3-杂环基硫取代-1,3,4,5-四氢-2-氧代-苯并氮杂衍生物的合成

以芳酰肼为原料, 合成了一系列3-巯基-5-芳基-1,2,4-三唑、2-巯基-5-芳基-1,3,4-噁二唑和2-巯基-5-芳 基-1,3,4-噻二唑, 并通过硫原子对3-溴-2-氧代-苯并氮杂3-位上的亲核取代反应将杂环化合物引入了苯并氮杂的结构当中, 合成了32个新的苯并氮杂杂环衍生物. 为提高其在有机溶剂中的溶解性, 在苯并氮杂的N原子上引入乙酸乙酯和乙酸叔丁酯基取代基, 合成了36个新衍生物. 所有化合物经质谱、核磁共振谱及元素分析确证了结构并初步测定了抗菌活性.

Synthesis of 3-Thioheterocycloyl-1,3,4,5-tetrahdro- 2-oxo-1H-benazepine

3-Thiol-1,2,4-triazole, 2-thiol-1,3,4-oxadiazole and 2-thiol-1,3,4-thiadiazole compounds were synthesized from hydrazides through different ways. By the nucleophilic substitution of S for Br on 3-bromo- 1,3,4,5-tetrahydro-2-oxo- 1H-benazepine, 32 derivatives of tetrahydro-2-oxo- 1H-benazepine were synthesized. In order to improve dissolving ability in organic solvents, other 36 derivatives, which have a substituent of acetate on the 1-N position of benazepine, were also prepared. The structures of these compounds were confirmed by MS, 1H and ^13C NMR spectra and elemental analysis. The primary antibacterial activity test indicated that some of the compounds were effective against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Streptococcus and Candida albicans.