Method for synthesizing kukoamine A and analogue thereof
The invention relates to the technical field of medicines, and relates to a method for synthesizing a natural product kukoamine A and analogue thereof. The method comprises the following steps: (1) performing a nucleophilic reaction on hydroxyl, halogen or C1-C10 alkoxy or C1-C10 alkyl substituted o...
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creator | Tian Ye Zhang Hui Liu Jianyu Liu Yifeng Xu Yongnan Zhang Hefeng Liu Dan Zhan Yong Zhao Qingchun Chi Mingshuang Ao Jiwei |
description | The invention relates to the technical field of medicines, and relates to a method for synthesizing a natural product kukoamine A and analogue thereof. The method comprises the following steps: (1) performing a nucleophilic reaction on hydroxyl, halogen or C1-C10 alkoxy or C1-C10 alkyl substituted or unsubstituted benzaldehyde and malonic acid to obtain a compound 1; (2) reacting the compound 1 in the step (1) with N-hydroxy succinimide to obtain a compound 2; (3) reacting the compound 2 with spermine to obtain a compound 3; and (4) reacting the compound 3 with hydrogen to reduce carbon-carbon double bond, and purifying. The preparation method is simple, and provides a compound base to pharmacological activity research of compounds with similar structures.
本发明涉及医药技术领域,涉及天然产物地骨皮甲素及其类似物的合成方法。该方法包括:1)由羟基、卤素或C1-C10烷氧基或C1-C10烷基取代或未取代的苯甲醛与丙二酸进行亲核反应得化合物1;2)步骤1)所得化合物1和N-羟基琥珀酰亚胺反应,得化合物2;3)化合物2和精胺反应,得化合物3;4)化合物3用氢气反应以还原碳-碳双键,纯化即得。本发明制备方法简单,为类似结构化合物的药物活性研究提供了化合物基础。 |
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本发明涉及医药技术领域,涉及天然产物地骨皮甲素及其类似物的合成方法。该方法包括:1)由羟基、卤素或C1-C10烷氧基或C1-C10烷基取代或未取代的苯甲醛与丙二酸进行亲核反应得化合物1;2)步骤1)所得化合物1和N-羟基琥珀酰亚胺反应,得化合物2;3)化合物2和精胺反应,得化合物3;4)化合物3用氢气反应以还原碳-碳双键,纯化即得。本发明制备方法简单,为类似结构化合物的药物活性研究提供了化合物基础。</description><language>chi ; eng</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2016</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=20160831&DB=EPODOC&CC=CN&NR=105906525A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20160831&DB=EPODOC&CC=CN&NR=105906525A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Tian Ye</creatorcontrib><creatorcontrib>Zhang Hui</creatorcontrib><creatorcontrib>Liu Jianyu</creatorcontrib><creatorcontrib>Liu Yifeng</creatorcontrib><creatorcontrib>Xu Yongnan</creatorcontrib><creatorcontrib>Zhang Hefeng</creatorcontrib><creatorcontrib>Liu Dan</creatorcontrib><creatorcontrib>Zhan Yong</creatorcontrib><creatorcontrib>Zhao Qingchun</creatorcontrib><creatorcontrib>Chi Mingshuang</creatorcontrib><creatorcontrib>Ao Jiwei</creatorcontrib><title>Method for synthesizing kukoamine A and analogue thereof</title><description>The invention relates to the technical field of medicines, and relates to a method for synthesizing a natural product kukoamine A and analogue thereof. The method comprises the following steps: (1) performing a nucleophilic reaction on hydroxyl, halogen or C1-C10 alkoxy or C1-C10 alkyl substituted or unsubstituted benzaldehyde and malonic acid to obtain a compound 1; (2) reacting the compound 1 in the step (1) with N-hydroxy succinimide to obtain a compound 2; (3) reacting the compound 2 with spermine to obtain a compound 3; and (4) reacting the compound 3 with hydrogen to reduce carbon-carbon double bond, and purifying. The preparation method is simple, and provides a compound base to pharmacological activity research of compounds with similar structures.
