Table 3.
Entry | R (#) | RCY (%)# |
---|---|---|
1 | H (118F) | 21 ± 5 (n=7) |
2 | Ac (218F) | 13 ± 3 (n=5) |
3 | CN (318F) | 20 ± 5 (n=4) |
4 | F (418F) | 16 ± 2 (n=7) |
5 | I (518F) | 14 ± 1 (n=4) |
6 | Br (618F) | 12 ± 3 (n=5) |
7 | Cl (718F) | 11 ± 2 (n=4) |
8 | Me (818F) | 15 ± 2 (n=5) |
9 | Ph (918F) | 14 ± 2 (n=5) |
10 | MeO (1018F) | 0 (n=7) |
General conditions: aliquots of a prestirred stock solution containing Ag[18F]F (92.5–129.5 MBq) and PhI(OAc)2 (2 equiv) in CH2Cl2 (200 μL) were added to vials containing substrate (0.042 mmol) and Pd2(dba)3 (10 mol %) in CH2Cl2 (550 μL). Reactions were heated at 145 oC for 30 min, RCC was determined by radio-TLC.