为了寻找新的含苯并噻(噁)唑稠杂环农药先导化合物,利用(6-氯)-苯并噻(噁)唑酮与取代苯基异氰酸酯发生偶合反应,合成了15个N-取代苯基-苯并噻(噁)唑酮-3-甲酰胺化合物3,并利用1H NMR,IR,MS及元素分析对其结构进行了表征.初步生物活性试验结果表明,在试验浓度下部分目标化合物具有一定的杀菌和杀虫活性.考察了部分过渡金属催化剂对该偶合反应的催化效果,结果表明在钯催化、温和条件下即可较高产率得到产物.
In order to find new benzothiazole/benzoxazole lead compounds,15 N-arylaminocarbonyl-2-benzothiazolinone/benzoxazolone derivatives were synthesized from a coupling reaction of 2-benzothia-zolinone/benzoxazolone and aryl isocyanates catalyzed by transition-metal.Their structures were confirmed by 1H NMR,IR,MS techniques and elemental analysis.The preliminary bioassay showed that some of them exhibited certain fungicidal and insecticidal activities.The influence of some transition-metal catalyst on the coupling reaction was studied.The results showed that the corresponding prducts were obtained in high yields in the presence of palladium catalyst under mild reaction conditions.