One-step synthesis of 2-arylbenzothiazole (‘BTA’) and -benzoxazole precursors for in vivo imaging of β-amyloid plaques

We report the simple and efficient synthesis of 2-arylbenzothiazoles (‘BTA’) and 2-arylbenzoxazoles by direct coupling of benzothiazoles or benzoxazoles with aryl bromides. This method permits direct one-step access to precursors of radiolabeled BTA-1 and BTA-2 and their 6-methoxy analogues, used for in vivo imaging of β-amyloid plaques with positron emission tomography (PET).