6533b7cefe1ef96bd12578d6

RESEARCH PRODUCT

Efficient alkali iodide promoted 18F-fluoroethylations with 2-[18F]fluoroethyl tosylate and 1-bromo-2-[18F]fluoroethane

Andreas BaumanFrank RöschMarkus PielRalf Schirrmacher

subject

chemistry.chemical_classificationReaction conditionsOrganic ChemistryIodideAlkali metalBiochemistrychemistry.chemical_compoundFluoroethyl tosylatechemistryYield (chemistry)LabellingDrug DiscoveryCholineFluoroethylNuclear chemistry

description

Abstract Radiochemical 18 F-fluorination yields of several compounds using the secondary labelling precursors 2-[ 18 F]fluoroethyl tosylate ([ 18 F]FETos) and 1-bromo-2-[ 18 F]fluoroethane ([ 18 F]BFE) could be considerably enhanced by the addition of an alkali iodide. The radiochemical yield of [ 18 F]fluoroethyl choline for example could be doubled with [ 18 F]BFE and increased from 13% to ≈80% with [ 18 F]FETos. By addition of alkali iodide to the precursor, the 18 F-fluoroethylation yields of established radiopharmaceuticals, especially in the case of automated syntheses, could be significantly increased without major changes of the reaction conditions.

yearjournalcountryeditionlanguage
2003-12-01Tetrahedron Letters
https://doi.org/10.1016/j.tetlet.2003.10.034