Tianjin Key Laboratory for Modern Drug Delivery and High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.
J Org Chem. 2011 Dec 16;76(24):10338-44. doi: 10.1021/jo202070h. Epub 2011 Nov 18.
Treatment of β-monosubstituted enamines with phenyliodine bis(trifluoroacetate) (PIFA) was found to give a variety of 4,5-disubstituted 2-(trifluoromethyl)oxazoles. This approach allows the incorporation of the trifluoromethyl moiety in PIFA into the final products, which presumably takes place via the oxidative β-trifluoroacetoxylation of the enamine substrates followed by subsequent intramolecular cyclization.
用苯碘二(三氟乙酸)(PIFA)处理β-单取代烯胺时,发现可以得到多种 4,5-二取代的 2-(三氟甲基)恶唑。这种方法可以将 PIFA 中的三氟甲基部分引入最终产物中,这可能是通过烯胺底物的氧化β-三氟乙氧羰基化作用,然后进行后续的分子内环化反应来实现的。