The synthesis of [carboxamido-~(14)C]SAR240550, [carnoxamido-~(14)C]lniparib, via monocarboxylation of 1,4-diiodobenzene

摘要

Iniparib (SAR240550,4-iodo-3-nitrobenzamide) is a novel investi-gational agent for the treatment of various cancers.1 The potential chemotherapeutic activity of this compound has long been recognised.2 To enable ADME (absorption, distribution, metabolism and elimination) and human studies, [carboxamido-~(14)C] SAR240550 (1) was required. As initial metabolic studies had indicated that the amide carbon was metabolically stable, we decided that labelling in that position would be appropriate.