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The expansion of catalytic methods is a focus of contemporary interest due to the adverse effects of the manufacturing process of fine chemicals, pharmaceuticals, and materials on the environment. In...

The first ‘in-water’ nickel-catalyzed chemoselective C3-allylation of (NH)-indoles employing allylic alcohols under mild conditions is reported here. Different indoles and allylic alcohols were found compatible with excellent chemo- (C vs...

The Structure Ligation Relationship (SLR) of free amino acids (AAs) under Pd‐catalysis were examined for the chemo‐ and regio‐selective indole C−H arylation reactions. While the majority of AAs were minor or ineffective, the L‐aspartic acid (L‐Asp) stands out promising to deliver high‐value C3‐arylated indoles with excellent chemo‐ (C vs N) and regioselectivity (C3 vs C2) with high functional group tolerance. Thus, the protocol offers a cost‐effective and sustainable alternative of phosphine‐based ligands for the indole C3−H arylation reactions. Preliminary mechanistic investigations suggested the simultaneous involvement of −NH2, α‐CO2H, and β‐CO2H functionalities of L‐Asp and found critical for its ligation efficiency. The developed catalytic system was compatible with the tandem decarboxylation/arylation procedure for the chemoselective synthesis of 3‐aryl indoles.magnified image

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