A novel one-pot palladium-mediated synthesis of N-[(2-hydroxyphenyl)methyl]-N-(4-phenoxy-3-pyridinyl) acetamide, the precursor to [C]PBR28, a PET biomarker for the peripheral benzodiazepine receptor |
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Authors: | Raphaël Hoareau |
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Institution: | Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA |
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Abstract: | Due to an urgent need to image the peripheral benzodiazepine receptor (PBR) in living human subjects using positron emission tomography imaging, we had cause to prepare N-(2-hydroxyphenyl)methyl]-N-(4-phenoxy-3-pyridinyl) acetamide (desmethyl-PBR28 (1)), the precursor to 11C]PBR28. Herein, we report a new synthesis of the precursor in which palladium-mediated reduction of the nitro pyridine to the corresponding amino pyridine, and subsequent reductive amination, can be achieved with decaborane in a convenient one-pot procedure. This procedure is operationally simpler than the current alternatives and provides high quality precursor suitable for use in clinical applications. |
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Keywords: | [11C]PBR28 Positron emission tomography Radiopharmaceutical synthesis |
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