新型含氟Philanthotoxin-12衍生物的无溶剂4组分Ugi反应合成及杀虫活性  

Solvent-free Ugi Four-component Synthesis and Insecticidal Activities of Novel Fluorine-Containing Philanthotoxins-12 Derivatives

作　　者：刘年金[1] 曹松[1] 马严明[1] 申丽[1] 钱旭红[1] 

机构地区：[1]上海市化学生物学重点实验室,华东理工大学药学院氟化学工程中心,上海200237

出　　处：《应用化学》2009年第10期1159-1164,共6页Chinese Journal of Applied Chemistry

基　　金：国家重点基础研究发展规划"九七三"项目(2003CB114405)

摘　　要：以无溶剂4组分Ugi反应合成关键含氟中间体,然后经三氟乙酸脱除保护基,合成了8种新型含氟Philanthotoxin-12衍生物。重要的中间体和目标化合物的结构经1HNMR、13CNMR和HRMS或MS测试技术的确认。对目标化合物进行了初步的杀虫活性测试,其中含氟的化合物6b在100mg/L浓度下对棉铃虫和菜青虫的杀死率分别为44%和42%。Eight novel fluorine-containing PhTX-12 derivatives were prepared from the intermediate obtained via one-pot Ugi four-component solvent-free reactions by the simple removal of the protecting groups in the presence of trifluoroacetic acid. Their structures were identified by ^1H NMR, ^13C NMR and HRMS or MS. Preliminary bioassays indicate that compound 6b showed 44% and 42% mortality rates against Heliothis armigera and Pieris rapae respectively at a concentration of 100 mg/L.

关 键 词：Philanthotoxin 无溶剂合成 4组分Ugi反应 杀虫活性 

分 类 号：O625.2[理学—有机化学]