KR102438417B1 - 할리콘드린의 합성 - Google Patents

할리콘드린의 합성 Download PDF

Info

Publication number
KR102438417B1
KR102438417B1 KR1020207003432A KR20207003432A KR102438417B1 KR 102438417 B1 KR102438417 B1 KR 102438417B1 KR 1020207003432 A KR1020207003432 A KR 1020207003432A KR 20207003432 A KR20207003432 A KR 20207003432A KR 102438417 B1 KR102438417 B1 KR 102438417B1
Authority
KR
South Korea
Prior art keywords
substituted
unsubstituted
delete delete
formula
salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
KR1020207003432A
Other languages
English (en)
Korean (ko)
Other versions
KR20200042464A (ko
Inventor
요시토 키시
얀란 아이
닝 예
차오이 왕
켄조 야하타
켄타로 이소
샌토시 레디 나이니
스지 야마시타
지훈 이
이사오 오하시
타카시 후쿠야마
Original Assignee
프레지던트 앤드 펠로우즈 오브 하바드 칼리지
에자이 알앤드디 매니지먼트 가부시키가이샤
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 프레지던트 앤드 펠로우즈 오브 하바드 칼리지, 에자이 알앤드디 매니지먼트 가부시키가이샤 filed Critical 프레지던트 앤드 펠로우즈 오브 하바드 칼리지
Priority to KR1020227029591A priority Critical patent/KR20220124279A/ko
Publication of KR20200042464A publication Critical patent/KR20200042464A/ko
Application granted granted Critical
Publication of KR102438417B1 publication Critical patent/KR102438417B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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
    • C07D493/22—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
    • 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

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)
  • Silicates, Zeolites, And Molecular Sieves (AREA)
  • Carbon And Carbon Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Furan Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
KR1020207003432A 2017-07-06 2018-07-06 할리콘드린의 합성 Active KR102438417B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020227029591A KR20220124279A (ko) 2017-07-06 2018-07-06 할리콘드린의 합성

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762529333P 2017-07-06 2017-07-06
US201762529310P 2017-07-06 2017-07-06
US62/529,310 2017-07-06
US62/529,333 2017-07-06
PCT/US2018/041005 WO2019010363A1 (en) 2017-07-06 2018-07-06 HALICHONDRINES SYNTHESIS

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020227029591A Division KR20220124279A (ko) 2017-07-06 2018-07-06 할리콘드린의 합성

Publications (2)

Publication Number Publication Date
KR20200042464A KR20200042464A (ko) 2020-04-23
KR102438417B1 true KR102438417B1 (ko) 2022-09-01

Family

ID=63036376

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020207003432A Active KR102438417B1 (ko) 2017-07-06 2018-07-06 할리콘드린의 합성
KR1020227029591A Ceased KR20220124279A (ko) 2017-07-06 2018-07-06 할리콘드린의 합성

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020227029591A Ceased KR20220124279A (ko) 2017-07-06 2018-07-06 할리콘드린의 합성

Country Status (14)

