UY35641A - PROCEDIMIENTO DE SÍNTESIS PARA PREPARAR ANÁLOGOS MACROCÍCLICOS C1-CETO DE HALICONDRINA B, E INTERMEDIARIOS ÚTILES INCLUYENDO INTERMEDIARIOS CONTENIENDO GRUPOS ?SO2-(p-TOLILO) - Google Patents
PROCEDIMIENTO DE SÍNTESIS PARA PREPARAR ANÁLOGOS MACROCÍCLICOS C1-CETO DE HALICONDRINA B, E INTERMEDIARIOS ÚTILES INCLUYENDO INTERMEDIARIOS CONTENIENDO GRUPOS ?SO2-(p-TOLILO)Info
- Publication number
- UY35641A UY35641A UY35641A UY35641A UY35641A UY 35641 A UY35641 A UY 35641A UY 35641 A UY35641 A UY 35641A UY 35641 A UY35641 A UY 35641A UY 35641 A UY35641 A UY 35641A
- Authority
- UY
- Uruguay
- Prior art keywords
- intermediaries
- halicondrine
- tolilo
- check
- containing groups
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 2
- UFNVPOGXISZXJD-XJPMSQCNSA-N eribulin Chemical compound C([C@H]1CC[C@@H]2O[C@@H]3[C@H]4O[C@H]5C[C@](O[C@H]4[C@H]2O1)(O[C@@H]53)CC[C@@H]1O[C@H](C(C1)=C)CC1)C(=O)C[C@@H]2[C@@H](OC)[C@@H](C[C@H](O)CN)O[C@H]2C[C@@H]2C(=C)[C@H](C)C[C@H]1O2 UFNVPOGXISZXJD-XJPMSQCNSA-N 0.000 abstract 1
- 229960003649 eribulin Drugs 0.000 abstract 1
- 239000000543 intermediate Substances 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
-
- 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
- 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
- C07D493/22—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Furan Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Se describe un compuesto de fórmula 1, o una sal farmacéuticamente aceptable del mismo, en donde R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 y R13 son como se describe en la presente. También se describe un procedimiento para la preparación de un compuesto de fórmula 1, o una sal farmacéuticamente aceptable del mismo, e intermediarios utilizados en el mismo. El compuesto de fórmula 1 puede ser utilizado en la preparación de análogos de halicondrina, tal como Eribulina; y también se describe un procedimiento para su preparación a partir del compuesto de fórmula 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361842467P | 2013-07-03 | 2013-07-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UY35641A true UY35641A (es) | 2015-01-30 |
Family
ID=52142965
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UY35641A UY35641A (es) | 2013-07-03 | 2014-07-02 | PROCEDIMIENTO DE SÍNTESIS PARA PREPARAR ANÁLOGOS MACROCÍCLICOS C1-CETO DE HALICONDRINA B, E INTERMEDIARIOS ÚTILES INCLUYENDO INTERMEDIARIOS CONTENIENDO GRUPOS ?SO2-(p-TOLILO) |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9850254B2 (es) |
| EP (1) | EP3016957A4 (es) |
| JP (1) | JP6511613B2 (es) |
| CN (1) | CN105431438A (es) |
| AR (1) | AR096643A1 (es) |
| AU (1) | AU2014286880B2 (es) |
| CA (1) | CA2916537C (es) |
| TW (1) | TW201522345A (es) |
| UY (1) | UY35641A (es) |
| WO (1) | WO2015000070A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2522663T3 (pl) | 2004-06-03 | 2015-08-31 | Eisai R&D Man Co Ltd | Produkty pośrednie do otrzymywania halichondryny B |
| EP2578576B9 (en) | 2007-10-03 | 2016-09-14 | Eisai R&D Management Co., Ltd. | Intermediates for the synthesis of halichondrin B analogs |
| 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 |
| HUE049387T2 (hu) | 2013-11-04 | 2020-09-28 | Eisai R&D Man Co Ltd | A halichondrin B analógjainak szintézisében hasznos makrociklizációs reakciók és köztitermékek |
| SG11201604545XA (en) | 2013-12-06 | 2016-07-28 | Eisai R&D Man Co Ltd | Methods useful in the synthesis of halichondrin b analogs |
| CN104860978A (zh) * | 2014-02-20 | 2015-08-26 | 正大天晴药业集团股份有限公司 | 软海绵素b类似物的合成中间体 |
| TW201617326A (zh) | 2014-03-06 | 2016-05-16 | Ａｌｐｈｏｒａ研發股份有限公司 | （ｓ）－１－（（２ｒ，３ｒ，４ｓ，５ｓ）－５－烯丙－３－甲氧－４－（對甲苯磺醯甲基）四氫呋喃－２－基）－３－氨基丙－２－醇之結晶衍生物 |
| JP2017520586A (ja) | 2014-06-30 | 2017-07-27 | 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 | ハリコンドリン類似体の合成およびその使用 |
| WO2016176560A1 (en) | 2015-04-30 | 2016-11-03 | President And Fellows Of Harvard College | Chromium-mediated coupling and application to the synthesis of halichondrins |
| KR102743950B1 (ko) * | 2015-05-07 | 2024-12-18 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 마크롤라이드의 합성에 유용한 마크로고리화 반응 및 중간체 및 기타 단편 |
