Comparison of synthetic routes for fully substituted (1H-1,2,3-triazol-4-yl)acetic acids
Why this work is in the frame
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Bibliographic record
Abstract
The new fully substituted (1H-1,2,3-triazol-4-yl)acetic acids were synthesized from available precursors (1H-1,2,3-triazol-4-yl)ethanones and 1Н-1,2,3-triazole-4-carboxylic acids, which are easily prepared by the Dimroth reaction from azides and 1,3-dicarbonyl compounds. The practical methods of homologization (the Arndt–Eistert reaction and homologization as a result of nucleophilic substitution by cyanide anion) and the Willgerodt-Kindler reaction were compared. The Willgerodt-Kindler method starting from (5-methyl-1H-1,2,3-triazol-4-yl)ethanones was selected as the most convenient method for the synthesis of 2-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)acetic acids, which are promising building blocks for drug discovery. Additionally, (1H-1,2,3-triazol-4-yl)ethanones were studied for the synthesis of alcohols, amines and in the Johnson–Corey–Chaykovsky reaction.
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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 | 0.000 | 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 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 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