Country Link
US (2) US11548898B2 (https=)
EP (2) EP4169924A3 (https=)
JP (2) JP7370313B2 (https=)
KR (2) KR102438417B1 (https=)
CN (2) CN118515685A (https=)
AU (2) AU2018297305B2 (https=)
BR (1) BR112020000141A2 (https=)
CA (2) CA3211559A1 (https=)
ES (1) ES2940688T3 (https=)
HU (1) HUE061306T2 (https=)
IL (3) IL271660B (https=)
MX (1) MX2020000142A (https=)
SG (1) SG11201912342QA (https=)
WO (1) WO2019010363A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
WO2019099646A1 (en) * 2017-11-15 2019-05-23 President And Fellows Of Harvard College Macrocyclic compounds and uses thereof
CN111484393A (zh) * 2019-01-28 2020-08-04 上海茂晟康慧科技有限公司 一种顺,顺-3,5-二甲基-1-环己醇的制备方法
CN117820275A (zh) * 2023-12-29 2024-04-05 上海科技大学 一种列净类药物及其中间体的催化合成方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013239290A1 (en) 2012-03-30 2014-10-30 Sandoz Ag Synthetic process for preparation of macrocyclic C1-keto analogs of Halichondrin B and intermediates useful therein
WO2016179607A1 (en) 2015-05-07 2016-11-10 Eisai R&D Management Co., Ltd. Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61191687A (ja) 1985-02-20 1986-08-26 Fujisawa Pharmaceut Co Ltd ハリコンドリンｂ
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
US5426194A (en) 1993-01-19 1995-06-20 Arizona Board Of Regents, A Body Corporate Acting On Behalf Of Arizona State University Isolation and structure of Halistatin 1
US5352804A (en) 1993-01-19 1994-10-04 Arizona Board Of Regents, A Body Corporate, Acting On Behalf Of Arizona State University Isolation and structure of Halistatin 2
JP2818381B2 (ja) 1994-01-18 1998-10-30 帝人株式会社 ７−チアプロスタグランジン類およびその製造法
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
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
JP2001305734A (ja) 2000-04-20 2001-11-02 Fuji Photo Film Co Ltd 光重合性組成物
JP2003261447A (ja) 2002-03-07 2003-09-16 Kyosei Seiyaku Kk 抗腫瘍剤
SI2522663T1 (sl) 2004-06-03 2015-08-31 Eisai R&D Management Co., Ltd. Vmesne spojine za pripravo halihondrina B
US20060154312A1 (en) 2004-12-09 2006-07-13 Sergei Agoulnik Tubulin isotype screening in cancer therapy using halichondrin B analogs
JP2009184924A (ja) 2006-05-31 2009-08-20 Eisai R & D Management Co Ltd 生物学的試薬用化合物
CN101657990B (zh) 2007-03-07 2014-03-19 交互数字技术公司 用于产生和处理MAC-ehs协议数据单元的方法和设备
US20100254996A1 (en) 2007-06-18 2010-10-07 Medimmune, Llc Synergistic treatment of cells that express epha2 and erbb2
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
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
WO2012096926A2 (en) 2011-01-10 2012-07-19 President And Fellows Of Harvard College Method for delivering agents into cells using bacterial toxins
WO2012147900A1 (en) 2011-04-28 2012-11-01 Eisai R&D Management Co., Ltd. Microreactor process for halichondrin b analog synthesis
JP2015501818A (ja) 2011-12-16 2015-01-19 アルフォラ リサーチ インコーポレイテッドＡｌｐｈｏｒａ Ｒｅｓｅａｒｃｈ Ｉｎｃ． ３−（（２ｓ，５ｓ）−４−メチレン−５−（３−オキソプロピル）テトラヒドロフラン−２−イル）プロパノール誘導体およびそれらの有用な中間体を調製する方法
CA2860446C (en) 2011-12-29 2017-01-10 Alphora Research Inc. 2-((2s,3s,4r,5r)-5-((s)-3-amino-2-hydroxyprop-1-yl)-4-methoxy-3-(phenylsulfonylmethyl)tetrahydrofuran-2-yl)acetaldehyde derivatives and process for their preparation
CA2909209A1 (en) 2013-05-15 2014-11-20 Alphora Research Inc. 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivatives, their preparation and intermediates useful thereof
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
US10556910B2 (en) 2014-06-30 2020-02-11 President And Fellows Of Harvard College Synthesis of halichondrin analogs and uses thereof
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
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
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
EP3582804A1 (en) 2017-02-20 2019-12-25 Polyphor Ag Pharmaceutical combinations for treating cancer
SMT202200455T1 (it) * 2017-04-05 2023-01-13 Harvard College Composto macrociclico e relativi usi
US9938288B1 (en) 2017-04-05 2018-04-10 President And Fellows Of Harvard College Macrocyclic compound and uses thereof
US11498892B2 (en) 2017-07-06 2022-11-15 President And Fellows Of Harvard College Fe/Cu-mediated ketone synthesis
WO2019010363A1 (en) 2017-07-06 2019-01-10 President And Fellows Of Harvard College HALICHONDRINES SYNTHESIS
WO2019009956A1 (en) 2017-07-06 2019-01-10 President And Fellows Of Harvard College SUMMARY OF MEDIUM MEDIATED KETONE
WO2019099646A1 (en) 2017-11-15 2019-05-23 President And Fellows Of Harvard College Macrocyclic compounds and uses thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013239290A1 (en) 2012-03-30 2014-10-30 Sandoz Ag Synthetic process for preparation of macrocyclic C1-keto analogs of Halichondrin B and intermediates useful therein
WO2016179607A1 (en) 2015-05-07 2016-11-10 Eisai R&D Management Co., Ltd. Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides

