Nitrile assisted, Brønsted acid catalyzed regio and stereoselective diarylphosphonylation of allyl silyl ethers
作者:Chun-Yu Ho、Chun-Wa Chan、Siu-Kwan Wo、Zhong Zuo、Lai-Ying Chan
DOI:10.1039/c001660h
日期:——
for the regio- and stereoselective synthesis of trisubstituted allyl diarylphosphonates from the corresponding disubstituted allyl silyl ethers, circumventing the challenges related to the preparation and availability of stereodefined trisubstituted olefins. A closely related arylation reaction was also discovered during the methodology development. By simply switching the reaction medium, high phos
我们已经发现了从相应的二取代的烯丙基甲硅烷基醚的区域和立体选择性合成三取代的烯丙基二芳基膦酸酯的温和的催化方案,规避了与立体定义的三取代的烯烃的制备和可用性有关的挑战。在方法开发过程中还发现了一个密切相关的芳基化反应。通过简单地切换反应介质,可以实现高的膦酰化/芳基化比,反之亦然。这可能不是改变溶剂极性的直接结果。评价烯丙基二芳基膦酸酯作为羧酸酯酶抑制剂,筛选结果表明,抑制效率与烯烃和芳基取代基的选择高度相关。