Alternative efficient tritium labeling of repaglinide

Abstract

There is a need for an efficient tritium labeling methodology for repaglinide to support numerous in vitro and in vivo studies. Numerous homogeneous and heterogeneous catalysts were screened for their capacity to tritiate repaglinide directly without the need to synthesize suitable precursors and to avoid multistep synthesis. In particular, boosting effects using a combination of homogeneous and heterogeneous catalysts were examined. Finally, a suitable method was selected for tritation and resulted in an efficient tritation of repaglinide via a heterogeneous catalyzed hydrogen–tritium exchange reaction with iridium black as the preferred catalyst.