Development and Application of N-acylation/Aza-Michael Addition Multicomponent Reaction of Di-/polyamines Using Trichloromethylketones as a Chemoselective Acylating Reagent
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
Multicomponent reactions (MCRs) are a class of reactions comprising three or more components in situ offering an array of advantages such as atom economy, efficiency, scaffold variability, and convenience compared to conventional stepwise synthesis. Herein, utilization of trichloromethyl ketones as a chemoselective acylating agent for the primary amine of a di-/polyamine with simultaneous Aza-Michael addition at the secondary amine is elaborated. The optimal reaction condition for the MCR was screened with different solvents, catalysts, and catalyst concentrations. Upon establishing appropriate parameters wide assessment of scope of the reaction was carried out to determine the versatility and limitations of using different Michael acceptors, di-/ polyamines, trichloromethyl ketones, and other electrophiles (i.e., isothiocyanate, carbamoyl imidazole). The utility of the MCR method in the synthesis of natural products or biologically active small molecules has been attempted with total synthesis of enisorine D in a convergent fashion.
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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 | 0.001 | 0.001 |
| Meta-epidemiology (narrow) | 0.001 | 0.001 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.001 | 0.001 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.001 | 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 it