Synthesis of an <sup>18</sup>F‐labeled cyclin‐dependent kinase‐2 inhibitor
Bibliographic record
Abstract
The radiosynthesis of N ‐(5‐(((5‐( tert ‐butyl)oxazol‐2‐yl)methyl)thio)thiazol‐2‐yl)‐4‐[ 18 F]fluoro‐benzamide [ 18 F]2 as a potential radiotracer for molecular imaging of cyclin‐dependent kinase‐2 (CDK‐2) expression in vivo by positron emission tomography is described. Two different synthesis routes were envisaged. The first approach followed direct radiofluorination of respective nitro‐ and trimethylammonium substituted benzamides as labeling precursors with no‐carrier‐added (n.c.a.) [ 18 F]fluoride. A second synthesis route was based on the acylation reaction of 2‐aminothiazole derivative with labeling agent [ 18 F]SFB. Direct radiofluorination afforded 18 F‐labeled CDK‐2 inhibitor in very low yields of 1%–3%, whereas acylation reaction with [ 18 F]SFB gave 18 F‐labeled CDK‐2 inhibitor [ 18 F]2 in high yields of up to 85% based upon [ 18 F]SFB during the optimization experiments. Large scale preparation afforded radiotracer [ 18 F]2 in isolated radiochemical yields of 37%–44% ( n = 3, decay‐corrected) after HPLC purification within 75 min based upon [ 18 F]SFB. This corresponds to a decay‐corrected radiochemical yield of 13%–16% based upon [ 18 F]fluoride. The radiochemical purity exceeded 95% and the specific activity was determined to be 20 GBq/µmol. Copyright © 2011 John Wiley & Sons, Ltd.
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How this classification was reachedexpand
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 | 0.001 | 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 | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.001 |
| Insufficient payload (model declined to judge) | 0.000 | 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 itClassification
machine, unvalidatedMachine predicted; a candidate call from one teacher head, not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".