AbstractThe muscarinic cholinergic receptor antagonist dexetimide and its pharmacologically inactive enantiomer levetimide were labelled with the positron emitter bromine‐76. [76Br]4‐Bromodexetide, [76Br]BrDEX, and [76Br]4‐bromolevetimide, [76]BrLEV, were prepared via electrophilic bromodesilylation of 4‐(trimethylsilyl)dexetimide and 4‐(trimethyylsilyl)levetimide with [76Br]NH4. The use of chloramine‐T in acid media resulted in radiochemical yields of 80%. The radiotracers were purified by semi‐preparative reverse‐phase HPLC. Radiochemical and chemical purities were assessed by radio‐TLC and HPLC and found to be 98%. The average time of synthesis including formulation was 60 minutes resulting in average specific activitie