Abstract
AbstractA three‐component cyclization of 2‐methylquinolines, trimethylsilyl cyanide, and alkylamines or α‐amino acids mediated by CuSO4 was developed. By employing oxygen as the clean oxidant, cyanated imidazo[1,5‐a]quinolines were constructed with high efficiency for the first time. The loading of CuSO4 could be lowered to 20 mol% with a slightly diminished yield. The synthetic utility of this method is further highlighted by the gram‐scale synthesis and tolerance of sensitive functional group.magnified image
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