Narumi Tetsuo, Tomita Kenji, Inokuchi Eriko, Kobayashi Kazuya, Oishi Shinya, Ohno Hiroaki, Fujii Nobutaka
Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto 606-8501, Japan.
Org Lett. 2007 Aug 16;9(17):3465-8. doi: 10.1021/ol701627v. Epub 2007 Jul 27.
Chemo- and stereoselective synthesis of fluoroalkenes was achieved in excellent yields via Pd-catalyzed C-F bond activation. In this transformation, Et3N plays a crucial role to produce reactive hydride species such as Ph(EtO)SiH2 and Ph(EtO)2SiH by promoting dehydrogenative coupling. The reaction proceeds efficiently at 50 degrees C with a variety of substrates and is also useful for the synthesis of fluoroalkene peptidomimetics.
通过钯催化的C-F键活化，以优异的产率实现了氟代烯烃的化学选择性和立体选择性合成。在该转化过程中，三乙胺通过促进脱氢偶联作用，在生成诸如Ph(EtO)SiH2和Ph(EtO)2SiH等活性氢化物种方面发挥着关键作用。该反应在50℃下能与多种底物高效进行，并且对氟代烯烃拟肽的合成也很有用。
