Miniaturization of Popular Reactions from the Medicinal Chemists’ Toolbox for Ultrahigh-Throughput Experimentation

18 May 2022, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


Miniaturization is a tactic employed in many technologies to accelerate discovery and enable new applications such as systems-level evaluation. The miniaturization of chemical synthesis to the limits of chemoanalytical and bioanalytical limits of detection could accelerate drug discovery by increasing the amount of experimental data collected per milligram of material consumed. Here we demonstrate the miniaturization of popular reactions used in drug discovery such as reductive amination, N-alkylation, N-Boc deprotection and Suzuki coupling for utilization in 1.2 μL reaction droplets. Reaction methods were evolved to perform in high boiling solvents at room temperature, enabling the diversification of precious starting materials, such as the complex natural product staurosporine.


Suzuki Coupling
Reductive Amination
High Throughput Experimentation


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