“In‐loop” <sup>18</sup>F‐fluorination: A proof‐of‐concept study
Why this work is in the frame
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Bibliographic record
Abstract
There is a great demand to develop more cost‐efficient and robust manufacturing processes for fluorine‐18 ( 18 F) labelled compounds and radiopharmaceuticals. Herein, we present to our knowledge the first radiofluorination “in‐loop,” where [ 18 F]triflyl fluoride was used as the labelling agent. Initial development of the “in‐loop” [ 18 F]fluorination method was optimized by reacting [ 18 F]triflyl fluoride with 1,4‐dinitrobenzene to form [ 18 F]1‐fluoro‐4‐nitrobenzene. This methodology was then applied for the syntheses of two well‐known radiopharmaceuticals, namely, [ 18 F]T807 for imaging of tau protein and [ 18 F]FEPPA for imaging the translocator protein 18 KDa. Both radiotracers were synthesized and formulated using an automated radiosynthesis module with nondecay corrected radiochemical yields of 27% and 29% (relative [ 18 F]F − ), respectively. The overall syntheses times for [ 18 F]T807 and [ 18 F]FEPPA were 65 and 55 minutes, respectively. In these cases, our “in‐loop” radiofluorination methodology enabled us to obtain equal or superior yields compared with conventional reactions in a vial. The radiochemical purities were more than 99%, and the molar activities were more than 350 GBq/μmol at the end‐of‐synthesis for both radiotracers. This novel method is simple, efficient, and allows for a reliable production of radiofluorinated compounds and radiopharmaceuticals.
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Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.002 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.001 | 0.000 |
| Research integrity | 0.000 | 0.002 |
| Insufficient payload (model declined to judge) | 0.003 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it