2-烷(芳)氧基苯并呋喃并[3,2-d]嘧啶-4(3H)-酮衍生物的合成及杀菌活性

应用膦亚胺3与芳基异氰酸酯的氮杂Wittig反应, 生成碳二亚胺4, 4再分别与酚、醇作用, 在碳酸钾或醇钠催化下关环, 以72%～88%的产率合成了2-烷(芳)氧基取代-苯并呋喃并[3,2-d]嘧啶-4(3H)-酮衍生物5和6, 其结构经IR, 1H NMR, MS和元素分析证实. 初步生物活性测试表明该类化合物表现出温和的杀菌活性. 如5f在50 mg/L浓度时, 对黄瓜灰霉菌的抑制率为55%.

Synthesis and Fungicidal Activity of 2-Alkoxy(aryloxy)-benzofuro- [3,2-d]pyrimidin-4(3H)-one Derivatives

The aza-Wittig reaction of iminophosphorane 3 with aromatic isocyanates gave carbodiimides 4, which were allowed to react further with various phenols and alcohols in the presence of a catalytic amount of solid potassium carbonate or sodium ethoxide to give 2-alkoxy(aryloxy)-benzofuro[3,2-d]pyrimidin- 4(3H)-ones in 72%～88% yields. Their structures were confirmed by 1H NMR, MS, IR and elemental analysis. The preliminary bioassays indicated that these compounds possessed moderate fungicidal activities against six kinds of fungi at a concentration of 50 mg/L.