Catalytic asymmetric(3+3)cycloaddition between different 2-indolylmethanols

摘要

The catalytic asymmetric(3+3)cycloaddition between different 2-indolylmethanols has been established,in which a series of chiral indole-fused six-membered heterocycles were constructed in high yields with excellent enantioselectivities.This work not only has established the first catalytic asymmetric cycloaddition between different 2-indolylmethanols but also provided a powerful strategy for constructing enantioenriched indole-fused six-membered rings.Additionally,biological evaluation discovered some products with promising antitumor activities.Notably,theoretical calculations performed on the reaction pathway and activation mode provide an in-depth understanding of this catalytic asymmetric(3+3)cycloaddition among different 2-indolylmethanols,which will advance the understanding of the chemistry of indolylmethanols.