CAJ | 학술논문

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~1H NMR、~(13)C NMR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100 mg/L浓度下对棉铃虫和菜青虫的杀死率分别为44%和42%.
이무용제4조분Ugi반응합성관건함불중간체,연후경삼불을산탈제보호기,합성료8충신형함불Philanthotoxin-12연생물. 중요적중간체화목표화합물적결구경~1H NMR、~(13)C NMR화HRMS혹MS측시기술적학인. 대목표화합물진행료초보적살충활성측시,기중함불적화합물6b재100 mg/L농도하대면령충화채청충적살사솔분별위44%화42%.
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, ~(13)C 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.