Molecules 2012-01-01

Simple, rapid and reliable preparation of [¹¹C]-(+)-α-DTBZ of high quality for routine applications.

Jinming Zhang, Xiaojun Zhang, Yungang Li, Jiahe Tian

Index: Molecules 17(6) , 6697-704, (2012)

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Abstract

[¹¹C]-(+)-α-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]-(+)-α-DTBZ for routine applications. [¹¹C]-(+)-α-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/μmol. Time elapsed was less than 20 min from end of bombardment to release of the product for quality control.