Towards a one-pot synthesis of <sup>11</sup> C-amides via copper(I) catalyzed [ <sup>11</sup> C]CO <sub>2</sub> fixation
Bibliographic record
Abstract
Synthesis of 11 C-amides has been hindered by the lack of versatile synthetic methods capable of directly and easily converting [ 11 C]CO 2 into 11 C-amides without conversion of [ 11 C]CO 2 into [ 11 C]CO. Herein, we explore an alternative one-pot synthesis of 11 C-amides using a metal catalyst via the addition of boronic acids/esters to [ 11 C]isocyanates generated in situ from primary amines and [ 11 C]CO 2 . A proof-of-concept for synthesizing [ 11 C]benzanilide directly from [ 11 C]CO 2 using organoboronic esters and tributylphosphoranylidines using copper(I) catalysis was demonstrated. We successfully utilized this novel method for the radiosynthesis of [ 11 C]benzanilide, in RCC of 12%. Further development of this methodology will be needed for wider application in the radiolabeling of 11 C PET radiotracers. Identification of catalyst capable of aiding the transmetallation step while not impeding [ 11 C]CO 2 fixation are likely needed for wider application of this methodology.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.001 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.001 |
| Open science | 0.001 | 0.000 |
| Research integrity | 0.001 | 0.001 |
| Insufficient payload (model declined to judge) | 0.002 | 0.001 |
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 source (direct Gemma or distilled Codex), 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".