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Article Abstract
The first iridium-catalyzed direct intermolecular indole C7-allylic alkylation of 4-aminoindoles and racemic branched allylic esters was reported. Various substituted substrates were applicable to give the corresponding C7-allylated products in moderate to high yields (43-80%) with high regio- and enantioselectivities (82-99% ee) under mild reaction conditions. Representative transformations of the vinyl group in the product were carried out to examine the utility of this protocol.
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Iridium-Catalyzed Regio- and Enantioselective C7-Allylic Alkylation of 4-Aminoindoles.
Org Lett
August 2025
School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen, 518107, P. R. China.
The first iridium-catalyzed direct intermolecular indole C7-allylic alkylation of 4-aminoindoles and racemic branched allylic esters was reported. Various substituted substrates were applicable to give the corresponding C7-allylated products in moderate to high yields (43-80%) with high regio- and enantioselectivities (82-99% ee) under mild reaction conditions. Representative transformations of the vinyl group in the product were carried out to examine the utility of this protocol.
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