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Molecules 2012, 17(6), 6697-6704; doi:10.3390/molecules17066697
Article

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

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Received: 27 April 2012 / Revised: 28 April 2012 / Accepted: 30 April 2012 / Published: 1 June 2012
(This article belongs to the Section Medicinal Chemistry)
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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: [11C]-(+)-a-DTBZ; VMAT2; position emission tomography; automated synthesis [11C]-(+)-a-DTBZ; VMAT2; position emission tomography; automated synthesis
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Zhang, J.; Zhang, X.; Li, Y.; Tian, J. Simple, Rapid and Reliable Preparation of [11C]-(+)-a-DTBZ of High Quality for Routine Applications. Molecules 2012, 17, 6697-6704.

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