5-(aminomethyl)-4-aryl thiophene-2-amine derivative and preparation method thereof
The invention discloses a 5-(aminomethyl)-4-aryl thiophene-2-amine derivative and a preparation method thereof. The preparation method comprises the steps that 3-aryl-substituted propargyl alcohol, N-protected amine, N-halogenated succinimide and thiourea or a thiourea derivative serve as raw materi...
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| creator | ZHAI JIULONG YANG HONG GUO HUIFENG WANG ZHIHAI ZHANG HUA LI TIANTIAN YIN YAN ZHANG QINGLIN WANG YAN |
| description | The invention discloses a 5-(aminomethyl)-4-aryl thiophene-2-amine derivative and a preparation method thereof. The preparation method comprises the steps that 3-aryl-substituted propargyl alcohol, N-protected amine, N-halogenated succinimide and thiourea or a thiourea derivative serve as raw materials and are subjected to a multi-step cascade reaction under the catalytic action of acid, and therefore, one-pot synthesis of 5-(aminomethyl)-4-aryl thiophene-2-amine derivative is realized. The preparation yield of 5-(aminomethyl)-4-aryl thiophene-2-amine ranges from 15% to 80%, the method has the advantages of being easy to operate, mild in condition, high in yield and the like, and a brand-new synthesis method is provided for the 5-(aminomethyl)-4-aryl thiophene-2-amine derivative.
本发明公开了一种5-(氨基甲基)-4-芳基噻吩-2-胺衍生物及其制备方法，该制备方法以3位芳基取代的炔丙醇、N保护的胺、N-卤代丁二酰亚胺、和硫脲或硫脲衍生物为原料，在酸催化作用下进行多步串联反应，从而实现5-(氨基甲基)-4-芳基噻吩-2-胺衍生物的一锅法合成。本发明的5-(氨基甲基)-4-芳基噻吩-2-胺的制备产率在15％～80％之间，具有操作简单、条件温和、产率高等优点，为5-(氨基甲基)-4-芳基噻吩-2-胺衍生物提供了一种全新的合成方法。 |
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本发明公开了一种5-(氨基甲基)-4-芳基噻吩-2-胺衍生物及其制备方法，该制备方法以3位芳基取代的炔丙醇、N保护的胺、N-卤代丁二酰亚胺、和硫脲或硫脲衍生物为原料，在酸催化作用下进行多步串联反应，从而实现5-(氨基甲基)-4-芳基噻吩-2-胺衍生物的一锅法合成。本发明的5-(氨基甲基)-4-芳基噻吩-2-胺的制备产率在15％～80％之间，具有操作简单、条件温和、产率高等优点，为5-(氨基甲基)-4-芳基噻吩-2-胺衍生物提供了一种全新的合成方法。</description><language>chi ; eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2021</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=20210806&DB=EPODOC&CC=CN&NR=113214183A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,309,782,887,25571,76555</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20210806&DB=EPODOC&CC=CN&NR=113214183A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>ZHAI JIULONG</creatorcontrib><creatorcontrib>YANG HONG</creatorcontrib><creatorcontrib>GUO HUIFENG</creatorcontrib><creatorcontrib>WANG ZHIHAI</creatorcontrib><creatorcontrib>ZHANG HUA</creatorcontrib><creatorcontrib>LI TIANTIAN</creatorcontrib><creatorcontrib>YIN YAN</creatorcontrib><creatorcontrib>ZHANG QINGLIN</creatorcontrib><creatorcontrib>WANG YAN</creatorcontrib><title>5-(aminomethyl)-4-aryl thiophene-2-amine derivative and preparation method thereof</title><description>The invention discloses a 5-(aminomethyl)-4-aryl thiophene-2-amine derivative and a preparation method thereof. The preparation method comprises the steps that 3-aryl-substituted propargyl alcohol, N-protected amine, N-halogenated succinimide and thiourea or a thiourea derivative serve as raw materials and are subjected to a multi-step cascade reaction under the catalytic action of acid, and therefore, one-pot synthesis of 5-(aminomethyl)-4-aryl thiophene-2-amine derivative is realized. The preparation yield of 5-(aminomethyl)-4-aryl thiophene-2-amine ranges from 15% to 80%, the method has the advantages of being easy to operate, mild in condition, high in yield and the like, and a brand-new synthesis method is provided for the 5-(aminomethyl)-4-aryl thiophene-2-amine derivative.
