State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032 (China).
Liaoning Shihua University, Dandong Lu West 1, Fushun 113001 (China).
Angew Chem Int Ed Engl. 2016 Jan 4;55(1):321-5. doi: 10.1002/anie.201508117. Epub 2015 Oct 29.
An efficient rhodium-catalyzed method for direct C-H functionalization at the C7 position of a wide range of indoles has been developed. Good to excellent yields of alkenylation products were observed with acrylates, styrenes, and vinyl phenyl sulfones, whereas the saturated alkylation products were obtained in good yield with α,β-unsaturated ketones. Both the N-pivaloyl directing group and the rhodium catalyst proved to be crucial for high regioselectivity and conversion.
现已开发出一种高效的铑催化方法，可在各种吲哚的 C7 位置进行直接 C-H 功能化。与丙烯酸酯、苯乙烯和乙烯基苯砜反应时，观察到烯基化产物具有良好至优异的产率，而与α，β-不饱和酮反应时，则可获得良好产率的饱和烷基化产物。N-特戊酰基导向基团和铑催化剂对于高区域选择性和转化率都是至关重要的。
