Studies of continuous-flow synthesis of nonpeptidal bistetrahydrofuran moiety of Darunavir
Bibliographic record
Abstract
The AIDS (acquired immunodeficiency syndrome) has become one of the most pressing medical concerns of our time. Specifically, the critical function of HIV protease has made it an important target for the treatment of HIV/AIDS. The approval of the first protease inhibitor (PI), saquinavir and its introduction into highly active antiretroviral therapy (HAART), with reverse transcriptase inhibitors, led to significantly enhanced HIV management and improved the quality of life of HIV/ AIDS patients. The future management of HIV/AIDS should rely upon the development of therapies that are less toxic and more effective in combating drugresistance. In this context, the Darunavir have enjoyed a surge in popularity as a new generation of PIs bearing a structure-based designed bis-THF ligand that effectively fills in the hydrophobic pocket and maximizes hydrogen bonding interactions with the backbone atoms of the S2-site. A number of bis-THF-derived inhibitors are exceedingly potent and have maintained very impressive potency against multidrug-resistant HIV-1 variants. We are interested in the use of continuous-flow approach in order to prepare the bis-THF moiety of PIs. This approach will allow a cascade effect by doing the reduction and the acetylation steps in a closed system.
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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 | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 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 | 0.001 |
| Insufficient payload (model declined to judge) | 0.002 | 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 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".