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A base promoted multigram synthesis of aminoisoxazoles: valuable building blocks for drug discovery and peptidomimetics†
Bohdan A. Chalyk,Inna Y. Kandaurova,Kateryna V. Hrebeniuk,Olga V. Manoilenko,Irene B. Kulik,Rustam T. Iminov,Vladimir Kubyshkin,Anton V. Tverdokhlebov,Osman K. Ablialimov
RSC Advances Pub Date : 03/01/2016 00:00:00 , DOI:10.1039/C6RA02365G
Abstract

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.

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