Solution versus fluorous versus solid-phase synthesis of 2,5-disubstituted 1,3-azoles. Preliminary antibacterial activity studies.
作者： Juan F. Sanz-Cervera , Raül Blasco , Julio Piera , Michael Cynamon , Ignacio Ibáñez
DOI: 10.1021/JO9016265
关键词:
摘要: A small library of compounds with an oxa(thia)zole scaffold and structural diversity in both positions 2 5 has been synthesized. Double acylation a protected glycine affords intermediate alpha-amido-beta-ketoesters, which turn can be dehydrated to afford 1,3-oxazoles or reacted Lawesson's reagent furnish 1,3-thiazoles. This procedure was designed its adaptation fluorous techniques mind. Thus, when tag the ester moiety is used as starting material, synthesis easily completed without column chromatography purification good excellent yields, thus affording suitable entry preparation libraries these bioactive compounds. The prepared oxa(thia)zoles were assayed for their antibacterial activity, several them active against Staphylococcus aureus.
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