An efficient synthesis of the precursors of [C-11]MDL 100907 labeled in two specific positions

An efficient, integrated route for the synthesis of two precursors of [C-11 ]MDL 100907 labeled in the 2'- or 3'-methoxy position is reported. The synt hesis involved a one-pot, two-step process to transform the intermediate es ters to ketones and subsequent resolution of the racemic alcohols to their respective enantiomers. The resolved, enantiomerically pure phenol precurso rs were reacted with high specific activity [C-11]methyl iodide to produce [C-11]MDL 100907 labeled in two specific positions.