| JP6786610B2 (ja) | 2016-02-12 | 2020-11-18 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | エリブリンの合成における中間体および関連する合成方法 |
| KR102456433B1 (ko) | 2016-03-02 | 2022-10-19 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 에리불린-기반 항체-약물 콘주게이트 및 사용 방법 |
| MX390072B (es) | 2016-06-30 | 2025-03-20 | Eisai R&D Man Co Ltd | Reaccion de prins e intermediarios utiles en la sintesis de macrolidos de halicondrina y analogos de los mismos. |
| 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 |
| HRP20221385T1 (hr) | 2017-04-05 | 2023-01-06 | President And Fellows Of Harvard College | Makrociklički spoj i njegova uporaba |
| CN108948064B (zh) * | 2017-05-17 | 2021-02-02 | 上海时莱生物技术有限公司 | 一种艾日布林中间体及其制备方法 |
| US11548898B2 (en) | 2017-07-06 | 2023-01-10 | President And Fellows Of Harvard College | Synthesis of halichondrins |
| US11498892B2 (en) | 2017-07-06 | 2022-11-15 | President And Fellows Of Harvard College | Fe/Cu-mediated ketone synthesis |
| EP3710454B1 (en) | 2017-11-15 | 2024-01-03 | President And Fellows Of Harvard College | Macrocyclic compounds and uses thereof |
| WO2019102490A1 (en) * | 2017-11-21 | 2019-05-31 | Natco Pharma Limited | Intermediates for the preparation of eribulin thereof |
| KR102799793B1 (ko) | 2018-01-03 | 2025-04-25 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 마크롤리드 및 그의 유사체의 합성에 유용한 프린스 반응 및 화합물 |
| CN112437775A (zh) * | 2018-07-20 | 2021-03-02 | 雷迪博士实验室有限公司 | 用于制备艾日布林及其中间体的纯化方法 |
| CN112409302A (zh) * | 2019-08-22 | 2021-02-26 | 上海茂晟康慧科技有限公司 | 一种艾日布林中间体er806060的合成方法 |
| CN114409616A (zh) * | 2021-12-28 | 2022-04-29 | 南京格亚医药科技有限公司 | 一种甲磺酸艾日布林关键中间体异构体的制备方法 |
| WO2023144733A1 (en) * | 2022-01-26 | 2023-08-03 | Simon Fraser University | Compounds and processes for the preparation of eribulin |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5436238A (en) | 1992-03-12 | 1995-07-25 | President And Fellows Of Harvard College | Halichondrins and related compounds |
| US5338865A (en) | 1992-03-12 | 1994-08-16 | President And Fellows Of Harvard College | Synthesis of halichondrin B and norhalichondrin B |
| IL139960A0 (en) * | 1998-06-17 | 2002-02-10 | Eisai Co Ltd | Macrocylic analogs and methods of their use and preparation |
| PL2522663T3 (pl) | 2004-06-03 | 2015-08-31 | Eisai R&D Man Co Ltd | Produkty pośrednie do otrzymywania halichondryny B |
| US8598373B2 (en) | 2008-04-04 | 2013-12-03 | Eisai R&D Management Co., Ltd. | Halichondrin B analogs |
| 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 |
| WO2013014299A1 (es) | 2011-07-27 | 2013-01-31 | GARCÍA VÁZQUEZ, Maria | Dispositivo y procedimiento para la generación de electricidad a partir de agua presurizada y de al menos un material explosivo |
| WO2013142999A1 (en) * | 2012-03-30 | 2013-10-03 | Alphora Research Inc. | Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein |
-
2014
- 2014-05-30 JP JP2016522151A patent/JP6511613B2/ja not_active Expired - Fee Related
- 2014-05-30 AU AU2014286880A patent/AU2014286880B2/en not_active Ceased
- 2014-05-30 EP EP14819850.0A patent/EP3016957A4/en not_active Withdrawn
- 2014-05-30 WO PCT/CA2014/050504 patent/WO2015000070A1/en not_active Ceased
- 2014-05-30 US US14/901,481 patent/US9850254B2/en active Active
- 2014-05-30 CN CN201480037966.0A patent/CN105431438A/zh active Pending
- 2014-05-30 CA CA2916537A patent/CA2916537C/en not_active Expired - Fee Related
- 2014-06-13 TW TW103120601A patent/TW201522345A/zh unknown
- 2014-06-18 AR ARP140102304A patent/AR096643A1/es unknown
- 2014-07-02 UY UY35641A patent/UY35641A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN105431438A (zh) | 2016-03-23 |
| AR096643A1 (es) | 2016-01-20 |
| CA2916537A1 (en) | 2015-01-08 |
| US9850254B2 (en) | 2017-12-26 |
| AU2014286880A2 (en) | 2016-03-03 |
| EP3016957A4 (en) | 2016-11-30 |
| CA2916537C (en) | 2021-07-27 |
| AU2014286880B2 (en) | 2017-12-14 |
| TW201522345A (zh) | 2015-06-16 |
| EP3016957A1 (en) | 2016-05-11 |
| JP6511613B2 (ja) | 2019-05-15 |
| AU2014286880A1 (en) | 2016-02-18 |
| JP2016528186A (ja) | 2016-09-15 |
| WO2015000070A1 (en) | 2015-01-08 |
| US20160137661A1 (en) | 2016-05-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 109 | Application deemed to be withdrawn |
Effective date: 20211206 |