Synthesis of [methoxy-11C]PD153035, a selective EGF receptor tyrosine kinase inhibitor

Abstract

[Methoxy-11C]PD153035, a potent and specific inhibitor of the EGF receptor tyrosine kinase, was prepared by O-alkylation of O-desmethyl PD153035 with [11C]methyl iodide in DMF. The radiochemical incorporation of [11C]CH3I was on the order of 45%. The mean specific activity obtained at end-of-synthesis (EOS) was 26 GBq/μmol (n=3; range 20–36 GBq/μmol) and total synthesis time was 45–50 minutes including formulation. © 1998 John Wiley & Sons, Ltd.