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采用两种方法以靛红酸酐为起始原料,分别与谷氨酸(L-Glu)和亚氨基二乙酸(Ida)反应制备两种含有游离羧基的1,4-苯并二氮杂-2,5-二酮类中间体2a和2b;同时,由2a或2b与氨基组分3c～3f,3h,3j进行缩合制备了含有1,4-苯并二氮杂-2,5-二酮环的肽模拟物4c～4f,4h,4j,5c～5f,5h,5j.另外,讨论了溶剂对微波辅助法合成1,4-苯并二氮杂-2,5-二酮酸的影响.所合成新化合物均经MS,1HNMR证明其结构.
Two methods were used to prepare two kinds of 1,4-benzodiazepine-free 1,4-benzodiazepine containing free carboxyl group by using isatoic anhydride as the starting material, respectively reacting with glutamic acid (L-Glu) and iminodiacetic acid (Ida) 2,5-diketo intermediates 2a and 2b; in the meantime, condensation reaction of 2a or 2b with amino components 3c to 3f, 3h, 3j to prepare 1,4-benzodiazepin-2,5- Diketone ring peptidomimetics 4c-4f, 4h, 4j, 5c-5f, 5h, 5j.In addition, the solvent-assisted microwave assisted synthesis of 1,4-benzodiazepine-2,5-dione Acid effect.The new compounds synthesized by MS, 1HNMR proved its structure.