Center for Drug Design, Academic Health Center, University of Minnesota, Minneapolis, Minnesota 55455, USA.
Org Lett. 2010 May 21;12(10):2286-9. doi: 10.1021/ol100657n.
The direct alkynylation of tautomerizable heterocylcles is described via a two-step process involving in situ C-OH activation with bromotripyrrolidinophosphonium hexafluorophosphate (PyBrOP) followed by Sonogashira coupling with a wide range of alkyl or aryl terminal alkynes using a copper-free system employing PdCl(2)(CH(3)CN)(2) and 2-(dicyclohexylphosphino)biphenyl.
描述了通过两步过程实现的可互变异构杂环的直接炔基化,该过程包括用溴三吡咯烷基鏻六氟磷酸盐(PyBrOP)原位进行 C-OH 活化,然后在无铜体系中使用 PdCl2(CH3CN)2 和 2-(二环己基膦基)联苯进行 Sonogashira 偶联,与各种烷基或芳基末端炔烃反应。