CAS: 105191-41-1; 4-Chloro-3-Formylbenzonitrile

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CAS号914106-36-8 2-氯-5-氰基苯甲酸甲酯 | CAS号89-54-3 5-氨基-2-氯苯甲酸 | CAS号89891-83-8 2-氯-5-氰基苯甲酸 | CAS号80866-80-4 2-氯-5-硝基苄醇 | CAS号105191-40-0 4-Chloro-3-(hyd... | CAS号89951-56-4 5-氨基-2-氯苯甲醇 | CAS号105191-15-9 2-(hydroxymethy... | CAS号105191-14-8 Ethyl 5-cyano-1...

2-氯-5-氰基苯甲酸置于4-二甲氨基吡啶 四氢吡咯,Potassium Tert-Butylate,N,N'-二环己基碳二亚胺,红铝体系中,用 二氯甲烷,甲苯 用作溶剂,化学反应 0.25H,反应生成4-氟-3-甲酰基苯腈
参考文献:Synthesis And In Vitro Antiprotozoal Activities Of Dicationic 3,5-Diphenylisoxazoles
标题:Synthesis And In Vitro Antiprotozoal Activities Of Dicationic 3,5-Diphenylisoxazoles
摘要:3,5-Bis(4-Amidinophenyl)Isoxazole (3)An Analogue Of 2,5-Bis(4-Amidinophenyl)Furan (Furamidine) In Which The Central Furan Ring Is Replaced By Isoxazoleand 42 Novel Analogues Were Prepared By Two General Synthetic Pathways. The 43 Isoxazole Derivatives Were Assayed Against Trypanosoma Brucei Rhodesiense (T. Brucei Rhodesiense) Stib900,Plasmodium Falciparum (P. Falciparum) K1,And Rat Myoblast L6 Cells (For Cytotoxicity) In Vitro. Eleven Compounds (3,13,16-18,22,26,29,31,37,And 41) Exhibited Antitrypanosomal Ic50 Values Less Than 10 Nm,Five Of Which Displayed Cytotoxic Indices (Ratios Of Cytotoxic Ic50 To Antiprotozoal Ic50 Values) At Least 10 Times Higher Than That Of Furamidine. Eighteen Compounds (4-8,12,14,18-22,25,26,28,29,32,And 43 Were More Active Against P. Falciparum Than Furamidine,With Ic50 Values Less Than 15 Nm. Fourteen Of These Compounds Had Cytotoxic Indices Ranging Between 10 And 120 Times Higher Than That Of Furamidine,And Five Analogues Exhibited High Selectivity For P. Falciparum Over T. Brucei Rhodesiense.
Doi:10.1021/jm0612867

专利信息

专利号:US-7951827-B2
优先权日:2005-05-05
标 题:Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles
发明人：TIDWELL RICHARD R; BAKUNOVA SVETLANA M; BAKUNOV STANISLAV; PATRICK DONALD A
权利人:UNIV NORTH CAROLINA
摘要:Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.

专利号:US-2006264487-A1
优先权日:2005-05-05
标 题:Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles

专利号:EP-1719767-A1
优先权日:2005-05-05
标题:Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles

专利号:CA-2545778-A1
优先权日:2005-05-05
标 题:Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles

专利号:CN-1869027-A
优先权日:2005-05-05
标 题:Synthesis and Antiprotozoal Activity of Dicationic 3,5-Diphenylisoxazoles