Table 2. Optimization of the Conditions for Hydroxamination of 2a.
| entry | reagent | base | solvent | time (h) | yield |
|---|---|---|---|---|---|
| 1. | NH2OH·HCl | MeOH | 48 | ||
| 2. | NH2OH·HCl | EtOH | 48 | ||
| 3. | NH2OH·HCl | i-PrOH | 48 | ||
| 4. | NH2OH·HCl | DMF | 48 | trace | |
| 5. | NH2OH·HCl | DMSO | 48 | ||
| 6. | NH2OH·HCl | NaHCO3 | MeOH | 36 | 67% |
| 7. | NH2OH·HCl | Na2CO3 | MeOH | 30 | 51% |
| 8. | NH2OH·HCl | K2CO3 | MeOH | 34 | 56% |
| 9. | NH2OH·HCl | NaOAc | MeOH | 48 | |
| 10. | (NH2OH)2·H2SO4 | MeOH | 48 | ||
| 11. | NH2OH | MeOH | 01 | 80% |
Isolated yields are reported; MeOH = methanol, EtOH = ethanol, i-PrOH = isopropanol, DMF = N,N-dimethylformamide, and DMSO = dimethyl sulfoxide.
