Late-Stage Saturation of Drug Molecules

Title	Late-Stage Saturation of Drug Molecules
Authors	De-Hai Liu, Philipp M. Pflüger, Andrew Outlaw, Lukas Lückemeier, Fuhao Zhang, Clinton Regan, Hamid Rashidi Nodeh, Tim Cernak, Jiajia Ma, Frank Glorius
Magazine	Journal of the American Chemical Society
Date	04/15/2024
DOI	10.1021/jacs.4c00807
Introduction	Contemporary chemical synthesis has enabled the widespread use of aromatic rings in pharmaceuticals. While these sp2-carbon-rich structures are easy to synthesise, their flat and lipophilic nature limits drug efficacy. This study demonstrates that mild rhodium-catalysed hydrogenation, acid-mediated reduction, and photocatalysed hydrogenation can convert aromatic and heteroaromatic drugs into saturated analogues with improved medicinal properties by increasing sp3 carbon content. These methods enhance the solubility, metabolic stability, and efficacy of drugs, and are effective across diverse chemical environments. Notably, the rhodium-catalysed approach is compatible with traces of DMSO or water, allowing the reformulation of stored compounds for chemical synthesis applications, as evidenced by the late-stage saturation of 768 complex drugs.
Quote	Liu, D.-H.; Pflüger, P. M.; Outlaw, A.; Lückemeier, L.; Zhang, F.; Regan, C.; Nodeh, H. R.; Cernak, T.; Ma, J.; Glorius, F. Late-Stage Saturation of Drug Molecules. J. Am. Chem. Soc. 2024, 146, 11866-11875. https://doi.org/10.1021/jacs.4c00807
Element	Carbon (C) , Rhodium (Rh)
Materials	Chemical Compounds
Industry	Pharmaceutical Industry

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