Electrochemical bromination of late stage intermediates and drug molecules

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