Raphaël Hoareau, P. Scott
Jun 30, 2010
Citations
0
Influential Citations
3
Citations
Journal
Tetrahedron Letters
Abstract
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 [ 11 C]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.