Preparation method of isavuconazole intermediate
The invention provides a preparation method of an isavuconazole intermediate. Specifically, the present invention provides a method for preparing (2R,3S)-1-(1H-1,2,4-triazol-1-yl)-2-(2,5-difluorophenyl)-3-cyano-2-butanol (an intermediate 10) by carrying out a ring-opening reaction on (2R,3S)-2-(2,5-...
Gespeichert in:
| Hauptverfasser: | , , , , , |
|---|---|
| Format: | Patent |
| Sprache: | chi ; eng |
| Schlagworte: | |
| Online-Zugang: | Volltext bestellen |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | |
|---|---|
| container_issue | |
| container_start_page | |
| container_title | |
| container_volume | |
| creator | SONG CHENG'EN LIN KUAILE PAN JING CHEN LIANG ZHOU WEICHENG ZHOU TING |
| description | The invention provides a preparation method of an isavuconazole intermediate. Specifically, the present invention provides a method for preparing (2R,3S)-1-(1H-1,2,4-triazol-1-yl)-2-(2,5-difluorophenyl)-3-cyano-2-butanol (an intermediate 10) by carrying out a ring-opening reaction on (2R,3S)-2-(2,5-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]ethylene oxide (an intermediate 9) and trimethylcyanosilane in the presence of tetrabutylammonium fluoride (TBAF). The product obtained by the method provided by the invention has high purity and yield, and the method has mild conditions, iseasy to control, and is suitable for industrial mass production.
本发明提供了一种艾沙康唑中间体的制备方法。具体地，本发明提供了一种(2R,3S)-2-(2,5-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]环氧乙烷(中间体9)在正丁基氟化铵(TBAF)存在下与三甲基氰硅烷开环制备(2R,3S)-1-(1H-1,2,4-三唑-1-基)-2-(2,5-二氟苯基)-3-氰基-2-丁醇(中间体10)的方法。通过本发明方法得到的产品纯度和收率高，且该方法条件温和、易控，适合工业放大生产。 |
| format | Patent |
| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_CN110498774A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>CN110498774A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_CN110498774A3</originalsourceid><addsrcrecordid>eNrjZDAIKEotSCxKLMnMz1PITS3JyE9RyE9TyCxOLCtNzs9LrMrPSVXIzCtJLcpNTclMLEnlYWBNS8wpTuWF0twMim6uIc4euqkF-fGpxQWJyal5qSXxzn6GhgYmlhbm5iaOxsSoAQCogSwC</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Preparation method of isavuconazole intermediate</title><source>esp@cenet</source><creator>SONG CHENG'EN ; LIN KUAILE ; PAN JING ; CHEN LIANG ; ZHOU WEICHENG ; ZHOU TING</creator><creatorcontrib>SONG CHENG'EN ; LIN KUAILE ; PAN JING ; CHEN LIANG ; ZHOU WEICHENG ; ZHOU TING</creatorcontrib><description>The invention provides a preparation method of an isavuconazole intermediate. Specifically, the present invention provides a method for preparing (2R,3S)-1-(1H-1,2,4-triazol-1-yl)-2-(2,5-difluorophenyl)-3-cyano-2-butanol (an intermediate 10) by carrying out a ring-opening reaction on (2R,3S)-2-(2,5-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]ethylene oxide (an intermediate 9) and trimethylcyanosilane in the presence of tetrabutylammonium fluoride (TBAF). The product obtained by the method provided by the invention has high purity and yield, and the method has mild conditions, iseasy to control, and is suitable for industrial mass production.
本发明提供了一种艾沙康唑中间体的制备方法。具体地，本发明提供了一种(2R,3S)-2-(2,5-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]环氧乙烷(中间体9)在正丁基氟化铵(TBAF)存在下与三甲基氰硅烷开环制备(2R,3S)-1-(1H-1,2,4-三唑-1-基)-2-(2,5-二氟苯基)-3-氰基-2-丁醇(中间体10)的方法。通过本发明方法得到的产品纯度和收率高，且该方法条件温和、易控，适合工业放大生产。</description><language>chi ; eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2019</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20191126&DB=EPODOC&CC=CN&NR=110498774A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20191126&DB=EPODOC&CC=CN&NR=110498774A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>SONG CHENG'EN</creatorcontrib><creatorcontrib>LIN KUAILE</creatorcontrib><creatorcontrib>PAN JING</creatorcontrib><creatorcontrib>CHEN LIANG</creatorcontrib><creatorcontrib>ZHOU WEICHENG</creatorcontrib><creatorcontrib>ZHOU TING</creatorcontrib><title>Preparation method of isavuconazole intermediate</title><description>The invention provides a preparation method of an isavuconazole intermediate. Specifically, the present invention provides a method for preparing (2R,3S)-1-(1H-1,2,4-triazol-1-yl)-2-(2,5-difluorophenyl)-3-cyano-2-butanol (an intermediate 10) by carrying out a ring-opening reaction on (2R,3S)-2-(2,5-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]ethylene oxide (an intermediate 9) and trimethylcyanosilane in the presence of tetrabutylammonium fluoride (TBAF). The product obtained by the method provided by the invention has high purity and yield, and the method has mild conditions, iseasy to control, and is suitable for industrial mass production.
