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A guide for the synthesis of key nucleoside scaffolds in drug discovery

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Abstract

This review aims to provide an overview of the synthetic strategies employed for generating modifications within the sugar backbone of nucleoside analogs. We have focused our discussions on the more popular scaffolds seen in medicinal chemistry including modifications to ribose-based nucleosides and 4ʹ-thionucleosides. Importantly, the syntheses of emerging nucleoside chemotypes from recent patent literature are also discussed. We believe a detailed review centered in this critical area of research may help identify unsolved synthetic challenges and inspire the development of new methods for expanding the accessible chemical space in nucleoside-based drug discovery.

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  1. These authors contributed equally: Dinithi G. Rajapaksha, Subhojit Mondal, Jason W. Wang

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  1. Department of Chemistry, University of Alberta, Edmonton, AB, Canada

    Dinithi G. Rajapaksha, Subhojit Mondal, Jason W. Wang & Michael W. Meanwell

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Rajapaksha, D.G., Mondal, S., Wang, J.W. et al. A guide for the synthesis of key nucleoside scaffolds in drug discovery. Med Chem Res 32, 1315–1333 (2023). https://doi.org/10.1007/s00044-023-03096-w

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