MX2017014237A - Reacciones de macro-ciclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina. - Google Patents

Reacciones de macro-ciclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina.

Info

Publication number
MX2017014237A
MX2017014237A MX2017014237A MX2017014237A MX2017014237A MX 2017014237 A MX2017014237 A MX 2017014237A MX 2017014237 A MX2017014237 A MX 2017014237A MX 2017014237 A MX2017014237 A MX 2017014237A MX 2017014237 A MX2017014237 A MX 2017014237A
Authority
MX
Mexico
Prior art keywords
synthesis
intermediates
fragments useful
macrocyclization reactions
halichondrin macrolides
Prior art date
Application number
MX2017014237A
Other languages
English (en)
Other versions
MX380284B (es
Inventor
G Fang Francis
Shik KIM Dae-
Wook CHOI Hyeong-
E Chase Charles
Original Assignee
Eisai R&D Man Co Ltd
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 Eisai R&D Man Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of MX2017014237A publication Critical patent/MX2017014237A/es
Publication of MX380284B publication Critical patent/MX380284B/es

Links

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
    • 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
    • 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
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • 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
    • 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
    • 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
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • 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
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/6552—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a six-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyrane Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

En general, la invención presenta compuestos útiles para la síntesis de análogos de halicondrina B, tales como aribulina o sales farmacéuticamente aceptables de la misma, v.gr., mesilato de eribulina. Compuestos ejemplares son de la formula (I), (II), o (III).
MX2017014237A 2015-05-07 2016-05-09 Reacciones de macrociclización e intermediarios y otros fragmentos útiles en la síntesis de macrólidos de halicondrina. MX380284B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562158506P 2015-05-07 2015-05-07
US201662291918P 2016-02-05 2016-02-05
PCT/US2016/031546 WO2016179607A1 (en) 2015-05-07 2016-05-09 Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides

Publications (2)

Publication Number Publication Date
MX2017014237A true MX2017014237A (es) 2018-09-17
MX380284B MX380284B (es) 2025-03-12

Family

ID=57218352

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2017014237A MX380284B (es) 2015-05-07 2016-05-09 Reacciones de macrociclización e intermediarios y otros fragmentos útiles en la síntesis de macrólidos de halicondrina.
MX2021002629A MX392296B (es) 2015-05-07 2016-05-09 Reacciones de macrociclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina.

Family Applications After (1)

Application Number Title Priority Date Filing Date
MX2021002629A MX392296B (es) 2015-05-07 2016-05-09 Reacciones de macrociclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina.

Country Status (9)

Country Link
US (2) US10308661B2 (es)
EP (1) EP3292130B1 (es)
JP (1) JP6840090B2 (es)
KR (2) KR20250012090A (es)
CN (3) CN107849057B (es)
IL (2) IL255408B (es)
MX (2) MX380284B (es)
RU (2) RU2020141025A (es)
WO (1) WO2016179607A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101899026B (zh) 2004-06-03 2016-08-03 卫材R&D管理有限公司 用于制备软海绵素b的类似物的中间体
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
BR112012018232B8 (pt) 2010-01-26 2023-01-10 Eisai R&D Man Co Ltd Compostos derivados de furo [3,2-b] pirano úteis na síntese de análogos de halicondrina b e métodos de sintetização de er-80402 e de eribulina
HUE049387T2 (hu) 2013-11-04 2020-09-28 Eisai R&D Man Co Ltd A halichondrin B analógjainak szintézisében hasznos makrociklizációs reakciók és köztitermékek
SG10201805024YA (en) 2013-12-06 2018-07-30 Eisai R&D Man 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
US10344038B2 (en) 2015-04-30 2019-07-09 President And Fellows Of Harvard College Chromium-mediated coupling and application to the synthesis of halichondrins
MX380284B (es) 2015-05-07 2025-03-12 Eisai R&D Man Co Ltd Reacciones de macrociclización e intermediarios y otros fragmentos útiles en la síntesis de macrólidos de halicondrina.
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
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
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
JP7168580B2 (ja) 2017-04-05 2022-11-09 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 大環状化合物およびその使用
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
IL295588B2 (en) * 2017-07-06 2024-03-01 Harvard College Synthesis of halichondrins
ES2974243T3 (es) 2017-11-15 2024-06-26 Harvard College Compuestos macrocíclicos y usos de los mismos
KR20250057138A (ko) * 2018-01-03 2025-04-28 에자이 알앤드디 매니지먼트 가부시키가이샤 할리콘드린 마크롤리드 및 그의 유사체의 합성에 유용한 프린스 반응 및 화합물
CN115583875B (zh) * 2022-09-28 2023-12-01 联化科技（台州）有限公司 在连续流反应器中将烯丙型醇氧化为α,β-不饱和醛酮的方法

