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Table 2 Comparison of the main steps in the preparation of [18F]LBT999 on TRACERlab FXFN and AIO modules and synthetic results compared to the initial work by Dollé’s group (Dolle et al., 2007)

From: Fully automated radiosynthesis of [18F]LBT999 on TRACERlab FXFN and AllinOne modules, a PET radiopharmaceutical for imaging the dopamine transporter in human brain

Synthetic results of production of [18F]LBT999 Dollé’s work (n > 20) FXFN (n > 16) AIO (n = 5)
1. Azeotropic drying
K2.2.2. 12–15 mg 7.2 mg in 715 μL ACN 7.2 mg in 715 μL ACN
K2CO3 1 mL of a 1.0/mL solution 3.8 mg in 285 μL H2O 3.8 mg in 285 μL H2O
Evaporation/Temperature 145–150 °C 10 min 70–100 °C 10 min 95 °C 10 min
2. Radiofluorination
 Precursor 3.5–4.5 mg 3 mg 5.5–6 mg
 DMSO 0.6 mL 1 mL 0.8 mL
 Reaction time 10 min 10 min 7 min 30
 Temperature 165 °C 165 °C 155 °C
3. HPLC Purification
 Eluent H2O/CH3CN/TFA: 72/28/0.1 AcNH4 (0.1 M)/ CH3CN: 40/60 AcNH4 (0.1 M)/ CH3CN: 40/60 + Na-Asc (0.5%).
 Flow rate 5 mL/min 4 mL/min 4 mL/min
Column Symmetry®C18, Waters (300 × 7.8 mm, 7 μm) Alltima® C18, Grace (250 X 10 mm, 5 μm) Agilent Zorbax Eclipse XDB-C18 (250 X 9.4 mm, 5 μm)
4. Formulation
 ETOH 2.0 mL 1.5 mL 2.5 mL
 NaCl (0.9%) 8.0 mL (volume adjusted bring EtOH concentration below 10%) 13.5 mL 22.5 mL + Na-Asc (0.5%).
Synthetic results
 Starting activity (GBq) 37 77.2 ± 2.1 102.7 ± 19
 Radioactivity at EOS (GBq) 3.7–5.92 16.8 ± 1.9 23.8 ± 7.1
 Radiochemical yield at EOS (%) 17.3–27.7 35.3 ± 5.1 32.7 ± 5.9
 Activity yield at EOS (GBq) 10–16 23.3 ± 4.3 23.1 ± 4.5
 Radiochemical purity (EOS) >  95 99.4 ± 0.2 98.3 ± 0.5
 Total synthesis time (min) 85–90 65.8 ± 3.8 48 ± 1.9
 Molar activity at EOS(GBq/μmol) 37–111 158.6 ± 79.8 154.3 ± 51.1