Reductive N-alkylation of secondary amines with [2-11C]acetone
โ 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
- DOI
- 10.1002/jlcr.740
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โฆ Synopsis
Abstract
The development of a labeling method for secondary amines with [2โ^11^C]acetone is described since the R~2~Nโisopropyl 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]1โisopropylโ4โphenylpiperazine ([^11^C]iPPP) was synthesized from [2โ^11^C]acetone and 1โphenylpiperazine in a decayโcorrected radiochemical yield of 72%. The overall synthesis time, from EOB to HPLC analysis of [^11^C]iPPP, was 20 min. Specific activity was 142โ208 GBq/ฮผmol at the end of synthesis. Copyright ยฉ 2003 John Wiley & Sons, Ltd.
๐ SIMILAR VOLUMES
The reactions of 1,2-dichloroethane with 2-(ethylamino)ethanol or diethylamine have been investigated in several solvents from 51 to 80ยฐC. A reaction mechanism has been proposed where 1,2-dichloroethane reacts with the secondary amines in both bimolecular substitution (SN 2) and elimination (E2) rea
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