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. 2021 Sep 15;23(19):7434–7438. doi: 10.1021/acs.orglett.1c02645

Table 1. Effect of the Ligand in the Copper-Catalyzed Borylation.

graphic file with name ol1c02645_0007.jpg

entrya L 2a:3ab yield (%)c
1 L1 65:35 71
2 L2 50:50 84
3 L3 ≥98:2 86
4 L4 83:17 58
5 L5 64:36 79
6 L6 73:27 69
7d L3 ≥98:2 69
8 60:40 13
a

Reaction conditions: 1a (0.1 mmol), B2pin2 (0.11 mmol), KOt-Bu (0.5 equiv), CuCl (10 mol %), L (11 mol %), MeOH (0.2 mmol), THF (0.2 M).

b

Determined by 1H NMR.

c

Isolated yields.

d

With 5 mol % of CuCl and 6 mol % of L3.