1,3-偶极环加成法合成异噁唑啉新化合物及其生物活性的研究

Synthesis of Isoxazolines by 1,3-Dipolar Cycloaddition and Their Bioactivity

以N-甲羟胺硫酸盐和芳香族羰基化合物为主要原料合成了一系列不同的1,3-偶极化合物,并合成了四种不同的单取代苯乙烯.以该系列1,3-偶极化合物和单取代苯乙烯为主要中间体,采用1,3-偶极环加成反应合成了一系列异噁唑啉类新化合物.同时研究了1,3-偶极化合物与单取代烯发生的1,3-偶极环加成反应,该合成过程为理想的绿色反应,合成产物是5位取代异噁唑啉.通过质谱和核磁共振等表征了化合物的化学结构.同时对系列异噁唑啉类新化合物进行了实验室内植物生物活性的测试,发现了对植物灰霉病有效的新化合物.

A series of new isoxazolines were prepared by 1,3-dipolar cycloaddition between different mono-substituted styrenes and new 1,3-dipolar compounds which were synthesized by the reaction of N-methylhydroxylamine sulfate with aromatic carbonyl compounds. This synthetic pathway of 5-substituted isoxazolines was an good process in green chemistry. The chemical structures of these products were characterized by ^1H NMR, ^13C NMR, COSY, HSQC and DEPT. Their bioactivities have been tested also in the laboratory, finding that some new compounds inhibited Botrytis Cinerea effectively.