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Synthesis of [methoxy‐ 11 C]PD153035, a selective EGF receptor tyrosine kinase inhibitor
Author(s) -
Johnström Peter,
Fredriksson Anna,
Thorell JanOlov,
StoneElander Sharon
Publication year - 1998
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199807)41:7<623::aid-jlcr120>3.0.co;2-q
Subject(s) - chemistry , tyrosine kinase , methyl iodide , alkylation , iodide , desmethyl , tyrosine kinase inhibitor , receptor tyrosine kinase , tyrosine , chemical synthesis , receptor , stereochemistry , in vitro , biochemistry , medicinal chemistry , medicine , organic chemistry , cancer , metabolite , catalysis
[Methoxy‐ 11 C]PD153035, a potent and specific inhibitor of the EGF receptor tyrosine kinase, was prepared by O ‐alkylation of O ‐desmethyl PD153035 with [ 11 C]methyl iodide in DMF. The radiochemical incorporation of [ 11 C]CH 3 I 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.