[1]杨汉民,陈阳露,郑文.N|取代邻苯二甲酰亚胺衍生物的合成研究[J].徐州工程学院学报(自然科学版),2020,(03):37-40.
　YANG Hanmin,CHEN Yanglu,ZHENG Wen.Synthesis of N|substituted Phthalimide Derivatives[J].Journal of Xuzhou Institute of Technology(Natural Sciences Edition),2020,(03):37-40.
点击复制

N|取代邻苯二甲酰亚胺衍生物的合成研究()
分享到：

《徐州工程学院学报》（自然科学版）[ISSN:1674-358X/CN:32-1789/N]

卷:
期数:
2020年03期
页码:
37-40
栏目:
教授论坛
出版日期:
2020-09-30

文章信息/Info

Title:
Synthesis of N|substituted Phthalimide Derivatives
文章编号:
1674-358X(2020)03-0037-04
作者:
杨汉民1; 陈阳露1; 郑文2
(1.中南民族大学 化学与材料科学学院,湖北 武汉430074; 2.武汉朋和科技有限公司,湖北 武汉430074 )
Author(s):
YANG Hanmin1; CHEN Yanglu1; ZHENG Wen2
(1.School of Chemistry and Materials Science,South|Central University for Nationalities,Wuhan 430074,China; 2.Wuhan Penghe Technology Co.,Ltd.,Wuhan 430074,China)
关键词:
1; 2; 3|苯三甲酸;  免疫调节剂;  温和条件
Keywords:
1; 2; 3|benzenetricarboxylic acid;  immunomodulator;  mild conditions
分类号:
TQ246.1
文献标志码:
A
摘要:
以 1,2,3|苯三甲酸为原料,依次经分子内脱水、胺解反应、酯化和酰胺缩合反应合成了用于生产新生血管生成抑制剂和免疫调节剂的医药中间体N|取代邻苯二甲酰亚胺衍生物.反应可在温和条件下进行,且有较高产率,适用于工业化生产.
Abstract:
Using 1,2,3|benzenetricarboxylic acid as the raw material,a pharmaceutical intermediate N|substituted pthalmide derivatives for the production of angiogenesis inhibitors and immunomodulators was synthesized via intramolecular dehydration,amination reaction,esterification and amide condensation.The reaction can be carried out under mild conditions and has a higher yield,which is suitable for industrial production.

参考文献/References:

[1] 吕文文,孙迎东,姜宏,等.新型N|取代邻苯二甲酰亚胺类衍生物抗肿瘤血管生成活性评价[J].药学研究,2016,35(10):583|586.
[2] MÜLLER G,STIRLING D,CORRAL L,et al.Discovery of(S)|N| {2|[1|(3|ethoxy|4|methoxyphenyl)|2|methanesulfonylethyl] |1,3|dioxo|2,3|dihydro|1H|isoindol|4|yl}acetamide(apremilast),a potent and orally active phosp hodieste|rase 4 and tumor necrosis factor|αinhibitor[J].Journal of Medicinal Chemistry,2009,52(6):1522|1524.
[3] 张文娟,罗浩,李锐,等.新型PI3K抑制剂邻苯二甲酰亚胺及其衍生物的设计合成与抗肿瘤活性[J].中国药物化学杂志,2013,23(3):181|186.
[4] GEORGE W M,MARY G S,WONG L W,et al.Thalidomide analogs and PDE4 inhibition[J].Bioorganic & Medicinal Chemistry Letters,1998,8(19):2669|2674.
[5] D'AMATO R J,LOUGHMAN M S,FLYNN E,et al.Thalidomide is an inhibitor of angiogenesis[J].Proceedings of the National Academy of Sciences of the United States of America,1994,91(9):4082|4085.
[6] GALUSTIAN C,MEYER B,LABARTHE M C,et al.The anticancer agents lenalidomide and pomalidomide inhibit the proliferation and function of T regulatory cells[J].Cancer Immuno l Immunother,2009,58(7):1033|1045.
[7] SCHAFER F H,GANDHI A K,LOVELAND M A,et al.Enhancement of cytokine production and AP|1 transcriptional activity in T cells by thalidomide |related immunomodulatory drugs[J].Journal of Pharmacology & Experimental Therapeutics,2003,305(3):1222|1232.
[8] ITO H,WILLSON C G,FRECHET J M J.Positive/negative mid UV resist with high thermal stability[J].Proceedings of SPIE | The International Society for Optical Engineering,1987,771:24|31.
[9] 吕早生,黄吉林,赵金龙,等.2|丁炔|1,4|二醇双对甲苯磺酸酯的合成工艺研究[J].化学与生物工程,2012(19):56|58.)
[10] RASBENY R D,WU X Y,BULLOCH B N,et al.A small molecule diacid with long|term chiral memory[J].Organic Letters,2009,11(12):2599|2602.

相似文献/References:

[1]李同祥,李文,孙会刚,等.农药2,4-滴丁酯与敌敌畏降解菌株的筛选及性能研究[J].徐州工程学院学报(自然科学版),2017,(2):30.
　LI Tongxiang,LI Wen,SUN Huigang,et al.Identification and Degradation of a Bacterium LT1 in Degrading Pesticide 2,4-D Butyl Ester and DDVP[J].Journal of Xuzhou Institute of Technology(Natural Sciences Edition),2017,(03):30.

备注/Memo

备注/Memo:
收稿日期:2020-01-09
作者简介:杨汉民(1968-),男,教授,博士,硕士生导师,主要从事有机化学研究.
更新日期/Last Update: 2020-09-30