Synthesis of two radiofluorinated cocaine analogues using distilled 2-[18F]fluoroethyl bromide
Identifieur interne : 000B83 ( Istex/Curation ); précédent : 000B82; suivant : 000B84Synthesis of two radiofluorinated cocaine analogues using distilled 2-[18F]fluoroethyl bromide
Auteurs : Alan A. Wilson [Canada] ; Jean N. Dasilva [Canada] ; Sylvain Houle [Canada]Source :
- Applied Radiation and Isotopes [ 0969-8043 ] ; 1995.
Abstract
Two fluorinated congeners of cocaine, 2'-fluoroethyl (IR-2-exo-3-exo)-8-methyl-3-(4-methylphenyl)-8azabicyclo[3.2.I ]octane-2-carboxylate (FETT) and its 4-chlorophenyl analogue (FECT) were synthesized. Radiolabelling with 18F was achieved by O-[18F]fluoroalkylation of the corresponding carboxylic acid salts with distilled 2-[18F]fluoroethyl bromide in DMF. After HPLC purification, yields of radiochemically pure, formulated products were 22–30% (not corrected for decay) in a synthesis time of 60–70 min. The use of distilled 2-['8F]fluoroethyl bromide was indispensable for the reliable production of pure products.
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DOI: 10.1016/0969-8043(95)00028-C
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<front><div type="abstract" xml:lang="en">Two fluorinated congeners of cocaine, 2'-fluoroethyl (IR-2-exo-3-exo)-8-methyl-3-(4-methylphenyl)-8azabicyclo[3.2.I ]octane-2-carboxylate (FETT) and its 4-chlorophenyl analogue (FECT) were synthesized. Radiolabelling with 18F was achieved by O-[18F]fluoroalkylation of the corresponding carboxylic acid salts with distilled 2-[18F]fluoroethyl bromide in DMF. After HPLC purification, yields of radiochemically pure, formulated products were 22–30% (not corrected for decay) in a synthesis time of 60–70 min. The use of distilled 2-['8F]fluoroethyl bromide was indispensable for the reliable production of pure products.</div>
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