Synthesis of MMP inhibitor radiotracer [11C]CGS 25966, a new potential PET tumor imaging agent

[C-11]CGS 25966, a novel radiolabeled matrix metalloproteinase (MMP) inhibitor, has been synthesized for evaluation as new potential positron emission tomography (PET) tumor imaging agent. The precursor was labeled by [C-11]methyl triflate through O-[C-11]methylation method at the hydroxyl position of phenol under basic conditions and isolated by HPLC purification to produce pure target compound in 15-25% radiochemical yield, based on (CO2)-C-11, decay corrected to end of bombardment. Copyright (C) 2003 John Wiley Sons, Ltd.