The Institute for Advanced Studies , Wuhan University , Wuhan , Hubei 430072 , China.
Org Lett. 2019 Jun 7;21(11):3968-3971. doi: 10.1021/acs.orglett.9b01120. Epub 2019 May 10.
A novel nickel-catalyzed 1,2-arylboration of vinylarenes is reported. A variety of 2-boryl-1,1-diarylalkanes, which constitute a class of significant pharmacophores, are efficiently prepared from readily available olefins and aryl halides in the presence of bis(pinacolato)diboron under mild reaction conditions. The success of this three-component cascade is mainly attributed to the redox-active nitrogen-based ligand. Moreover, this method exhibits good functional group tolerance and excellent chemo- and stereoselectivity.
本文报道了一种新型镍催化的乙烯基芳烃 1,2-芳基硼酸化反应。在温和的反应条件下，以双频哪醇硼酸酯为硼源，在氧化还原活性氮配体的作用下，从易得的烯烃和芳基卤化物出发，高效合成了多种 2-硼酸基-1,1-二芳基烷烃，这些化合物是一类重要的药效团。此外，该方法还具有良好的官能团耐受性和优秀的化学选择性和立体选择性。
