嘌呤6位含氟基团取代衍生物的合成

以6-氯嘌呤衍生物和6-溴嘌呤衍生物为原料, 通过卤素交换反应制得6-氟嘌呤衍生物; 通过烷氧基化反应制得6-三氟乙氧基嘌呤衍生物, 通过三氟甲基化反应制得6-三氟甲基嘌呤衍生物, 所有化合物的结构均经过1H NMR, MS和元素分析表征. 分析了所得化合物对稻草芽孢杆菌、黑曲酶和热带假丝酵姆的抑菌活性, 结果表明: 化合物2b, 4b对稻草芽孢杆菌(Bacillus subtillis)有比较好的杀菌效果, 化合物4a, 4b对黑曲酶(Aspergillus niger)有比较好的杀菌效果, 化合物3b, 4b对热带假丝酵姆(Cardida tropicals)有比较好的杀菌效果.

Synthesis of 6-Fluorine-substituted-purine Derivatives

Using 6-chloropurine as a starting material, 6-fluoropurine derivatives were prepared through the reaction of halogen exchange. 6-Trifluoethoxylpurine derivatives were prepared through substitution by β,β,β-trifluoroethoxyl sodium, while 6-trifluomethylpurine derivatives were prepared by the trifluomethyl action with CF3COONa/CuI/DMF at 160 ℃. All of the products were characterized by 1H NMR, mass spectra and elemental analysis. Fungicidal activities of all compounds were tested, showing that compounds 2b and 4b have good activity to Bacillus subtillis, compounds 4a and 4b have good activity to Aspergillus niger, and compounds 3b and 4b have good activity to Cardida tropicals.