Table 1. Efficiency and Yield of Labeling Reaction with SAL-Esters 1a–fa.
| entry | SAL-ester | yield |
|---|---|---|
| 1 | 1a | 12 h, 31% |
| 2 | 1b | 12 h, trace amountb |
| 3 | 1c | 12 h, trace amountc |
| 4 | 1d | 3 h, 36% |
| 5 | 1e | 3 h, 63% |
| 6 | 1f | 3 h, 50% |
Conditions: phosphate buffer (0.1 M, pH 7.0), DMSO (2%, v/v), room temperature. The concentration of SAL-ester was 10 mM, and the concentration of Ac-3AT-OMe was 10 mM.
The majority of 1b was consumed by hydrolysis in the buffer.
No desired product was isolated due to the low reaction conversion.
