作者:Elena Y. Zelina、Tatyana A. Nevolina、Ludmila N. Sorotskaja、Dmitry A. Skvortsov、Igor V. Trushkov、Maxim G. Uchuskin
DOI:10.1021/acs.joc.8b01669
日期:2018.10.5
A simple one-pot method for the synthesis of isomeric pyrrolo[1,2-x][1,4]diazepinones in reasonable yields was developed. The method is based on the condensation of readily available N-Boc amino acids with biomass-derived furans containing aminoalkyl groups followed by deprotection, furan ring opening, and Paal–Knorr cyclization. Using this approach, we synthesized pyrrolo[1,2-a][1,4]diazepin-3(2H)-ones
开发了一种简单的一锅法,以合理的产率合成吡咯并[1,2- x ] [1,4]二氮杂ze酮。该方法基于容易获得的N- Boc氨基酸与生物质衍生的含氨基烷基的呋喃的缩合,然后进行脱保护,呋喃开环和Paal-Knorr环化。使用这种方法,我们从糠胺和β-氨基酸和吡咯并[1,2- d ] [1,4]二氮杂合成了吡咯并[1,2- a ] [1,4]二氮杂-3(2 H)-来自2-(2-呋喃基)乙胺和α-氨基酸的-4(5 H)-1。研究了合成的吡咯并二氮杂酮的细胞毒性。