Efficient Aerobic Oxidative Coupling of Methyl Heteroarenes with Indoles

Direct oxidative coupling of inert C(sp(3))-H bond has been a great challenge. Herein, an environmentally friendly aerobic oxidative coupling of alpha-methyl substituted N-heteroarenes with indoles is reported. A variety of diheteroaryl ketones were prepared in good yields (up to 72 %). This protocol features simple operation and broad substrates scope (26 examples). Significantly, a plausible mechanism about catalytic cycle was proposed, and two key intermediates were confirmed by high resolution mass spectrometry.

Automated summary

An environmentally friendly method for the oxidative coupling of alpha-methyl substituted N-heteroarenes with indoles is reported. This method features simple operation and a wide range of substrates.