EaStCHEM, School of Chemistry, University of St Andrews , North Haugh, St. Andrews, Fife, KY16 9ST, United Kingdom.
Org Lett. 2014 Feb 7;16(3):964-7. doi: 10.1021/ol403697h. Epub 2014 Jan 16.
A one-pot isothiourea-mediated Michael addition/lactonization/thiol elimination cascade sequence for the formation of 4,6-disubstituted and 3,4,6-trisubstituted 2-pyrones from (phenylthio)acetic acids and α,β-unsaturated trifluoromethyl ketones is described. The synthesis of a COX-2 inhibitor and the wide-ranging derivatization of the 2-pyrone moiety to trifluoromethyl substituted aromatics and heteroaromatics is also disclosed.
一锅法硫代乙内酰脲介导的迈克尔加成/内酯化/硫醚消除级联反应，用于从（苯硫基）乙酸和α,β-不饱和三氟甲基酮合成 4,6-二取代和 3,4,6-三取代的 2-吡喃酮。还公开了 COX-2 抑制剂的合成以及 2-吡喃酮部分的广泛衍生化，以得到三氟甲基取代的芳烃和杂芳烃。
