Table 3.
Optimization of reaction conditions.
| entry | product | reagent | additive | base | time | yielda |
| 1 | 15a | DCC | HOBt | Et3N | 24 h | 63% |
| 2 | 15a | EDCI | HOBt | Et3N | 18 h | 86% |
| 3 | 15a | EDCI | OxymaPure | DIPEA | 18 h | 88% |
| 4 | 15a | COMU | – | DIPEA | 2 h | 92% |
| 5 | 15b | COMU | – | DIPEA | 3 h | 91% |
| 6 | 15c | COMU | – | DIPEA | 3 h | 94% |
| 7 | 15d | COMU | – | DIPEA | 3 h | 92% |
| 8 | 15e | COMU | – | DIPEA | 3 h | 92% |
aYield of dipeptide analogues 15 after isolation.