Chemical Synthesis of (<i>S</i>)‐Spiro(estradiol‐17,2′‐[1,4]oxazinan)‐6′‐one Derivatives Bearing Two Levels of Molecular Diversity
Bibliographic record
Abstract
Abstract The present study shows the development of a strategy that can afford different estradiol derivatives bearing a 17‐spiro‐δ‐lactone moiety with a nitrogen atom inserted in the lactone ring. Such [1,4]oxazinan‐6′‐one derivatives contain two levels of molecular diversity introduced to modulate biological activity. The strategy employed to prepare these compounds includes the stereoselective formation of a 17β‐oxirane from the carbonyl group of estrone, the regioselective opening of the resulting oxirane with various hydrophobic amino acids (giving the first level of diversity), the spirolactonization, the alkylation of nitrogen by different functional groups (producing the second level of diversity), and final deprotection, when necessary. A series of ( S )‐spiro(estradiol‐17,2′‐[1,4]oxazinan)‐6′‐one derivatives was generated to illustrate the usefulness of this diversification strategy, which could easily be extended to other steroidal and nonsteroidal ketone scaffolds for interacting with additional biological targets. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
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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 | 0.001 |
| 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 | 0.001 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| 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 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".