Diversity-Oriented Synthesis and Preliminary Biological Screening of Highly Substituted Five-Membered Lactones and Lactams Originating From an Allyboration of Aldehydes and Imines
Why this work is in the frame
A frame that forgets how it found something cannot be audited. These are the routes that admitted this work.
Bibliographic record
Abstract
alpha-exo-Methylene-gamma-lactones and alpha-exo-methylene-gamma-lactams are key structural units in a wide variety of natural products. These substances exhibit a high degree of bioactivity against numerous biological targets that play important roles in several diseases. A library of functionalized gamma-lactones and gamma-lactams containing both unsaturated and saturated side chains at the alpha position of the ring was synthesized. The generation of this library first involves sequential allylation of aldehydes or imines with 2-alkoxycarbonyl allylboronates, followed by ring closure to give alpha-exo-methylene-gamma-lactones or alpha-exo-methylene-gamma-lactams, which are subjected to various transition metal catalyzed coupling reactions to introduce additional diversity. A subset of the library was screened for inhibition of homoserine transacetylase (HTA) from Haemophilus influenzae and showed promising initial activity profiles.
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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 | 0.001 |
| 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 | 0.000 |
| 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 it