Selective Transformation of Strychnine and 1,2-Disubstituted Benzenes by C–H Borylation
作者:Yutaro Saito、Kotono Yamanoue、Yasutomo Segawa、Kenichiro Itami
DOI:10.1016/j.chempr.2020.02.004
日期:2020.4
as natural products, pharmaceuticals, and π-conjugated systems are at the heart of constructing and modifying organic molecules, whereby the selectivity and predictability are of the utmost importance. Herein, we report the highly C3-selective C–H borylation of strychnine along with olefin isomerization, catalyzed by an iridium complex with a diphosphine ligand. This method enabled us to rapidly produce
复杂分子(例如天然产物,药物和π共轭体系)的C–H功能化是构建和修饰有机分子的核心,因此,选择性和可预测性至关重要。在本文中,我们报道了由铱与二膦配体的配合物催化的士的宁的高度C3选择性C–H硼氢化以及烯烃异构化。这种方法使我们能够通过使用相应的C3硼化和异构化的类似物作为常见的合成中间体,快速生产15种士的宁衍生物。目前的催化剂体系通常对不对称1,2-二取代苯衍生物的C–H官能化也有效,包括稠合的π-体系(黄嘌呤,芴,萘和蒽)和药物(硝苯地平),