This work demonstrates efficient enantioselective synthesis of indolyl derivatives, suggesting a new method for complex chiral molecules.
A chiral bis(oxazoline)-Cu(II) complex-catalyzed asymmetric 1,4-conjugate addition of β-ketoesters to in situ generated 3-indole imine methides (3-IIMs) has been developed. The synergistic Lewis acid/Brønsted acid catalytic system enables the efficient construction of enantioenriched 3-indolyl derivatives featuring congested adjacent quaternary and tertiary stereocenters with excellent efficiency (up to >20:1 dr, 99% ee). This work not only provides a complementary and robust alternative to existing organocatalytic strategies for accessing chiral 3-indolyl scaffolds but also significantly enriches the synthetic chemistry of 3-indolylmethanols by expanding their asymmetric transformation repertoires.
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Zhai et al. (2026) studied this question.
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