1,5-苯并二氮杂的合成及其生物活性研究

Synthesis and Bioactivities of 1,5-Benzodiazepine Derivatives

采用两种方法:以三氧化铝为载体邻苯二胺与查尔酮为原料的无溶剂合成法和以PPA(多聚磷酸)为催化剂邻苯二胺与苯乙酮的一锅合成法,合成了1,5-苯并二氮杂,产物收率为53.7%～74.5%.通过1HNMR,13CNMR,MS,IR,元素分析等手段对所合成的化合物进行了结构确定,并测试了它们对菌和乙酰胆碱酶的抑制活性.

1,5-Benzodiazepine derivatives were synthesized by two different methods： the reaction of chalcone with benzene-l,2-diamine in aluminum oxide under solvent-free conditions and one-pot reaction of substituted-acetophenones with benzene-l,2-diamine in the presence of PPA （polyphosphoric acid） as cata- lyst with the yields of 53.7%-73.57%. They were characterized by ^1H NMR, ^13C NMR, MS, IR spectra and elemental analysis and evaluated against bacteria and acetylcholinesterase.