Abstract

The [ 11C]carbonation of simple Grignard reagents (RMgX, R = Et, Pr, cyclo-Bu; X = Br) with cyclotron-produced [ 11C]carbon dioxide followed by direct treatment of the 11C adducts with phthaloyl dichloride and 2,6-di-t-butylpyridine affords [1- 11C]acid chlorides in useful radiochemical yields (> 10–30%, decay-corrected from 11CO 2), as assessed by HPLC and TLC of the labelled amides formed by reaction with 1,2,3,4-tetrahydroisoquinoline. With suitable precuations these [1- 11C]acid chlorides can be isolated at high specific activity within 15 min from radionuclide production as labelling agents for potential radiopharmaceuticals for PET. The preparation of [1- 11C]benzoyl chloride without isolation has also been demonstrated.

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