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1. US20200095235 - Intermediate of eribulin and preparation method therefor

Office
United States of America
Application Number 16613329
Application Date 17.05.2018
Publication Number 20200095235
Publication Date 26.03.2020
Grant Number 11186570
Grant Date 30.11.2021
Publication Kind B2
IPC
C07D 307/30
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
30with 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
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 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 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
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 407/14
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 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 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 SELECTION BIOSCIENCE LLC
Inventors Fuyao Zhang
Huoming Li
Xinning Zhang
Agents MH2 Technology Law Group LLP
Title
(EN) Intermediate of eribulin and preparation method therefor
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.

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