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Reductive N-alkylation of secondary amines with [2-11C]acetone

โœ Scribed by Margaretha van der Meij; Nicholas I. Carruthers; Jacobus D.M. Herscheid; Jill A. Jablonowski; Josee E. Leysen; Albert D. Windhorst


Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
116 KB
Volume
46
Category
Article
ISSN
0022-2135

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โœฆ Synopsis


Abstract

The development of a labeling method for secondary amines with [2โ€^11^C]acetone is described since the R~2~Nโ€isopropyl moiety is present in many biologically active compounds. The influence of a variety of parameters (e.g. reagents, solvents, temperature, and time) on the reaction outcome is discussed. Under the optimal reaction conditions, [^11^C]1โ€isopropylโ€4โ€phenylpiperazine ([^11^C]iPPP) was synthesized from [2โ€^11^C]acetone and 1โ€phenylpiperazine in a decayโ€corrected radiochemical yield of 72%. The overall synthesis time, from EOB to HPLC analysis of [^11^C]iPPP, was 20 min. Specific activity was 142โ€“208 GBq/ฮผmol at the end of synthesis. Copyright ยฉ 2003 John Wiley & Sons, Ltd.


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