制备2-(5-氨基-1-芳基-1 H -1,2,3-三唑-4-基)-2-亚氨基乙腈和2-(5-氨基-1-芳基-1)的温和方法通过二氨基马来腈与苯基/取代的苯基重氮氯化物的反应获得H -1,2,3-三唑-4-基)-2-氧代乙腈。4-硝基苯基重氮氯化物得到2-氨基-3-(3-(4-(硝基苯基)三唑-1-en-1-基)马来腈。三唑iminoacetonitrile和马来腈衍生物与过量的丙酮和苯甲醛进一步反应用1,8-二氮杂双环[5.4.0]十一碳-7-烯的催化量以得到5 -(5-亚氨基甲基-2,2-二甲基-2, 5-二氢恶唑-4-基)-3-芳基-3 H -1,2,3-三唑-4-胺和(E)-N-亚苄基-5-(5-亚氨基-2-芳基-2,5-二氢恶唑-4-基)-3-芳基-3 H -1,2,3-三唑-4-胺。当三唑氧乙腈和马来腈衍生物与乙酸羟胺在乙酸钠存在下反应时,观察到两个竞争反应,即亲核取代和亲核加成。
Synthesis, reactions, and biological activity of 1,4-benzothiazine derivatives
作者:Eman M. H. Abbas、Thoraya A. Farghaly
DOI:10.1007/s00706-010-0312-6
日期:2010.6
7-Dimethoxy-2H-1,4-benzothiazin-3(4H)-one reacts with dimethylformamide dimethylacetal (DMF-DMA) to give the novel enaminone 2-(dimethylaminomethylene)-6,7-dimethoxy-2H-1,4-benzothiazin-3(4H)-one. The reaction of the latter with various active methylene compounds afforded pyrido[3,2-b][1,4]benzothiazines. Also, coupling of the enaminone with diazotized aniline derivatives gave 2-(arylhydrazono)-6,7-dimethoxy-2H-1
摘要6,7-二甲氧基-2 H -1,4-苯并噻嗪-3(4 H)-与二甲基甲酰胺二甲基缩醛(DMF-DMA)反应生成新的烯胺基2-(二甲基氨基亚甲基)-6,7-二甲氧基-2 H -1,4-苯并噻嗪-3(4 H)-1 。后者与各种活性亚甲基化合物的反应提供了吡啶并[3,2- b ] [1,4]苯并噻嗪。同样,烯胺酮与重氮化苯胺衍生物的偶合得到2-(芳基肼基)-6,7-二甲氧基-2 H -1,4-苯并噻嗪-3(4 H)-那些。光谱数据表明,后者化合物主要以hydr互变异构形式存在。另外,将烯胺酮与重氮化的杂环胺偶联得到四和五杂环体系。筛选了一些合成化合物的抗肿瘤和抗菌活性。 图形概要
ANTIMICROBIAL AND CYTOTOXIC COMPOUNDS AND METHODS FOR TREATING CANCER, A BACTERIAL INFECTION, AND/OR A FUNGAL INFECTION
申请人:King Abdulaziz University
公开号:US20180201598A1
公开(公告)日:2018-07-19
Small molecules and methods of treating cancer, a bacterial infection, and/or a fungal infection. The small molecules are chromenone derivatives. They have antimicrobial properties and are cytotoxic towards colon, liver, and breast cancer cell lines.
Synthesis of 1-Arylazo-3-acetyl-1H-cinnolin-4-one Derivatives
作者:Mohamed S. Abbady、Abd El-Aal M. Gaber
DOI:10.1135/cccc19921149
日期:——
The biological activity of azocinnoline derivatives especially in the chemotherapy of Trypanosomiasis was already reported. Considering the foregoing and in continuation of our previous work, 3-acetyl-1H-cinnolin-4-one (I) has been well exploited as a coupling component.
Farag, Ahmed M.; Hassaneen, Hamdi M.; Abbas, Ikhlas M., Phosphorus and Sulfur and the Related Elements, 1988, vol. 40, p. 243 - 250
作者:Farag, Ahmed M.、Hassaneen, Hamdi M.、Abbas, Ikhlas M.、Shawali, Ahmad S.、Algharib, Mohamad S.
DOI:——
日期:——
Synthesis of 1,4,5-trisubstituted-1,2,3-triazoles via coupling reaction of diaminomaleonitrile with aromatic diazonium salts
作者:Amal Al-Azmi、Anita K. Kalarikkal
DOI:10.1016/j.tet.2013.11.003
日期:2013.12
3-triazol-4-yl)-2-iminoacetonitriles and 2-(5-amino-1-aryl-1H-1,2,3-triazol-4-yl)-2-oxoacetonitriles was achieved by the reaction of diaminomaleonitrile and phenyl/substituted phenyl diazonium chlorides. 4-Nitrophenyl diazonium chloride afforded 2-amino-3-(3-(4-nitrophenyl)triaz-1-en-1-yl)maleonitrile. Triazole iminoacetonitrile and maleonitrile derivatives were reacted further with excess acetone and benzaldehyde
制备2-(5-氨基-1-芳基-1 H -1,2,3-三唑-4-基)-2-亚氨基乙腈和2-(5-氨基-1-芳基-1)的温和方法通过二氨基马来腈与苯基/取代的苯基重氮氯化物的反应获得H -1,2,3-三唑-4-基)-2-氧代乙腈。4-硝基苯基重氮氯化物得到2-氨基-3-(3-(4-(硝基苯基)三唑-1-en-1-基)马来腈。三唑iminoacetonitrile和马来腈衍生物与过量的丙酮和苯甲醛进一步反应用1,8-二氮杂双环[5.4.0]十一碳-7-烯的催化量以得到5 -(5-亚氨基甲基-2,2-二甲基-2, 5-二氢恶唑-4-基)-3-芳基-3 H -1,2,3-三唑-4-胺和(E)-N-亚苄基-5-(5-亚氨基-2-芳基-2,5-二氢恶唑-4-基)-3-芳基-3 H -1,2,3-三唑-4-胺。当三唑氧乙腈和马来腈衍生物与乙酸羟胺在乙酸钠存在下反应时,观察到两个竞争反应,即亲核取代和亲核加成。