A catalyst-free four-component domino reaction for the synthesis of functionalized 3-acyl-1,5-benzodiazepines
作者:Yue-Wei Sun、Yue-Ming Bei、Lan-Zhi Wang
DOI:10.1039/c8ob02903b
日期:——
groups at the 2-position were synthesized via an efficient, sustainable and catalyst-free domino reaction. During the synthesis process, one new cycle and four new bonds (one C–C, two C–N and one CC) were constructed by the nucleophilic substitution, nucleophilic addition, dehydration and cyclization reaction by the H+ shift. Furthermore, a total of 26 examples were examined by reacting inexpensive
通过有效,可持续和无催化剂的多米诺反应,合成了各种在2位含有羧基,酯基和酰基的3-酰基-1,5-苯并二氮杂官能团。在合成过程中,通过亲核取代,亲核加成,脱水和环化反应,通过H +移位,构建了一个新的循环和四个新的键(一个C–C,两个C–N和一个C C)。此外,通过使廉价的N,N原料反应,共检查了26个实例-二甲基甲酰胺二甲基乙缩醛,芳族酮,1,2-苯二胺化合物和醛衍生物。因此,它显示出了广泛的底物范围,良好的官能团耐受性,高收率(77-97%),并且在不涉及有毒溶剂和柱色谱的情况下易于获得目标化合物,这为广泛的合成方法提供了一种新方法各种与生物有关的1,5-苯并二氮杂s。