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Molecules 2012, 17(6), 6697-6704;

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

Department of Nuclear Medicine, the PLA General Hospital, Beijing 100853, China
Authors to whom correspondence should be addressed.
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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[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. View Full-Text
Keywords: [11C]-(+)-a-DTBZ; VMAT2; position emission tomography; automated synthesis [11C]-(+)-a-DTBZ; VMAT2; position emission tomography; automated synthesis

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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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