论文部分内容阅读
1,5-苯并二氮-2-酮作为一个独特的骨架广泛存在于很多具有生理活性的化合物中,而全氟烷基的引入影响到有机化合物的理化性质以及生理活性的改变.因此将全氟代烷基引入1,5-苯并二氮-2-酮的方法的研究正变得日趋重要.发展了一个制备全氟代烷基取代的1,5-苯并二氮-2-酮的简易方法.采用全氟代炔酸甲酯为含氟砌块,与邻芳基二胺,以无水甲苯为溶剂,在无催化剂存在条件下,80℃反应24 h,以较好的收率顺利得到4-全氟烷基-1,3-二氢-1,5-苯并二氮-2-酮类化合物.
1,5-benzodiazepine-2-one is widely existed in many physiologically active compounds as a unique skeleton, and the introduction of perfluoroalkyl groups affects the physicochemical properties and the changes of physiological activities of organic compounds. It is becoming more and more important to study the method of introducing perfluoroalkyl groups into 1,5-benzodiazepine-2-ones.A process for the preparation of perfluoroalkyl-substituted 1,5-benzodiazepine 2-one. Using perfluoroalkynoic acid methyl ester as a fluorine-containing block, with o-aryl diamine, anhydrous toluene as a solvent, in the absence of a catalyst, at 80 ° C for 24 h, reacting The better yield gives 4-perfluoroalkyl-1,3-dihydro-1,5-benzodiazepine-2-ones.