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

Article abstract of DOI:10.1002/(SICI)1099-1344(199807)41:7<623::AID-JLCR120>3.0.CO;2-Q

[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.