Intermediate of eribulin and preparation method therefor

Intermediate of eribulin and preparation method therefor

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 ac...

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Hauptverfasser: Zhang, Xinning, Li, Huoming, Zhang, Fuyao
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator Zhang, Xinning
Li, Huoming
Zhang, Fuyao
description 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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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. 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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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2021</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNyrEOAUEQBuBtFIJ3GA8gsQRXE0KN-jLsv7lN7mY2c-P9NR5A9TXfNDQ3cdiAVNhBmglWXp--CLEkqobKxl5UaIB3msg7GLLaPEwy9yMWP2dheTk_TtcVqrYYK78h8PZ5jzE2-91hfdxs_zlfM84uzw</recordid><startdate>20211130</startdate><enddate>20211130</enddate><creator>Zhang, Xinning</creator><creator>Li, Huoming</creator><creator>Zhang, Fuyao</creator><scope>EVB</scope></search><sort><creationdate>20211130</creationdate><title>Intermediate of eribulin and preparation method therefor</title><author>Zhang, Xinning ; Li, Huoming ; Zhang, Fuyao</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US11186570B23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2021</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>Zhang, Xinning</creatorcontrib><creatorcontrib>Li, Huoming</creatorcontrib><creatorcontrib>Zhang, Fuyao</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Zhang, Xinning</au><au>Li, Huoming</au><au>Zhang, Fuyao</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Intermediate of eribulin and preparation method therefor</title><date>2021-11-30</date><risdate>2021</risdate><abstract>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.</abstract><oa>free_for_read</oa></addata></record>
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HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Intermediate of eribulin and preparation method therefor
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