Table 2. Conjugation Conditions (Exploratory Runs) and Conversion Rates.
| porphyrin–peptide combinations | activation method/time (min) | conversiona (%) |
|---|---|---|
| PP-P1 | PyBOP-DIPEA/30 | 96.8 |
| HATU-DIPEA/60 | 100 | |
| TBTU-DIPEA/30 | 97.6 | |
| DIC-Oxyma/180 + 60 | 98.7 | |
| MP-P3 | PyBOP-DIPEA/30 | 78.9 |
| HATU-DIPEA/60 | 59.9 | |
| TBTU-DIPEA/30 | 98.6 | |
| DIC-Oxyma-DIPEA/180 + 60 | 99.5 | |
| PP-P3 | TBTU-DIPEA/30 | 90.1 |
| DIC-Oxyma/180 + 60 | 98.5 | |
| MP-P1 | TBTU-DIPEA/30 | 67.3 |
| DIC-Oxyma-DIPEA/180 + 60 | 97.1 | |
| P2-MP | DIC-Oxyma-DIPEA/180 + 60 | 99.6 |
| P2-PP | DIC-Oxyma/180 + 60 | 99.4 |
a
Conversions >95% are in boldface.