1236352-56-9Relevant articles and documents
Radiosynthesis of the HIV integrase inhibitor [18F]MK-0518 (Isentress)
Li, Wenping,Thompson, Wayne,Fisher, Thorsten,Wai, John S.,Hazuda, Daria,Burns, H. Donald,Hamilla, Terence G.
, p. 517 - 520 (2010)
The human immunodeficiency virus integrase inhibitor, [18F]MK- 0518, was prepared via a three-step, one-pot radiosynthesis. [ 18F]4-Fluorobenzylamine was produced from the fluorination of 4-cyano-N,N,N-trimethylammonium triflate with [18F]fluoride and reduction with borane methylsulfide complex in 50-68% radiochemical yield. The final step, the coupling of [18F]4-fluorobenzylamine with an ester coupling partner, achieved an overall uncorrected radiochemical yield after HPLC purification of ~2%, based on the starting [18F]fluoride. In a typical run, the total synthesis time was about 90 min and gave 0.37-1.74 GBq (10-47 mCi) of [18F]MK-0518. The radiochemical purity of [ 18F]MK-0518 was >98% and the specific activity was 243-1275 Ci/mmol (EOS, n = 4). A convenient three-step, one-pot radiosynthesis of [ 18F]MK-0518 via [18F]4-fluorobenzylamine has been developed, giving sufficient quantities of [18F]MK-0518 for animal positron emission tomography studies. Copyright