Simple, Rapid and Reliable Preparation of [<sup>11</sup>C]-(+)-a-DTBZ of High Quality for Routine Applications

Abstract

[¹¹C]-(+)-a-DTBZ has been used as a marker of dopaminergic terminal densities in human striatum and expressed in islet beta cells in the pancreas. We aimed to establish a fully automated and simple procedure for the synthesis of [¹¹C]-(+)-a-DTBZ for routine applications. [¹¹C]-(+)-a-DTBZ was synthesized from a 9-hydroxy precursor in acetone and potassium hydroxide with [¹¹C]-methyl triflate and was purified by solid phase extraction using a Vac tC-18 cartridge. Radiochemical yields based on [¹¹C]-methyl triflate (corrected for decay) were 82.3% ± 3.6%, with a specific radioactivity of 60 GBq/mmol. Time elapsed was less than 20 min from end of bombardment to release of the product for quality control.

Keywords

• [<sup>11</sup>C]-(+)-a-DTBZ
• VMAT2
• position emission tomography
• automated synthesis