Table 1. Solvent Effects on the Coupling of 2-Deoxy-2-[18F]fluoro-1,3,5-tri-O-benzoyl-d-arabinofuranose (18F-Labeled Sugar) and O,O′-Bis(trimethylsilyl)thymine in the Radiosynthesis of [18F]FMAU (β-anomer).
solvent | polarity | class of residual solventsa | concentration limit (ppm)a | toxicity | % yield of β-anomerb | ratio of anomers (β/α) |
---|---|---|---|---|---|---|
DMSO | polar | 3 | 5000 | low | NDc | ND |
DMF | polar | 2 | 880 | moderate | ND | ND |
THF | polar | 2 | 720 | moderate | 5.37 | 2.86 |
DCE | nonpolar | 1 | 5 | high | 32.68 | 1.24 |
1,4-dioxane | nonpolar | 2 | 380 | moderate | 48.07 | 1.06 |
Data are cited from the United States Pharmacopeia (USP) General Chapter ⟨467⟩ Residual Solvents, Rev. 20190927.
Radiochemical yields (%) are reported based on analytical HPLC.
ND; not detected.