Among the currently available positron emitters suitable for Positron Emission Tomography (PET), 124
I has the longest physical half-life (4.2 days). The long half-life and well-investigated behavior of iodine in vivo
I very attractive for pharmacological studies. In this communication, we describe a simple yet effective method for the synthesis of novel 124
I labeled compounds intended for PET imaging of arylsulfatase activity in vivo
. Arylsulfatases have important biological functions, and genetic deficiencies of such functions require pharmacological replacement, the efficacy of which must be properly and non-invasively evaluated. These enzymes, even though their natural substrates are mostly of aliphatic nature, hydrolyze phenolic sulfates to phenol and sulfuric acid. The availability of [124
I]iodinated substrates is expected to provide a PET-based method for measuring their activity in vivo
. The currently available methods of synthesis of iodinated arylsulfates usually require either introducing of a protected sulfate ester early in the synthesis or introduction of sulfate group at the end of synthesis in a separate step. The described method gives the desired product in one step from an aryl-alkyl cyclic sulfate. When treated with iodide, the source cyclic sulfate opens with substitution of iodide at the alkyl center and gives the desired arylsulfate monoester.