Family Cites Families (34)

* Cited by examiner, † Cited by third party
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
US8097648B2 (en) 1998-06-17 2012-01-17 Eisai R&D Management Co., Ltd. Methods and compositions for use in treating cancer
IL139960A0 (en) 1998-06-17 2002-02-10 Eisai Co Ltd Macrocylic analogs and methods of their use and preparation
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
CN101899026B (zh) * 2004-06-03 2016-08-03 卫材R&D管理有限公司 用于制备软海绵素b的类似物的中间体
US20060045846A1 (en) 2004-08-30 2006-03-02 Horstmann Thomas E Reagents and methods for labeling terminal olefins
WO2006076100A2 (en) 2004-12-09 2006-07-20 Eisai Co. Ltd. Tubulin isotype screening in cancer therapy using halichondrin b analogs
EP1940758B1 (en) 2005-09-26 2012-11-28 Symrise AG Intramolecular prins 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
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
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
JP5134686B2 (ja) 2007-11-16 2013-01-30 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アナログ合成のための新規な中間体及び前記中間体に用いるための新規な脱スルホニル化反応
JP6001857B2 (ja) * 2008-04-04 2016-10-05 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
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
BR112012018232B8 (pt) 2010-01-26 2023-01-10 Eisai R&D Man Co Ltd Compostos derivados de furo [3,2-b] pirano úteis na síntese de análogos de halicondrina b e métodos de sintetização de er-80402 e de eribulina
WO2012147900A1 (en) * 2011-04-28 2012-11-01 Eisai R&D Management Co., Ltd. Microreactor process for halichondrin b analog synthesis
EP2785687B1 (en) * 2011-11-30 2019-02-20 Sandoz AG Process for preparation of (3r)-2,4-di-leaving group-3-methylbut-1-ene
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
AU2014286880B2 (en) * 2013-07-03 2017-12-14 Sandoz Ag Synthetic process for preparation of macrocyclic C1-keto analogs of Halichondrin B and intermediates useful therein including intermediates containing -SO2-(p-TOLYL) groups
HUE049387T2 (hu) 2013-11-04 2020-09-28 Eisai R&D Man Co Ltd A halichondrin B analógjainak szintézisében hasznos makrociklizációs reakciók és köztitermékek
SG10201805024YA (en) 2013-12-06 2018-07-30 Eisai R&D Man 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"
MX380284B (es) 2015-05-07 2025-03-12 Eisai R&D Man Co Ltd Reacciones de macrociclización e intermediarios y otros fragmentos útiles en la síntesis de macrólidos de halicondrina.
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
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 (en) 2017-05-24 2018-11-29 Eisai R&D Management Co., Ltd. Fluorine-labelled halichondrin derivatives and related methods of synthesis
KR20250057138A (ko) 2018-01-03 2025-04-28 에자이 알앤드디 매니지먼트 가부시키가이샤 할리콘드린 마크롤리드 및 그의 유사체의 합성에 유용한 프린스 반응 및 화합물

