Synthesis of deuterium-labeled celecoxib and its metabolites

AbstractCelecoxib are COX2 inhibitors approved to reduce the COX2 level. Celecoxib and its major metabolites labeled with deuteriums are applied for drug metabolism studies. [2H4] celecoxib was prepared from [2H4] 4-acetamidobenzenesolfonyl through amination, hydrosis, diazotization, reduction and cyclization. After bromination and hydrolysis reaction, [2H4] hydroxy celecoxib was obtained and further oxidized by tetrabutylammonium permanganate to afford [2H4] celecoxib carboxylic acid. The title compounds showed remarkable chemical purity and isotope abundance which can be utilized in pharmacokinetic research.
Source: Journal of Radioanalytical and Nuclear Chemistry - Category: Nuclear Medicine Source Type: research