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

RSC Adv. 2016, 6 (31), 25713-25723

DOI: 10.1039/C6RA02365G

Chalyk B. A.; Kandaurova I. Y.; Hrebeniuk K. V.; Manoilenko O. V.; Kulik I. B.; Iminov R. T.; Kubyshkin V.; Tverdokhlebov A. V.; Ablialimov O. K.; Mykhailiuk P. K.

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.

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

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