Table 3.
Optimization of reaction for the semi-synthesis of asperpyrroindotide A (8)a
Entry | Solvent | Equiv b | Yieldc/% |
---|---|---|---|
1 | Dichloromethane | 2 | 4.9 |
2 | Ethanol | 2 | 0 |
3 | Acetone | 2 | 0 |
4 | 1,4-Dioxane | 2 | 0 |
5 | Dichloromethane | 4 | 15.6 |
6 | Dichloromethane | 6 | 19.6 |
7 | Dichloromethane | 8 | 19.6 |
a8 Equiv trifluoroacetic acid (TFA) catalyst was used in all cases, and the reaction time was 1 h
bThe equiv of meta-chloroperoxybenzoic acid (m-CPBA)
cThe yield of asperpyrroindotide A (8)