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An Automated Electrochemical Flow Platform to Accelerate Library Synthesis and Reaction Optimization.

Authors :
Rial‐Rodríguez, Eduardo
Williams, Jason D.
Cantillo, David
Fuchß, Thomas
Sommer, Alena
Eggenweiler, Hans‐Michael
Kappe, C. Oliver
Laudadio, Gabriele
Source :
Angewandte Chemie; 12/16/2024, Vol. 136 Issue 51, p1-6, 6p
Publication Year :
2024

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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
00448249
Volume :
136
Issue :
51
Database :
Complementary Index
Journal :
Angewandte Chemie
Publication Type :
Academic Journal
Accession number :
181516707
Full Text :
https://doi.org/10.1002/ange.202412045