MK-8457

Aromatic C-H bromination is one of the applications of late stage functionalization that provides precursors for generation of radio-labeled compounds to support drug metabolism and pharmacokinetic (DMPK) studies or provide a handle for further functionalization to expand SAR studies without having to resort to de novo synthesis.Electrochem. aromatic bromination was attempted on late stage intermediates and drug mols. such as cytidine, uridine, Tenofovir, MK-4618, Sch48973 and MK-8457.The reactions were conducted under mild galvanostatic electrolysis condition in aqueous NaBr solutionThe brominated products were obtained and converted to the corresponding tritium labeled products.Electrochem. methodol. provides an alternative way to quickly generate aryl bromides of late stage intermediates or drug mols. that are very useful in drug discovery.