61714-13-4Relevant academic research and scientific papers
Synthesis of carbon-14 labelled (3-{[(Z)-5-Chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indol-1-yle]carbonylamino}propyl)trimethylammonium chloride, a potential cartilage-targeted antirheumatic drug
Giraud, Isabelle,Rapp, Maryse,Dupuy, Jean-Michel,Maurizis, Jean-Claude,Madelmont, Jean-Claude
, p. 297 - 308 (2007/10/03)
A [14C]-labelled form of (3-{[(Z)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indol-1-yle]carbonylamino}propyl)trimethylammonium chloride, a potential cartilage-targeted antirheumatic drug, was required for pharmacokinetic studies. This compound, labelled with [14C] located in the C-3 methylene position, was prepared in four steps starting from N-[3-(dimethylamino)propyl]-5-chloro-2,3-dihydro-2-oxo-1H-indole-1-carboxamide and 2-thiophene-[14C]carbonyl chloride, previously synthesized by a two-step sequence from barium [14C]-carbonate and 2-thienyllithium. The desired product was obtained with a specific activity of 359 MBq/mmol (9.7 mCi/mmol). The overall radiochemical yield was 50% based on barium [14C]-carbonate.
