The Center for Combinatorial Chemistry and Drug Discovery of Jilin University, The School of Pharmaceutical Sciences, Jilin University, 1266 Fujin Road, Changchun, Jilin 130021, P. R. China.
J Org Chem. 2021 May 7;86(9):6458-6466. doi: 10.1021/acs.joc.1c00303. Epub 2021 Apr 28.
A one-pot synthetic method for indole/pyrrole-fused 1,4-diazepanone scaffolds has been developed. This method involves a sequential amide coupling/intramolecular aza-Michael addition of 1-indole/pyrrole-2-carboxylic acids with Morita-Baylis-Hillman-derived allylamines. The readily available starting materials, good stereoselectivity, and gram-scale synthesis make this method valuable for the construction of highly substituted fused heterocycles containing the 1,4-diazepanone moiety.
已开发出一种用于吲哚/吡咯并合的 1,4-二氮杂环酮骨架的一锅合成方法。该方法涉及 1-吲哚/吡咯-2-羧酸与 Morita-Baylis-Hillman 衍生的烯丙胺的顺序酰胺偶联/分子内氮杂迈克尔加成。易得的起始原料、良好的立体选择性和克级规模合成使得该方法对于构建含有 1,4-二氮杂环酮部分的高度取代的稠合杂环非常有价值。
