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[目的]寻找具有较高生物活性的吡咯并[3,4-d]嘧啶类农药先导化合物。[方法]以N-叔丁氧羰基-4-氧代-3-吡咯烷甲酸乙酯等为原料,经过4步反应,合成目标化合物8a、8b、8c及8d,其结构经 ~1H NMR、LC-MS和HPLC确证且同时进行杀菌活性测定。[结果]目标化合物8a、8b、8c及8d在测试浓度下具有较好的杀菌活性,化合物8a对黄瓜灰霉病菌的抑制率达49.8%,化合物8b和8d对棉花枯萎病菌的抑制率分别达71.3%和80.9%,化合物8c对小麦赤霉病菌抑制率达69.7%。[结论]目标化合物可作为先导化合物进一步研究,设计合成农用杀菌剂。
[Objective] The research aimed to find pyrrolo [3,4-d] pyrimidine pesticide lead compound with high biological activity. [Method] The target compounds 8a, 8b, 8c and 8d were synthesized via 4 steps using ethyl N-tert-butoxycarbonyl-4-oxo-3-pyrrolidinecarboxylate as starting material. LC-MS and HPLC were confirmed and bactericidal activity was determined simultaneously. [Result] The target compounds 8a, 8b, 8c and 8d had good bactericidal activity under the test concentration. The inhibitory rate of compound 8a to Botrytis cinerea reached 49.8%. The inhibitory rates of compound 8b and 8d to Fusarium oxysporum were 71.3% and 80.9% respectively. The inhibitory rate of compound 8c against Gibberella zeae was 69.7%. [Conclusion] The target compounds could be used as lead compounds for further research and design of synthetic agricultural fungicides.