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Regiocontrolled Direct C-?HArylation of Indoles at the C4 and C5Positions
Release time:2017-03-08    clicks:1944

The group publishes a Regiocontrolled Direct C-HArylation of Indoles at the C4 and C5Positions on Angew. Congrats Yang and Gao!

Abstract: An effective and practical strategy has been estab-lished for the direct and site-selective arylation of indoles at theC4 and C5 positions with the aid of areadily accessible,cheap,and removable pivaloyl directing group at the C3 position. Thistransformation shows good functional-group tolerance andcould serve as apowerful synthetic tool for the synthesis ofmedicinally relevant compounds.This method and thosedeveloped in previous researchtogether enable the regiocon-trolled direct arylation of indole at eachC@Hbond withoutprefunctionalization of the reactive sites.