2-烷氧基-3H-喹唑啉-4-酮的合成与杀菌活性

研究了合成2-烷氧基-3H-喹唑啉-4-酮衍生物4的方法,该方法应用膦亚胺1与芳基异氰酸酯的氮杂Wittig反应,得到的碳二亚胺2再与醇在醇钠催化下反应,合成了12种未见文献报道的喹唑啉酮衍生物4.所得产物4的结构由NMR,MS,IR所确证.探讨了成环反应的条件以及所合成的新型杂环化合物的杀菌活性,结果表明部分化合物表现出较好的抑菌活性,如41在50 mg/L浓度时,对水稻纹枯菌的抑制率为89%.

Synthesis and Fungicidal Activities of 2-Alkoxy-3H-quinazolin-4-ones

Twelve unreported 2-alkoxy-3H-quinazolin-4-ones 4 were synthesized by a new synthetic method, which included aza-Wittig reaction of iminophosphorane 1 with aromatic isocynates to give carbodiimides 2 and subsequent reaction of 2 with various ROH in presence of catalytic NaOR. The structure of 4 was confirmed by 1H NMR, MS and IR analysis. The conditions of cyclization and the biological activities of these new compounds synthesized were investigated. The results showed that most of the compounds 4 exhibited good fungicidal activities. For example, 4l exhibited 89% inhibition of Pellicularia sasakii in 50 mg/L.