 3
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 241001333452 Bridelia insulana Species 0.000 abstract 1
- 241000721662 Juniperus Species 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 238000007363 ring formation reaction Methods 0.000 abstract 1
Classifications
-
- 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
- C07D407/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D321/00—Heterocyclic compounds containing rings having two oxygen atoms as the only ring hetero atoms, not provided for by groups C07D317/00 - C07D319/00
-
- 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
- C07D493/02—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
-
- 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
- C07D493/16—Peri-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
- C07D493/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- C07F9/6561—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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
- Pyrane Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662357031P | 2016-06-30 | 2016-06-30 | |
PCT/US2017/040401 WO2018006031A1 (en) | 2016-06-30 | 2017-06-30 | Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
SG11201811671XA true SG11201811671XA (en) | 2019-01-30 |
Family
ID=60786711
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG11201811671XA SG11201811671XA (en) | 2016-06-30 | 2017-06-30 | Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof |
Country Status (9)
Country | Link |
---|---|
US (1) | US11136335B2 (es) |
EP (1) | EP3478691A4 (es) |
JP (3) | JP7068204B2 (es) |
KR (1) | KR102404629B1 (es) |
CN (2) | CN109641917B (es) |
IL (2) | IL263845B (es) |
MX (1) | MX2018016329A (es) |
SG (1) | SG11201811671XA (es) |
WO (1) | WO2018006031A1 (es) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101434673B1 (ko) | 2004-06-03 | 2014-08-26 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 b 유사체의 제조를 위한 중간체 |
CN104311571B (zh) | 2007-10-03 | 2019-07-02 | 卫材R&D管理有限公司 | 用于合成软海绵素b类似物的中间体和方法 |
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. |
WO2015066729A1 (en) | 2013-11-04 | 2015-05-07 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b |
CN105916861B (zh) | 2013-12-06 | 2018-12-14 | 卫材R&D管理有限公司 | 可用于合成软海绵素b类似物的方法 |
RU2739034C2 (ru) | 2015-05-07 | 2020-12-21 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Реакции макроциклизации и промежуточное соединение и другие фрагменты, полезные в синтезе макролидов галихондринов |
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 |
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 |
CN110218213B (zh) * | 2018-03-02 | 2020-09-04 | 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 |
Family Cites Families (33)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
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 |
TW255880B (es) | 1992-09-09 | 1995-09-01 | Hoechst Ag | |
JP2001500498A (ja) | 1996-09-06 | 2001-01-16 | イーライ・リリー・アンド・カンパニー | 触媒選択的スルホニル化法 |
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 |
WO1999065894A1 (en) | 1998-06-17 | 1999-12-23 | Eisai Co., Ltd. | Macrocyclic analogs and methods of their use and preparation |
US8097648B2 (en) | 1998-06-17 | 2012-01-17 | Eisai R&D Management Co., Ltd. | Methods and compositions for use in treating cancer |
US6653341B1 (en) | 1998-06-17 | 2003-11-25 | Eisai 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 |
KR101434673B1 (ko) | 2004-06-03 | 2014-08-26 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 b 유사체의 제조를 위한 중간체 |
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 |
WO2007039342A1 (en) | 2005-09-26 | 2007-04-12 | Symrise Gmbh & Co. Kg | Intramolecular prins reaction and catalysts suitable therefor |
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 |
CN104311571B (zh) * | 2007-10-03 | 2019-07-02 | 卫材R&D管理有限公司 | 用于合成软海绵素b类似物的中间体和方法 |
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 |
WO2009124237A1 (en) | 2008-04-04 | 2009-10-08 | 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 |
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 |
WO2015066729A1 (en) | 2013-11-04 | 2015-05-07 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b |
CN105916861B (zh) | 2013-12-06 | 2018-12-14 | 卫材R&D管理有限公司 | 可用于合成软海绵素b类似物的方法 |
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 |
RU2739034C2 (ru) | 2015-05-07 | 2020-12-21 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Реакции макроциклизации и промежуточное соединение и другие фрагменты, полезные в синтезе макролидов галихондринов |
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 |
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 |
-
2017
- 2017-06-30 WO PCT/US2017/040401 patent/WO2018006031A1/en unknown
- 2017-06-30 JP JP2018568296A patent/JP7068204B2/ja active Active
- 2017-06-30 CN CN201780052964.2A patent/CN109641917B/zh active Active
- 2017-06-30 EP EP17821400.3A patent/EP3478691A4/en active Pending
- 2017-06-30 KR KR1020197002930A patent/KR102404629B1/ko active IP Right Grant
- 2017-06-30 US US16/313,196 patent/US11136335B2/en active Active
- 2017-06-30 CN CN202210653392.6A patent/CN114805322A/zh active Pending
- 2017-06-30 MX MX2018016329A patent/MX2018016329A/es unknown
- 2017-06-30 SG SG11201811671XA patent/SG11201811671XA/en unknown
-
2018
- 2018-12-19 IL IL263845A patent/IL263845B/en unknown
-
2021
- 2021-11-28 IL IL288460A patent/IL288460B2/en unknown
-
2022
- 2022-04-28 JP JP2022073976A patent/JP7440563B2/ja active Active
-
2024
- 2024-02-15 JP JP2024020885A patent/JP2024056892A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
MX2018016329A (es) | 2019-09-18 |
KR102404629B1 (ko) | 2022-06-02 |
RU2019102375A (ru) | 2020-07-30 |
US20190161495A1 (en) | 2019-05-30 |
JP2019524674A (ja) | 2019-09-05 |
IL263845B (en) | 2022-01-01 |
CN114805322A (zh) | 2022-07-29 |
JP7068204B2 (ja) | 2022-05-16 |
IL288460A (en) | 2022-01-01 |
JP2024056892A (ja) | 2024-04-23 |
IL288460B1 (en) | 2023-04-01 |
EP3478691A4 (en) | 2020-07-22 |
KR20190039103A (ko) | 2019-04-10 |
IL263845A (en) | 2019-01-31 |
JP2022105115A (ja) | 2022-07-12 |
RU2019102375A3 (es) | 2021-07-05 |
CN109641917B (zh) | 2022-06-14 |
EP3478691A1 (en) | 2019-05-08 |
CN109641917A (zh) | 2019-04-16 |
US11136335B2 (en) | 2021-10-05 |
JP7440563B2 (ja) | 2024-02-28 |
IL288460B2 (en) | 2023-08-01 |
WO2018006031A1 (en) | 2018-01-04 |
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