Table 1.
# | Method | Conditions | Library | Success Rate, %a | Average Yield, % |
|
---|---|---|---|---|---|---|
All Experiments | Successful Experiments | |||||
1 | A | 1. HATU, i-Pr2NEt, DMSO, rt, 16 h 2. CF3COOH, i-Pr3SiH, H2O, rt, 6 h 3. HATU, i-Pr2NEt, DMSO, rt, 16 h |
11 | 77 | 34 | 44 |
2 | B | 1-2. Same as for A 3. i-Pr2NEt, NMP,b 100°C, 16 h |
12 | 60 | 26 | 43 |
3 | C | 1-2. Same as for A 3. i-Pr2NEt, DMF, 80°C, 16 h |
13 | 53 | 16 | 31 |
4 | D | 1. i-Pr2NEt, NMP,b 100°C, 16 h 2-3. Same as for A |
14 | 81 | 30 | 38 |
5 | E | 1. HATU, i-Pr2NEt, DMF, rt, 16 h 2. i-Pr2NEt, Cu(OAc)2, 80°C, 16 h |
15 | 80 | 41 | 51 |
See Also Tables S1 and S2, Figures S1 and S2.
Fraction of 400 experiments that allowed for the preparation of the target product.
NMP, N-methyl-2-pyrrolidone.