Artificial Macrocycles by Ugi Reaction and Passerini Ring Closure

作者:Abdelraheem Eman M M; Kurpiewska Katarzyna; Kalinowska Tluscik Justyna; Domling Alexander*
来源:Journal of Organic Chemistry, 2016, 81(19): 8789-8795.
DOI:10.1021/acs.joc.6b01430

摘要

Artificial macrocycles can be convergently synthesized by a sequence of an Ugi multicomponent reaction (MCR) followed by an intramolecular Passerini MCR used, to close the macrocycle. Significantly, in this work, the first intramolecular macrocyclization through a Passerini reaction is described. We describe 21 macrocycles of a size of 15-20. The resulting macrocyclic depsipeptides are model compounds for natural products and could find applications in drug discovery.

  • 出版日期2016-10-7