Synthesis of covalent [14C]-labeled diarylsulfonylurea (DASU) inhibitors of the processing and release of IL-1

CP-452,759 and CP-470,947, two covalent [14C]-labeled diarylsulfonylurea (DASU) inhibitors of the processing and release of IL-1 from human monocytes, have been synthesized. The radiosyntheses utilize [14C]-labeled phosgene to prepare labeled isocyanates which are coupled with an epoxide sulfonamide to give the [14C]-DASUs. These tools should allow future studies aimed at purifying and identifying the DASU binding protein involved in the inhibition of the processing and release of IL-1 from human monocytes. Copyright © 2002 John Wiley & Sons, Ltd.