本发明公开了一种5-(氨基甲基)-4-芳基噻吩-2-胺衍生物及其制备方法，该制备方法以3位芳基取代的炔丙醇、N保护的胺、N-卤代丁二酰亚胺、和硫脲或硫脲衍生物为原料，在酸催化作用下进行多步串联反应，从而实现5-(氨基甲基)-4-芳基噻吩-2-胺衍生物的一锅法合成。本发明的5-(氨基甲基)-4-芳基噻吩-2-胺的制备产率在15％～80％之间，具有操作简单、条件温和、产率高等优点，为5-(氨基甲基)-4-芳基噻吩-2-胺衍生物提供了一种全新的合成方法。</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>eNrjZAgy1dVIzM3My89NLcmozNHUNdFNLKrMUSjJyMwvyEjNS9U10gXJpyqkpBZlliWWZJalKiTmpSgUFKUWJBYB-fl5CiC9-SlAPalFqflpPAysaYk5xam8UJqbQdHNNcTZQze1ID8-tbggMRlobEm8s5-hobGRoYmhhbGjMTFqAKKUN1w</recordid><startdate>20210806</startdate><enddate>20210806</enddate><creator>ZHAI JIULONG</creator><creator>YANG HONG</creator><creator>GUO HUIFENG</creator><creator>WANG ZHIHAI</creator><creator>ZHANG HUA</creator><creator>LI TIANTIAN</creator><creator>YIN YAN</creator><creator>ZHANG QINGLIN</creator><creator>WANG YAN</creator><scope>EVB</scope></search><sort><creationdate>20210806</creationdate><title>5-(aminomethyl)-4-aryl thiophene-2-amine derivative and preparation method thereof</title><author>ZHAI JIULONG ; YANG HONG ; GUO HUIFENG ; WANG ZHIHAI ; ZHANG HUA ; LI TIANTIAN ; YIN YAN ; ZHANG QINGLIN ; WANG YAN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN113214183A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>chi ; eng</language><creationdate>2021</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>ZHAI JIULONG</creatorcontrib><creatorcontrib>YANG HONG</creatorcontrib><creatorcontrib>GUO HUIFENG</creatorcontrib><creatorcontrib>WANG ZHIHAI</creatorcontrib><creatorcontrib>ZHANG HUA</creatorcontrib><creatorcontrib>LI TIANTIAN</creatorcontrib><creatorcontrib>YIN YAN</creatorcontrib><creatorcontrib>ZHANG QINGLIN</creatorcontrib><creatorcontrib>WANG YAN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>ZHAI JIULONG</au><au>YANG HONG</au><au>GUO HUIFENG</au><au>WANG ZHIHAI</au><au>ZHANG HUA</au><au>LI TIANTIAN</au><au>YIN YAN</au><au>ZHANG QINGLIN</au><au>WANG YAN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>5-(aminomethyl)-4-aryl thiophene-2-amine derivative and preparation method thereof</title><date>2021-08-06</date><risdate>2021</risdate><abstract>The invention discloses a 5-(aminomethyl)-4-aryl thiophene-2-amine derivative and a preparation method thereof. The preparation method comprises the steps that 3-aryl-substituted propargyl alcohol, N-protected amine, N-halogenated succinimide and thiourea or a thiourea derivative serve as raw materials and are subjected to a multi-step cascade reaction under the catalytic action of acid, and therefore, one-pot synthesis of 5-(aminomethyl)-4-aryl thiophene-2-amine derivative is realized. The preparation yield of 5-(aminomethyl)-4-aryl thiophene-2-amine ranges from 15% to 80%, the method has the advantages of being easy to operate, mild in condition, high in yield and the like, and a brand-new synthesis method is provided for the 5-(aminomethyl)-4-aryl thiophene-2-amine derivative.
本发明公开了一种5-(氨基甲基)-4-芳基噻吩-2-胺衍生物及其制备方法，该制备方法以3位芳基取代的炔丙醇、N保护的胺、N-卤代丁二酰亚胺、和硫脲或硫脲衍生物为原料，在酸催化作用下进行多步串联反应，从而实现5-(氨基甲基)-4-芳基噻吩-2-胺衍生物的一锅法合成。本发明的5-(氨基甲基)-4-芳基噻吩-2-胺的制备产率在15％～80％之间，具有操作简单、条件温和、产率高等优点，为5-(氨基甲基)-4-芳基噻吩-2-胺衍生物提供了一种全新的合成方法。</abstract><oa>free_for_read</oa></addata></record> |
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| title | 5-(aminomethyl)-4-aryl thiophene-2-amine derivative and preparation method thereof |
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