A base promoted multigram synthesis of aminoisoxazoles: valuable building blocks for drug discovery and peptidomimetics

作者:Chalyk Bohdan A; Kandaurova Inna Y; Hrebeniuk Kateryna V; Manoilenko Olga V; Kulik Irene B; Iminov Rustam T; Kubyshkin Vladimir; Tverdokhlebov Anton V; Ablialimov Osman K; Mykhailiuk Pavel K
来源:RSC Advances, 2016, 6(31): 25713-25723.
DOI:10.1039/c6ra02365g

摘要

A practical multigram metal free synthesis of isoxazole-containing building blocks from commercially available amino acids was elaborated. The key reaction was a regioselective [3 + 2]-cycloaddition of in situ generated nitrile oxides with alkynes/enamines. The obtained building blocks were used in the preparation of bioactive compounds and peptidomimetics.

  • 出版日期2016