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. 2014 Dec 5;16(24):6334–6337. doi: 10.1021/ol503078h

Table 4. Optimization of Cyclization to indole 3a.

graphic file with name ol-2014-03078h_0010.jpg

entry Lewis acid X solvent temp (°C) yield (%)
1 none   CH2Cl2 45 0
2 AlCl3 0.2 CH2Cl2 45 0
3 Sc(OTf)3 0.2 CH2Cl2 45 0
4 TiCl4 0.2 CH2Cl2 45 0
5 BF3·OEt2 0.2 CH2Cl2 45 19
6 BF3·OEt2 1.1 THF 70 0
7 BF3·OEt2 1.1 PhCH3 85 61
8 BF3·OEt2 2.5 DCE 90 91