Synthesis and carbon-11 labeling of (R)- and (S)-thionisoxetine, norepinephrine reuptake inhibitors, potential radioligands for positron emission tomography

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• 作者：Maria Azzurra Filannino ; Mario Matarrese ; Elia Anna Turolla ; Valeria Masiello ; Rosa Maria Moresco ; Sergio Todde ; Elisa Verza ; Fulvio Magni ; Angela Cattaneo ; Angela Bachi ; Marzia Galli Kienle ; Ferrucc
• 关键词：Norepinephrine uptake inhibitor ; NET ; Depression ; Carbon-11 ; PET
• 刊名：Applied Radiation and Isotopes
• 出版年：2007
• 期刊代码：6_09698043
• 类别：ce
• 出版时间：November 2007
• 卷：65
• 期：11
• 页码：1232-1239
• 文件大小：233 K

摘要

Standards and des-methyl precursors of (R)- and (S)-thionisoxetine, potent and selective norepinephrine reuptake inhibitors, were synthesized and radiolabeled with carbon-11. Both enantiomers of the N-methyl-3-(2-thiomethylphenoxy)-3-phenylpropanamine and the 3-(2-thiomethylphenoxy)-3-phenylpropylamine were obtained via multi-step syntheses, while the radiosyntheses were carried out using [¹¹C]CH₃I. The radiochemical yields were 26%, decay corrected and the specific radioactivity ranging from 2 to 3 Ci/μmol. The HPLC analyses were performed using a chiral column: during the radiolabeling, no racemization occurred and the isomers were synthesized with high enantiomeric purity.