Department of Chemistry, Korea Advanced Institute of Science and Technology (KAIST), Daejeon, 305-701, Korea.
Org Lett. 2011 Aug 19;13(16):4466-9. doi: 10.1021/ol2018278. Epub 2011 Jul 28.
A new efficient method for the direct alkenylation of chromones via a palladium(II)-catalyzed C-H functionalization reaction was developed. The use of pivalic acid with Cu(OAc)(3)/Ag(2)CO(3) provided superior reactivity in the cross-coupling of chromones with alkene partners. This approach represents a significant advance over the existing two-step method and afforded various 3-vinylchromone derivatives, which are privileged structures in many biologically active compounds and versatile synthetic building blocks.
开发了一种通过钯(II)催化的 C-H 功能化反应将色酮直接烯基化的新有效方法。使用三氟乙酸与 Cu(OAc)(3)/Ag(2)CO(3)的组合在色酮与烯烃偶联中提供了优异的反应性。与现有的两步法相比,这种方法是一个重大进展,并提供了各种 3-乙烯基色酮衍生物,这些衍生物是许多生物活性化合物和多功能合成砌块中的重要结构。