2,3-Disubstituted indoles are widely present in natural products and bioactive compounds with medicinal importance, so developing an efficient synthesis of unsymmetrical 2,3-diaryl-substituted indoles remains desirable. Here, the authors report a three-component reaction of an arylamine, an arylglyoxal, and a boronic acid, achieving the selective synthesis of 2,3-diaryl substituted indoles and 2,2-diaryl substituted indolin-3-ones, by redirecting the α-iminol rearrangements via Petasis reactions.
- Hui-Min Zhu
- Tong Lei
- An-Xin Wu