In:
Journal of Labelled Compounds and Radiopharmaceuticals, Wiley, Vol. 53, No. 7 ( 2010-06-15), p. 517-520
Abstract:
The human immunodeficiency virus integrase inhibitor, [ 18 F]MK‐0518, was prepared via a three‐step, one‐pot radiosynthesis. [ 18 F]4‐Fluorobenzylamine was produced from the fluorination of 4‐cyano‐ N , N , N ‐trimethylammonium triflate with [ 18 F]fluoride and reduction with borane methylsulfide complex in 50–68% radiochemical yield. The final step, the coupling of [ 18 F]4‐fluorobenzylamine with an ester coupling partner, achieved an overall uncorrected radiochemical yield after HPLC purification of ∼2%, based on the starting [ 18 F]fluoride. In a typical run, the total synthesis time was about 90 min and gave 0.37–1.74 GBq (10–47 mCi) of [ 18 F]MK‐0518. The radiochemical purity of [ 18 F]MK‐0518 was 〉 98% and the specific activity was 243–1275 Ci/mmol (EOS, n =4). A convenient three‐step, one‐pot radiosynthesis of [ 18 F]MK‐0518 via [ 18 F]4‐fluorobenzylamine has been developed, giving sufficient quantities of [ 18 F]MK‐0518 for animal positron emission tomography studies. Copyright © 2010 John Wiley & Sons, Ltd.
Type of Medium:
Online Resource
ISSN:
0362-4803
,
1099-1344
Language:
English
Publisher:
Wiley
Publication Date:
2010
detail.hit.zdb_id:
1491841-9
detail.hit.zdb_id:
196095-7
SSG:
15,3
