Development of a solid‐phase traceless‐Ugi multicomponent reaction for backbone anchoring and cyclic peptide synthesis
Bibliographic record
Abstract
Abstract A new one‐pot methodology to anchor peptides by their backbone to a solid support using an isocyanide‐based multicomponent reaction is described. The approach uses a microwave‐assisted Ugi four‐component reaction to simultaneously condense and bind an N‐protected amino acid and an amino ester to a supported aldehyde. Afterward, the generated backbone anchored dipeptide can be used in solid‐phase peptide synthesis to prepare head‐to‐tail cyclic peptides. Moreover, we also show that peptide fragment ligation can be performed with the described one‐pot anchoring. The backbone anchored peptides can be efficiently released from the resin by microwave‐assisted acidolysis with trifluoroacetic acid. This straightforward one‐pot anchoring approach was also applied to condense fragments and prepare a variety of linear and macrocyclic peptides.
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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 | 0.001 | 0.000 |
| Meta-epidemiology (narrow) | 0.001 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.001 | 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) | 0.001 | 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".