el-Zohry M F, Abd-Alla M A
Department of Chemistry, Faculty of Science, Assiut University, Egypt.
J Chem Technol Biotechnol. 1992;55(3):209-15. doi: 10.1002/jctb.280550303.
3-(2'-Chloroethyl)-2-methyl-3,4-dihydroquinazolin-4-one was reacted with acetylacetone, ethyl acetoacetate and diethylmalonate in the presence of sodium ethoxide to afford the alkylation products IV, V and VI. Compounds IV, V and VI were reacted with hydrazine hydrate, phenylhydrazine, hydroxylamine hydrochloride, urea and thiourea to yield 3-(2'-heterocyclicethyl)-2-methyl-3,4-dihydroquinazolin-4-on e derivatives VII-XV. The structures of the synthesized compounds were elucidated by elemental analyses and spectroscopic (IR and 1H-NMR) analyses. The prepared compounds were tested for their antimicrobial activities in comparison with tetracycline as a reference compound.
3-(2'-氯乙基)-2-甲基-3,4-二氢喹唑啉-4-酮在乙醇钠存在下与乙酰丙酮、乙酰乙酸乙酯和丙二酸二乙酯反应,得到烷基化产物IV、V和VI。化合物IV、V和VI与水合肼、苯肼、盐酸羟胺、尿素和硫脲反应,生成3-(2'-杂环乙基)-2-甲基-3,4-二氢喹唑啉-4-酮衍生物VII - XV。通过元素分析和光谱(红外和1H - NMR)分析确定了合成化合物的结构。将制备的化合物与作为参考化合物的四环素相比,测试了它们的抗菌活性。