AI Article Synopsis
- - Automated electrochemical platforms face challenges in miniaturization and flow design, limiting their development compared to established thermal and photochemical setups.
- - A new automated electrochemical flow platform was created, demonstrating successful electrochemical C-N cross-couplings with a variety of amines, showcasing its potential for medicinal chemistry.
- - The platform underwent Design of Experiments (DoE) optimization, leading to a 6-fold increase in reaction yield for a previously unsuccessful library target, highlighting its versatility and efficiency.
Article Abstract
Automated batch and flow setups are well-established for high throughput experimentation in both thermal chemistry and photochemistry. However, the development of automated electrochemical platforms is hindered by cell miniaturization challenges in batch and difficulties in designing effective single-pass flow systems. In order to address these issues, we have designed and implemented a new, slug-based automated electrochemical flow platform. This platform was successfully demonstrated for electrochemical C-N cross-couplings of E3 ligase binders with diverse amines (44 examples), which were subsequently transferred to a continuous-flow mode for confirmation and isolation, showing its applicability for medicinal chemistry purposes. To further validate the versatility of the platform, Design of Experiments (DoE) optimization was performed for an unsuccessful library target. This optimization process, fully automated by the platform, resulted in a remarkable 6-fold increase in reaction yield.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11627123 | PMC |
| http://dx.doi.org/10.1002/anie.202412045 | DOI Listing |
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