Abstract
A carbon-11-labeled sulfamate derivative was designed and synthesized as a new potential positron-emission-tomography dual aromatase–steroid sulfatase inhibitor radiotracer for imaging of aromatase and steroid sulfatase expression in breast cancer. The target tracer 2-chloro-4-(((4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino)methyl)-6-[11C]methoxyphenyl sulfamate ([11C]7) was prepared from its corresponding precursor 2-chloro-4-(((4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino)methyl)-6-hydroxyphenyl sulfamate (18) with [11C]CH3OTf under basic conditions through the O-[11C]methylation and isolated by the reversed-phase high-performance liquid chromatography in 40–45% radiochemical yields based on [11C]CO2 and decay corrected to end of bombardment. The specific activity at end of synthesis was 111-185 GBq/μmol.
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