Table 1.
Radiobromination of iodonium salts after elution from a QMA column
Entry | R1/R2 | X | Elution1 (%) | 130 °C Yield (%)2
|
|
---|---|---|---|---|---|
10 min | 30 min | ||||
1 | Me/Me (4) | OTs | 55 | 27 | 50 |
2 | H/H (1) | OTf | 94 | 53 | 91 |
3 | H/H (1) | OTf | 1001 | / | 92 |
4 | H/Me (3) | OTs | 73 | 24/12 | 43/24 |
5 | H/H (2) | Cl | 92 | 41 | 73 |
6 | H/OMe (5) | OTs | 55 | 19/0 | 47/0 |
7 | COOH/H (6) | OTf | 0 | / | / |
Notes:
Eluted with iodonium salts in methanol, except that entry 3 was eluted in DMSO;
Radiochemical yield of desired product was determined by HPLC analysis.