Application of 7‐Indolylmethanols in Catalytic Asymmetric Arylations with Tryptamines: Enantioselective Synthesis of 7‐indolylmethanes

Abstract The application of 7‐indolylmethanols in catalytic asymmetric reactions has been established via an enantioselective arylation reaction with tryptamines in the presence of chiral phosphoric acid, which afforded a series of structurally diversified chiral 7‐indolylmethanes in moderate to good yields and generally excellent enantioselectivities (23 examples, up to 92% ee). This reaction not only provides a useful strategy for the enantioselective synthesis of chiral 7‐indolylmethanes, but also represents a good example of 7‐indolylmethanol‐involved catalytic asymmetric reaction, which will greatly enrich the chemistry of indolylmethanols. magnified image