新型四氢吡啶并[4,3-d]嘧啶类化合物的合成及杀菌活性测定

Synthesis and Fungicidal Activity of Tetrahydropyrido[4,3-d] pyrimidine

[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。

[Aims] The paper aims to find pesticide lead compounds of tetrahydropyrido [4,3-d]pyrimidine with high active bioactivity. [Methods] The target compounds（8a）, （8b） and （8c） were synthesized after 4 steps with 1-tert-butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate and so on as materials. The target compounds were characterized by ^1H NMR, LC-MS and HPLC and determinated for fungicidal activity. [Results] The target compounds （8a）, （8b） and （8c） showed good fungicidal activity under test concertration, 76.2% of inhibition rate for A lternaria solani, 66.9% of inhibition rate for Fusarium oxysporum and 84.7% of inhibition rate for Fusarium oxysporum respectively. [Conclusions] The target compounds might be considered as promising lead compounds for further design and synthesis of agricultural fungicides.