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

Article abstract of DOI:10.1002/(SICI)1099-1344(199910)42:10<949::AID-JLCR253>3.0.CO;2-S

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