本发明涉及医药技术领域,涉及天然产物地骨皮甲素及其类似物的合成方法。该方法包括:1)由羟基、卤素或C1-C10烷氧基或C1-C10烷基取代或未取代的苯甲醛与丙二酸进行亲核反应得化合物1;2)步骤1)所得化合物1和N-羟基琥珀酰亚胺反应,得化合物2;3)化合物2和精胺反应,得化合物3;4)化合物3用氢气反应以还原碳-碳双键,纯化即得。本发明制备方法简单,为类似结构化合物的药物活性研究提供了化合物基础。</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2016</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLDwTS3JyE9RSMsvUiiuzCvJSC3OrMrMS1fILs3OT8zNzEtVcFRIzEsB4sSc_PTSVAWgkqLU_DQeBta0xJziVF4ozc2g6OYa4uyhm1qQH59aXJCYnJqXWhLv7GdoYGppYGZqZOpoTIwaAAwaLkk</recordid><startdate>20160831</startdate><enddate>20160831</enddate><creator>Tian Ye</creator><creator>Zhang Hui</creator><creator>Liu Jianyu</creator><creator>Liu Yifeng</creator><creator>Xu Yongnan</creator><creator>Zhang Hefeng</creator><creator>Liu Dan</creator><creator>Zhan Yong</creator><creator>Zhao Qingchun</creator><creator>Chi Mingshuang</creator><creator>Ao Jiwei</creator><scope>EVB</scope></search><sort><creationdate>20160831</creationdate><title>Method for synthesizing kukoamine A and analogue thereof</title><author>Tian Ye ; Zhang Hui ; Liu Jianyu ; Liu Yifeng ; Xu Yongnan ; Zhang Hefeng ; Liu Dan ; Zhan Yong ; Zhao Qingchun ; Chi Mingshuang ; Ao Jiwei</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN105906525A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>chi ; eng</language><creationdate>2016</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>Tian Ye</creatorcontrib><creatorcontrib>Zhang Hui</creatorcontrib><creatorcontrib>Liu Jianyu</creatorcontrib><creatorcontrib>Liu Yifeng</creatorcontrib><creatorcontrib>Xu Yongnan</creatorcontrib><creatorcontrib>Zhang Hefeng</creatorcontrib><creatorcontrib>Liu Dan</creatorcontrib><creatorcontrib>Zhan Yong</creatorcontrib><creatorcontrib>Zhao Qingchun</creatorcontrib><creatorcontrib>Chi Mingshuang</creatorcontrib><creatorcontrib>Ao Jiwei</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Tian Ye</au><au>Zhang Hui</au><au>Liu Jianyu</au><au>Liu Yifeng</au><au>Xu Yongnan</au><au>Zhang Hefeng</au><au>Liu Dan</au><au>Zhan Yong</au><au>Zhao Qingchun</au><au>Chi Mingshuang</au><au>Ao Jiwei</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Method for synthesizing kukoamine A and analogue thereof</title><date>2016-08-31</date><risdate>2016</risdate><abstract>The invention relates to the technical field of medicines, and relates to a method for synthesizing a natural product kukoamine A and analogue thereof. The method comprises the following steps: (1) performing a nucleophilic reaction on hydroxyl, halogen or C1-C10 alkoxy or C1-C10 alkyl substituted or unsubstituted benzaldehyde and malonic acid to obtain a compound 1; (2) reacting the compound 1 in the step (1) with N-hydroxy succinimide to obtain a compound 2; (3) reacting the compound 2 with spermine to obtain a compound 3; and (4) reacting the compound 3 with hydrogen to reduce carbon-carbon double bond, and purifying. The preparation method is simple, and provides a compound base to pharmacological activity research of compounds with similar structures.
本发明涉及医药技术领域,涉及天然产物地骨皮甲素及其类似物的合成方法。该方法包括:1)由羟基、卤素或C1-C10烷氧基或C1-C10烷基取代或未取代的苯甲醛与丙二酸进行亲核反应得化合物1;2)步骤1)所得化合物1和N-羟基琥珀酰亚胺反应,得化合物2;3)化合物2和精胺反应,得化合物3;4)化合物3用氢气反应以还原碳-碳双键,纯化即得。本发明制备方法简单,为类似结构化合物的药物活性研究提供了化合物基础。</abstract><oa>free_for_read</oa></addata></record> |
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subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY |
title | Method for synthesizing kukoamine A and analogue thereof |
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