Acoustic Droplet Ejection Enabled Automated Reaction Scouting
| Autor: | Shabnam Shaabani, Katarzyna Kurpiewska, Justyna Kalinowska-Tluscik, Joe Olechno, Yuanze Wang, Alexander Dömling, Matthew Groves, Richard N. Ellson, Li Gao, Maryam Ahmadianmoghaddam, Michael Kossenjans, Ruixue Xu, Victoria Helan |
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| Přispěvatelé: | Drug Design, Medicinal Chemistry and Bioanalysis (MCB) |
| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
010405 organic chemistry
business.industry General Chemical Engineering Pipeline (computing) General Chemistry 010402 general chemistry 01 natural sciences 0104 chemical sciences chemistry.chemical_compound Chemistry chemistry Miniaturization Organic synthesis Process engineering business Acoustic droplet ejection QD1-999 Research Article |
| Zdroj: | ACS Central Science, Vol 5, Iss 3, Pp 451-457 (2019) ACS central science, 5(3), 451-457. AMER CHEMICAL SOC INC ACS Central Science |
| ISSN: | 2374-7951 2374-7943 |
| Popis: | Miniaturization and acceleration of synthetic chemistry are critically important for rapid property optimization in pharmaceutical, agrochemical, and materials research and development. However, in most laboratories organic synthesis is still performed on a slow, sequential, and material-consuming scale and not validated for multiple substrate combinations. Herein, we introduce fast and touchless acoustic droplet ejection (ADE) technology into small-molecule chemistry to transfer building blocks by nL droplets and to scout a newly designed isoquinoline synthesis. With each compound in a discrete well, 384 random derivatives were synthesized in an automated fashion, and their quality was monitored by SFC-MS and TLC-UV-MS analysis. We exemplify a pipeline of fast and efficient nmol scouting to mmol- and mol-scale synthesis for the discovery of a useful novel reaction with great scope. High-throughput automated nmol synthesis of novel isoquinolines via acoustic droplet ejection technology leads to unprecedented fast exhaustive reaction evaluation and rapid scope and limitation. |
| Databáze: | OpenAIRE |
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