F‐18 labelled N,N‐bis‐haloethylamino‐phenylsulfoxides — a new class of compounds for the imaging of hypoxic tissue

Abstract

AbstractTwo N,N‐bis‐chloroethylamino‐phenylsulfoxides have been synthesized and radiolabelled with F‐18 via halogen exchange. The radiolabelling of both compounds proceeds smoothly with K[18F]F‐kryptofix 2.2.2 complex at 100 °C in DMSO. Decay‐corrected radiochemical yields were 25–35% for [18F]12 (SO201) and 35–45% for [18F]11 (SO101), with an average specific activity of 1.8 Ci/µmol. Both compounds remained 80% intact in plasma over a period of 2 h. In vivo binding in a stroke model indicates that both markers are selectively retained in hypoxic tissue. Copyright © 2006 John Wiley & Sons, Ltd.