Also Published As

Publication number Publication date
EP3649135B1 (en) 2022-12-28
BR112020000141A2 (pt) 2020-07-14
KR20220124279A (ko) 2022-09-13
JP7370313B2 (ja) 2023-10-27
CN111433211B (zh) 2024-05-07
CA3211559A1 (en) 2019-01-10
CA3069160A1 (en) 2019-01-10
HUE061306T2 (hu) 2023-06-28
US20230128195A1 (en) 2023-04-27
US20210230177A1 (en) 2021-07-29
CN111433211A (zh) 2020-07-17
IL307273B2 (en) 2025-03-01
ES2940688T3 (es) 2023-05-10
IL271660A (en) 2020-02-27
EP4169924A2 (en) 2023-04-26
IL295588B1 (en) 2023-11-01
AU2018297305B2 (en) 2023-02-16
JP2023166381A (ja) 2023-11-21
WO2019010363A1 (en) 2019-01-10
AU2018297305A1 (en) 2020-01-16
CN118515685A (zh) 2024-08-20
US11548898B2 (en) 2023-01-10
MX2020000142A (es) 2020-07-22
SG11201912342QA (en) 2020-01-30
IL307273A (en) 2023-11-01
RU2020104842A (ru) 2021-08-06
WO2019010363A8 (en) 2019-06-06
AU2023203013A1 (en) 2023-06-01
CA3069160C (en) 2023-10-17
IL295588B2 (en) 2024-03-01
KR20200042464A (ko) 2020-04-23
IL307273B1 (en) 2024-11-01
IL295588A (en) 2022-10-01
JP7764432B2 (ja) 2025-11-05
JP2020536046A (ja) 2020-12-10
AU2023203013B2 (en) 2025-06-05
EP4169924A3 (en) 2023-07-05
IL271660B (en) 2022-09-01
EP3649135A1 (en) 2020-05-13

Similar Documents

Publication Publication Date Title
KR102438417B1 (ko) 할리콘드린의 합성
US11220513B2 (en) Chromium-mediated coupling and application to the synthesis of halichondrins
NZ248559A (en) Preparation of 13-ether milbemycins; 7 and/or 15-hydroxy protected intermediates
US11498892B2 (en) Fe/Cu-mediated ketone synthesis
WO2019032936A1 (en) LINCONSAMIDE ANTIBIOTICS AND USES THEREOF
EP3160970A1 (en) Synthesis of halichondrin analogs and uses thereof
WO2019009956A1 (en) SUMMARY OF MEDIUM MEDIATED KETONE
US20230135188A1 (en) Fe/cu-mediated ketone synthesis
WO2022019921A1 (en) Ketone synthesis and applications
RU2794176C2 (ru) Синтез галихондринов
Qiu Progress Towards the Total Synthesis of Curvulamine
WO2026025019A1 (en) Synthesis of macrobicyclic thiolincosamines
Roushanbakhti Synthesis of the EFG-ring system of pectenotoxin-4
Trenkle Phosphine-promoted cross-coupling reactions of propargylcopper reagents and alkenyl iodides and the total synthesis of (-)-gloeosporone via nickel-catalyzed epoxide-alkyne reductive macrocyclization
Lu Part I: Synthetic studies toward the southern portion of Azaspiracid-1; Part II: Total synthesis of amphidinolide B₁ and the proposed structure of amphidinolide B₂

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

A107 Divisional application of patent
GRNT Written decision to grant
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-OTH-PR1001 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 4