Deuterium in drug discovery: progress, opportunities and challenges

RMC Di Martino, BD Maxwell, T Pirali - Nature Reviews Drug Discovery, 2023 - nature.com
Substitution of a hydrogen atom with its heavy isotope deuterium entails the addition of one
neutron to a molecule. Despite being a subtle change, this structural modification, known as …

Electrocatalytic reductive deuteration of arenes and heteroarenes

F Bu, Y Deng, J Xu, D Yang, Y Li, W Li, A Lei - Nature, 2024 - nature.com
The incorporation of deuterium in organic molecules has widespread applications in
medicinal chemistry and materials science,. For example, the deuterated drugs austedo …

The Versatile and Strategic O-Carbamate Directed Metalation Group in the Synthesis of Aromatic Molecules: An Update

RD Jansen-van Vuuren, S Liu, MAJ Miah… - Chemical …, 2024 - ACS Publications
The aryl O-carbamate (ArOAm) group is among the strongest of the directed metalation
groups (DMGs) in directed ortho metalation (D o M) chemistry, especially in the form Ar …

Palladium(II)‐Catalyzed Nondirected Late‐Stage C(sp2)−H Deuteration of Heteroarenes Enabled Through a Multi‐Substrate Screening Approach

J Dey, S Kaltenberger… - Angewandte Chemie …, 2024 - Wiley Online Library
The importance of deuterium labelling in a variety of applications, ranging from mechanistic
studies to drug‐discovery, has spurred immense interest in the development of new …

Sulfonium Salt Reagents for the Introduction of Deuterated Alkyl Groups in Drug Discovery

K Ban, K Imai, S Oyama, J Tokunaga… - Angewandte Chemie …, 2023 - Wiley Online Library
The pharmacokinetics of pharmaceutical drugs can be improved by replacing C− H bonds
with the more stable C− D bonds at the α‐position to heteroatoms, which is a typical …

Electrochemical α-deuteration of amides

S Ning, C Wu, L Zheng, M Liu, Y Zhang, X Che… - Green …, 2023 - pubs.rsc.org
Precise deuterium incorporation of bioactive molecules is highly desirable in order to
improve ADME properties and monitor pharmacokinetics. Organic electrochemistry offers a …

Two is better than one: Deuterium in analytical mass spectrometry

R Bąchor, M Modzel, M Cebrat, M Kijewska… - TrAC Trends in …, 2024 - Elsevier
This review explores the diverse applications of deuterium in medicinal chemistry,
particularly as an analytical tool in mass spectrometry. Deuterium applications extend …

Late-Stage C–H Deuteration of Organic Compounds via Ligand-Enabled Palladium-Catalyzed Hydrogen Isotope Exchange

J Dey, M van Gemmeren - Synlett, 2024 - thieme-connect.com
Over the past years our lab has established a research program towards the late-stage
introduction of deuterium into organic molecules using Pd-catalyzed reversible C–H …

Deuteration for Metabolic Stabilization of SARS-CoV-2 Inhibitors GC373 and Nirmatrelvir

TJ Van Oers, A Piercey, A Belovodskiy, B Reiz… - Organic …, 2023 - ACS Publications
Nirmatrelvir and GC373 inhibit the SARS-CoV-2 3CL protease and hinder viral replication in
COVID-19. As nirmatrelvir in Paxlovid is oxidized by cytochrome P450 3A4, ritonavir is …

Unlocking the potential of hydrogen deuterium exchange via an iterative continuous-flow deuteration process

K Tatoueix, M Lepron, C Barboux… - Nature …, 2025 - nature.com
Labelled compounds bearing hydrogen isotopes are keystones in diverse areas constituting
a multi-billion dollar global market including drugs, diagnostics, biology, toxicology and …