Table 2. One-Pot Borylation/Cross-Coupling Process.
| ||||
---|---|---|---|---|
entry | HetAr-X | Ar-X | yield (%) | rxn temp (°C) |
1 | 95 | 80 | ||
2 | 84 | 80 | ||
3 | 88 a | 80 | ||
4 | 78; 82 a | 65 | ||
5 | 39 | 65 | ||
6 | 86 | 65 | ||
7 | 79 | 65 | ||
8 | 59 | 65 | ||
9 | 63 | 80 | ||
10 | 53 | 80 | ||
11 | 31 | 65 | ||
12 | 61 | 65 | ||
42 | 80 | |||
13 | 28 | 65 |
7.6 mmol scale, 0.75% Pd-G2-XPhos, 1.5% XPhos, 3 equiv ethylene glycol, 3 equiv KOAc, 1.5 equiv BBA