Direct C3-arylations of 2-indolylmethanols with tryptamines and tryptophols via an umpolung strategy.

摘要: A Bronsted acid-catalyzed direct C3-arylation of 2-indolylmethanols with tryptamines and tryptophols has been established, leading to a series potentially bioactive 2,3′-biindole derivatives broad substrate scope generally good yields (38 examples, up 96% yield). In this process, the reactivity C3-position 2-indolylmethanol is switched from nucleophilic electrophilic, which can serve as an umpolung strategy in indole chemistry. This protocol not only provides new for accessing structurally diversified 2,3′-biindolyl frameworks, but also satisfies requirement green