The most popular reactions used by medicinal chemists are often incompatible with nanoscale ultrahigh-throughput experimentation (ultraHTE). Now, a set of ultraHTE-amenable reaction conditions is reported for four of the most important transformations in drug discovery, and their generality and scalability tested on a range of complex natural products and drug candidates.
This is a preview of subscription content, log in via an institution to check access.
References
Krska, S. W., DiRocco, D. A., Dreher, S. D. & Shelvin, M. The evolution of chemical high-throughput experimentation to address challenging problems in pharmaceutical synthesis. Acc. Chem. Res. 50, 2976–2985 (2017). This conspectus presents the development of high-throughput experimentation in a medicinal chemistry setting.
Boström, J., Brown, D. G., Young, R. J. & Keserü, G. M. Expanding the medicinal chemistry synthetic toolbox. Nat. Rev. Drug. Discov. 17, 709–727 (2018). This perspective analyses the most common reactions used by medicinal chemists.
Santanilla, A. B. et al. Nanomole-scale high-throughput chemistry for the synthesis of complex molecules. Science 347, 49–53 (2015). This paper presents Buchwald–Hartwig amination in an ultraHTE setting.
Gesmundo, N. J. et al. Nanoscale synthesis and affinity ranking. Nature 557, 228–232 (2018). This paper presents a direct-to-biology merger of nanoscale chemical synthesis and a biochemical assay.
Shen, Y. et al. Automation and computer-assisted planning for chemical synthesis. Nat. Rev. Methods Primers 1, 23 (2021). This primer explores the prominent tools at the interface of chemical synthesis and data science.
Additional information
Publisher’s note Springer Nature remains neutral with regard to jurisdictional claims in published maps and institutional affiliations.
This is a summary of: Gesmundo, N. et al. Miniaturization of popular reactions from the medicinal chemists’ toolbox for ultrahigh-throughput experimentation. Nat. Synth. https://doi.org/10.1038/s44160-023-00351-1 (2023).
Rights and permissions
About this article
Cite this article
A miniaturized toolkit for medicinal chemists. Nat. Synth 2, 1018–1019 (2023). https://doi.org/10.1038/s44160-023-00352-0
Published:
Issue Date:
DOI: https://doi.org/10.1038/s44160-023-00352-0
- Springer Nature Limited