SYNTHESIS OF [METHOXY-C-11]PD153035, A SELECTIVE EGF RECEPTOR TYROSINE KINASE INHIBITOR

[Methoxy-C-11]PD153035, a potent and specific inhibitor of the EGF rec eptor tyrosine kinase, was prepared by O-alkylation of O-desmethyl PD1 53035 with [C-11]methyl iodide in DMF. The radiochemical incorporation of [C-11]CH3I was on the order of 45%. The mean specific activity obt ained at end-of-synthesis (EOS) was 26 GBq/mu mol (n = 3; range 20-36 GBq/mu mol) and total synthesis time was 45-50 minutes including formu lation.