Table 2.
Summary of 18F labeling reaction of isatin analog 2
| Reaction Entry |
Substrate (mg) |
K2CO3/K222 (mg) |
Solvent | Reaction Conditionb |
% Incorporation Yield (product)d |
|---|---|---|---|---|---|
| 1 | 7a (1.1)a | 1.4/5.5 | DMSO | 30+25 sec (MW) |
90 (17) |
| 2 | 7a (1.2)a wet | 1.6/5.5 | DMSO | 30+25 sec (MW) |
19 (17) |
| 3 | 7a (1.0) | 0.8/4 | DMSO | 30 (MW) 30c (MW) |
0 (17) 86 (17) |
| 4 | 7a (1.1) | 1.8/8.6 | DMSO | 30+30 Sec (MW) |
89 (17) |
| 5 | 12 (1.2) | 1.4/5.0 | DMSO | 30+25 sec (MW) |
80 (14) |
| 6 | 7b (1.0) | 2.1/12 | DMSO | 30 (MW) | 65 (17) |
a
Bu4NOH pre-treatment method: with 2 equivalents of Bu4NOH;
b
MW: Microwave (60W) with an interval of 1 min between each irradiation;
c
The reaction mixture was treated further with K2CO3 (3mg) and K222 (15mg) in DMSO;
d
Incorporation yields were determined by radioTLC (silica gel, 20% MeOH, 80% CH2Cl2).