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1. EP3626723 - INTERMEDIATE OF ERIBULIN AND PREPARATION METHOD THEREFOR

Office
European Patent Office
Application Number 18801562
Application Date 17.05.2018
Publication Number 3626723
Publication Date 25.03.2020
Publication Kind B1
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 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 C07D405/183
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 C07D405/183
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
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
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
Applicants SELECTION BIOSCIENCE LLC
Inventors ZHANG FUYAO
LI HUOMING
ZHANG XINNING
Designated States
Title
(DE) ZWISCHENPRODUKT VON ERIBULIN UND HERSTELLUNGSVERFAHREN DAFÜR
(EN) INTERMEDIATE OF ERIBULIN AND PREPARATION METHOD THEREFOR
(FR) INTERMÉDIAIRE D'ÉRIBULINE ET PROCÉDÉ DE PRÉPARATION ASSOCIÉ
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 C1-10alkyl substituted, alkyloxy substituted or unsubstituted aryl; R1and R2is an acetal protecting group or a thioacetal protecting group; R3is 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.