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High-throughput microdroplet-based synthesis using automated array-to-array transfer
Kai-Hung Huang1, Kitmin Chen1, Nicolás M Morato1,2
1Department of Chemistry, Purdue University West Lafayette Indiana 47907 USA cooks@purdue.edu.
Chemical Science
|April 2, 2025
Summary
Automated picomole scale synthesis using desorption electrospray ionization (DESI) accelerates drug discovery. This high-throughput system synthesizes and screens compounds rapidly, enabling efficient analog generation for bioactivity testing.
Area of Science:
- Chemical synthesis and drug discovery
- Analytical chemistry and instrumentation
Background:
- Automated synthesis and high-throughput screening are crucial for accelerating drug discovery.
- Current methods require integration of synthesis and screening technologies.
Purpose of the Study:
- To develop an automated high-throughput picomole scale synthesis system.
- To integrate synthesis and screening using a single technology.
Main Methods:
- Utilized desorption electrospray ionization (DESI) for microdroplet formation and transfer.
- Employed a two-dimensional reactant array for automated synthesis.
- Facilitated on-the-fly chemical transformations during droplet flight.
Main Results:
- Generated 172 analogs with a 64% success rate using multiple reaction types.
- Achieved synthesis throughput of approximately 45 seconds per reaction.
- Produced sufficient product amounts (low ng to low μg) for bioactivity screening.
- Validated quantitative performance using liquid chromatography-mass spectrometry (LC/MS).
Conclusions:
- The developed system consolidates key early drug discovery steps.
- It bridges high-throughput DESI for reaction screening and label-free bioassays.
- This technology enables efficient analog generation and screening for drug discovery.
