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[目的]寻找具有较高生物活性的四氢吡啶并[4,3-d]嘧啶类农药先导化合物。[方法]以N-Boc-4-哌啶酮-3-甲酸乙酯等为原料,经过4步反应,合成目标化合物(8a)、(8b)及(8c),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)及(8c)在测试浓度下具有较好的杀菌活性,化合物(8a)对番茄早疫病菌的抑制率达76.2%,化合物(8b)、(8c)对棉花枯萎病菌的抑制率分别达66.9%和84.7%。[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 the leading compound of tetrahydropyrido [4,3-d] pyrimidine pesticides with high biological activity. [Method] The target compounds (8a), (8b) and (8c) were synthesized by the reaction of N-Boc-4-piperidone-3-carboxylic acid ethyl ester, MS and HPLC were confirmed and bactericidal activity was determined simultaneously. [Results] The target compounds (8a), (8b) and (8c) had good bactericidal activities under the test concentration. The inhibitory rate of compound (8a) against A. tomentosa was 76.2% ) Inhibited Fusarium oxysporum cotton by 66.9% and 84.7%, respectively. [Conclusion] The target compounds could be used as lead compounds for further research and design of agricultural fungicides.