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Novel synthesis of [18F]-fluorobenzene and pyridinecarbohydrazide-folates as potential PET radiopharmaceuticals

✍ Scribed by I. Al Jammaz; B. Al-Otaibi; S. Okarvi; J. Amartey

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
144 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis

In an attempt to visualize folate receptors that over-express on many cancers, [ 18 F]fluorobenzene and pyridine carbohydrazide-folates were synthesized using two different synthetic approaches starting from nucleophilic displacement reactions on ethyl-trimethylammonium-benzoate and pyridine carboxylate precursors. The intermediates ethyl [ 18 F]-fluorinated benzene and pyridine esters were reacted with hydrazine to produce the [ 18 F]-fluorobenzene and pyridine carbohydrazides followed by coupling with NHS-folate 11 in the first approach. Whereas hydrazide-folate 5 was reacted with 2,5-dioxoazolidinyl [ 18 F]-fluorobenzenecarboxylate in the second approach. Based on starting [ 18 F]-fluoride, radiochemical yields and synthesis times were found to be around 80% (45 min) and 35% (80 min) for the first and the second approaches, respectively. The first synthetic approach holds considerable promise as a rapid and simple method for the radiofluorination of folic acid with high radiochemical yield and short time.

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