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1. CN108948064 - Eribulin intermediates and preparation method thereof

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China
Application Number 201710350260.5
Application Date 17.05.2017
Publication Number 108948064
Publication Date 07.12.2018
Grant Number 108948064
Grant Date 02.02.2021
Publication Kind B
IPC
C07F 7/18
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
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
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
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
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 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 493/22
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
C07F 7/188
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
1804Compounds having Si-O-C linkages
1872Preparation; Treatments not provided for in C07F7/20
188by reactions involving the formation of Si-O linkages
C07F 7/1804
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
1804Compounds having Si-O-C linkages
Applicants SHANGHAI SHILAI BIOTECHNOLOGY CO., LTD.
上海时莱生物技术有限公司
Inventors ZHANG FUYAO
张富尧
LI HUOMING
李火明
ZHANG XINNING
张歆宁
Title
(EN) Eribulin intermediates and preparation method thereof
(ZH) 一种艾日布林中间体及其制备方法
Abstract
(EN) The invention relates to Eribulin intermediates and a preparation method thereof. Particularly, the invention relates to compound shown in a formula II, formula III and formula V, wherein Ar is a C1-10 alkyl substituted or alkyloxy substituted or unsubstituted aryl group, R1 and R2 are aldehyde acetal protecting groups or thioacetal protecting groups, R3 is hydrogen or a hydroxy protecting group,and X is halogen or a leaving group. The invention particularly relates to the preparation method of the compounds shown in the formula II, formula III and formula V. The preparation method has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, and is suitable for large-scale production.
(ZH) 本发明涉及一种艾日布林中间体及其制备方法。具体而言，本发明涉及一种如式II、式III和式V所示的化合物，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。本发明还特别涉及一种如式II、式III和式V所示的化合物的制备方法，该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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