Also Published As

Publication number Publication date
CN107849057A (zh) 2018-03-27
US20180118755A1 (en) 2018-05-03
JP2018516885A (ja) 2018-06-28
RU2020141025A (ru) 2020-12-28
RU2017142100A3 (es) 2019-12-26
CN112250692A (zh) 2021-01-22
JP6840090B2 (ja) 2021-03-10
WO2016179607A1 (en) 2016-11-10
EP3292130A4 (en) 2018-12-05
IL255408B (en) 2020-08-31
IL276376B (en) 2021-09-30
US10308661B2 (en) 2019-06-04
KR20250012090A (ko) 2025-01-23
CN117024469A (zh) 2023-11-10
US10913749B2 (en) 2021-02-09
EP3292130B1 (en) 2020-09-30
CN112250692B (zh) 2023-08-29
KR20180013943A (ko) 2018-02-07
RU2739034C2 (ru) 2020-12-21
MX392296B (es) 2025-03-24
EP3292130A1 (en) 2018-03-14
US20190308992A1 (en) 2019-10-10
MX2021002629A (es) 2022-05-13
RU2017142100A (ru) 2019-06-07
IL276376A (en) 2020-09-30
IL255408A0 (en) 2017-12-31
MX380284B (es) 2025-03-12
CN107849057B (zh) 2020-11-10
KR102743950B1 (ko) 2024-12-18

Similar Documents

Publication Publication Date Title
MX2017014237A (es) Reacciones de macro-ciclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina.
CY1124059T1 (el) Αζαβενζιμιδαζολια και χρηση αυτων ως ρυθμιστες υποδοχεα ampa
CO2019000386A2 (es) Compuestos heterocíclicos como inmunomoduladores
MX376869B (es) Metodos utiles en la sintesis de analogos de halicondrina b.
CY1120935T1 (el) Νεες συνθεσεις, χρησεις και μεθοδοι για την παρασκευη αυτων
DOP2016000271A (es) Compuestos de heteroarilo o arilo bicíclicos fusionados
MX394380B (es) Compuestos dinucleótidos cíclicos para eltratamiento de cáncer
MX379110B (es) Derivados de azaspiro como antagonistas de trpm8.
UY36175A (es) 3-amino-1,5,6,7-tetrahidro-4h-indol-4-onas
CY1123574T1 (el) Αντιπολλαπλασιαστικες ενωσεις και φαρμακευτικες συνθεσεις και χρησεις αυτων
CY1122613T1 (el) Παραγωγα 4-οξο-3,4-διυδρο-1,2,3-βενζοτριαζινης ως ρυθμιστες toy gpr139
PH12017502255A1 (en) Nrf2 regulators
MX2016015565A (es) Ciertos inhibidores de la proteina quinasa.
CL2017001181A1 (es) Amidas de morfolina y 1,4-oxazepano como agonistas del receptor de somatostatina subtipo 4(sstr4)
CY1123465T1 (el) Αντιβακτηριακες ενωσεις ευρεως φασματος
MX2017013874A (es) Imidazopirazinas y pirazolopirimidinas y su uso como moduladores del receptor de ampa.
CL2014002661A1 (es) Compuestos derivados de tienopirimidina o sus sales, como inhibidores de la alk quinasa; su proceso de preparacion; composicion farmaceutica que los comprende, util para el tratamiento del cancer.
CY1121596T1 (el) Αμιδια βενζοξαζινονης ως αλατοκορτικοειδεις ρυθμιστες υποδοχεα
CR20160374A (es) Ciclopentanos sustituidos en 1,2 como antagonistas del receptor de orexina
NI201300070A (es) Ureas asimétricas y usos médicos de las mismas
CY1121273T1 (el) Παραγωγα 6-αλκυνυλο-πυριδινης ως smac μιμητικα
TR201819805T4 (tr) Flavaglin türevleri̇.
CY1125153T1 (el) Νεα ετεροκυκλικα αντiοιστρογονα
CL2017001310A1 (es) Péptidos cíclicos derivados de cd44v6 para el tratamiento de enfermedades relacionadas con cánceres y angiogénesis
NI201600091A (es) UREAS ASIMÉTRICAS p-SUSTITUIDAS Y USOS MÉDICOS DE LAS MISMAS