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1. WO2018210297 - INTERMEDIATE OF ERIBULIN AND PREPARATION METHOD THEREFOR

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Publication Number WO/2018/210297
Publication Date 22.11.2018
International Application No. PCT/CN2018/087247
International Filing Date 17.05.2018
IPC
C07F 7/18 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
7Compounds containing elements of Groups 4 or 14 of the Periodic System
02Silicon compounds
08Compounds having one or more C-Si linkages
18Compounds having one or more C-Si linkages as well as one or more C-O-Si linkages
C07D 407/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
407Heterocyclic 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 C07D405/183
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 307/28 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
26having one double bond between ring members or between a ring member and a non-ring member
28with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 493/22 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
22in which the condensed system contains four or more hetero rings
CPC
C07D 307/28
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
26having one double bond between ring members or between a ring member and a non-ring member
28with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 407/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
407Heterocyclic 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
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 407/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
407Heterocyclic 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
14containing three or more hetero rings
C07D 409/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 493/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • 上海时莱生物技术有限公司 SELECTION BIOSCIENCE LLC [CN]/[CN]
Inventors
  • 张富尧 ZHANG, Fuyao
  • 李火明 LI, Huoming
  • 张歆宁 ZHANG, Xinning
Agents
  • 上海弼兴律师事务所 SHANGHAI BESHINING LAW OFFICE
Priority Data
201710350260.517.05.2017CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) INTERMEDIATE OF ERIBULIN AND PREPARATION METHOD THEREFOR
(FR) INTERMÉDIAIRE D'ÉRIBULINE ET PROCÉDÉ DE PRÉPARATION ASSOCIÉ
(ZH) 一种艾日布林中间体及其制备方法
front page image
Abstract
(EN) Disclosed are an intermediate of Eribulin and a preparation method therefor. In particular, disclosed are compounds as represented by formula II, formula III and formula V and a preparation method therefor. Ar is C1-10 alkyl substituted, alkyloxy substituted or unsubstituted aryl; R1 and R2 is an acetal protecting group or a thioacetal protecting group; R3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.
(FR) La présente invention concerne un intermédiaire d'éribuline et son procédé de préparation. En particulier, l'invention concerne des composés représentés par la formule II, la formule III et la formule V et leur procédé de préparation. Ar est un aryle en C1-10 substitué par un alkyle, substitué par un alkyloxy ou non substitué ; R1 et R2 représentent un groupe protecteur acétal ou un groupe protecteur thioacétal ; R3 représente l'hydrogène ou un groupe protecteur hydroxyle ; et X représente l'halogène ou un groupe partant. Le procédé de préparation de l'invention présente des avantages de conditions de réaction modérées, de sélectivité élevée, de purification facile, de faible coût de synthèse et analogues, et peut être considéré pour une production à grande échelle.
(ZH) 一种艾日布林中间体及其制备方法被公开，具体而言，如式II、式III和式V所示的化合物及其制备方法被公开，其中，Ar为C1-10烷基取代或烷基氧基取代或非取代的芳基；R1，R2为缩醛保护基团或者硫缩醛保护基团；R3为氢或者羟基保护基；X为卤素或者离去基团，其制备方法具有反应条件温和，选择性高，易于纯化，合成成本低廉等优点，适于大规模生产。
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