本发明提供了一种艾沙康唑中间体的制备方法。具体地，本发明提供了一种(2R,3S)-2-(2,5-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]环氧乙烷(中间体9)在正丁基氟化铵(TBAF)存在下与三甲基氰硅烷开环制备(2R,3S)-1-(1H-1,2,4-三唑-1-基)-2-(2,5-二氟苯基)-3-氰基-2-丁醇(中间体10)的方法。通过本发明方法得到的产品纯度和收率高，且该方法条件温和、易控，适合工业放大生产。</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2019</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZDAIKEotSCxKLMnMz1PITS3JyE9RyE9TyCxOLCtNzs9LrMrPSVXIzCtJLcpNTclMLEnlYWBNS8wpTuWF0twMim6uIc4euqkF-fGpxQWJyal5qSXxzn6GhgYmlhbm5iaOxsSoAQCogSwC</recordid><startdate>20191126</startdate><enddate>20191126</enddate><creator>SONG CHENG'EN</creator><creator>LIN KUAILE</creator><creator>PAN JING</creator><creator>CHEN LIANG</creator><creator>ZHOU WEICHENG</creator><creator>ZHOU TING</creator><scope>EVB</scope></search><sort><creationdate>20191126</creationdate><title>Preparation method of isavuconazole intermediate</title><author>SONG CHENG'EN ; LIN KUAILE ; PAN JING ; CHEN LIANG ; ZHOU WEICHENG ; ZHOU TING</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN110498774A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>chi ; eng</language><creationdate>2019</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>SONG CHENG'EN</creatorcontrib><creatorcontrib>LIN KUAILE</creatorcontrib><creatorcontrib>PAN JING</creatorcontrib><creatorcontrib>CHEN LIANG</creatorcontrib><creatorcontrib>ZHOU WEICHENG</creatorcontrib><creatorcontrib>ZHOU TING</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>SONG CHENG'EN</au><au>LIN KUAILE</au><au>PAN JING</au><au>CHEN LIANG</au><au>ZHOU WEICHENG</au><au>ZHOU TING</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Preparation method of isavuconazole intermediate</title><date>2019-11-26</date><risdate>2019</risdate><abstract>The invention provides a preparation method of an isavuconazole intermediate. Specifically, the present invention provides a method for preparing (2R,3S)-1-(1H-1,2,4-triazol-1-yl)-2-(2,5-difluorophenyl)-3-cyano-2-butanol (an intermediate 10) by carrying out a ring-opening reaction on (2R,3S)-2-(2,5-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]ethylene oxide (an intermediate 9) and trimethylcyanosilane in the presence of tetrabutylammonium fluoride (TBAF). The product obtained by the method provided by the invention has high purity and yield, and the method has mild conditions, iseasy to control, and is suitable for industrial mass production.
本发明提供了一种艾沙康唑中间体的制备方法。具体地，本发明提供了一种(2R,3S)-2-(2,5-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]环氧乙烷(中间体9)在正丁基氟化铵(TBAF)存在下与三甲基氰硅烷开环制备(2R,3S)-1-(1H-1,2,4-三唑-1-基)-2-(2,5-二氟苯基)-3-氰基-2-丁醇(中间体10)的方法。通过本发明方法得到的产品纯度和收率高，且该方法条件温和、易控，适合工业放大生产。</abstract><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext_linktorsrc |
| identifier | |
| ispartof | |
| issn | |
| language | chi ; eng |
| recordid | cdi_epo_espacenet_CN110498774A |
| source | esp@cenet |
| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY |
| title | Preparation method of isavuconazole intermediate |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-21T15%3A02%3A48IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-epo_EVB&rft_val_fmt=info:ofi/fmt:kev:mtx:patent&rft.genre=patent&rft.au=SONG%20CHENG'EN&rft.date=2019-11-26&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3ECN110498774A%3C/epo_EVB%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true |