La maladie de Parkinson au Canada (serveur d'exploration)

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Synthesis of two radiofluorinated cocaine analogues using distilled 2-[18F]fluoroethyl bromide

Identifieur interne : 003F43 ( Main/Exploration ); précédent : 003F42; suivant : 003F44

Synthesis of two radiofluorinated cocaine analogues using distilled 2-[18F]fluoroethyl bromide

Auteurs : Alan A. Wilson [Canada] ; Jean N. Dasilva [Canada] ; Sylvain Houle [Canada]

Source :

RBID : ISTEX:6A92F1F303A7E7C251957485EA79760C59A3243E

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.

Url:
DOI: 10.1016/0969-8043(95)00028-C


Affiliations:


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Le document en format XML

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<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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