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Preparation of fluorine 18 labeled 6 fluoro 9 benzyl purine and 2 fluoro 9 benzyl purine as a potential brain scanning agent


, : Preparation of fluorine 18 labeled 6 fluoro 9 benzyl purine and 2 fluoro 9 benzyl purine as a potential brain scanning agent. International Journal of Applied Radiation & Isotopes 33(8): 633-636

The preparations of [18F]-6-fluoro-9-benzylpurine(I) and [18F]-2-fluoro-9-benzylpurine are described. I was prepared by 2 methods: halogen exchange of 6-chloro-9-benzylpurine with Ag18F; and displacement of trimethylpurin-6-ylammonium chloride with K18F, followed by 9N benzylation. The latter labeling method was far superior, both in radiochemical yield and in specific activity. I was relatively stable in a Tris-HCl buffer (0.4 M pH 7.6) at 37.degree. C but was easily hydrolyzed in 1 N HCl. Biodistribution of I in mice demonstrated high uptake in the brain. I is a potential brain-scanning radiopharmaceutical for positron computed tomography.

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Related references

Fukushi K.; Irie T.; Inoue O.; Yumazaki T., 1982: Fluorine 18 labeled 9 benzyl 6 fluoro purine a new type of metabolically trapped agent for brain studies. Journal of Nuclear Medicine 23(5): P23

Irie T.; Fukushi K.; Ido T., 1982: Synthesis of fluorine 18 labeled 6 fluoro purine and fluorine 18 labeled 6 fluoro 9 beta d ribo furanosyl purine. Introduction of 18F into the 6-position of purines is described. 18F-6-fluoropurine and 18F-6-fluoro-9-.beta.-D-ribofuranosylpurine were prepared with high radiochemical yields by nucleophilic displacement of the trimethylammonio-group of purine w...

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