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Canna~Fangled Abstracts

Synthesis of carbon-11-labeled aminoalkylindole derivatives as new candidates of cannabinoid receptor radioligands for PET imaging of alcohol abuse.

By December 4, 2014No Comments
2014 Dec 15;24(24):5581-6. doi: 10.1016/j.bmcl.2014.10.097. Epub 2014 Nov 6.

pm1Synthesis of carbon-11-labeled aminoalkylindole derivatives as new candidates of cannabinoidreceptor radioligands for PET imaging of alcohol abuse.

Abstract

Carbon-11-labeled aminoalkylindole derivatives (1-butyl-7-[(11)C]methoxy-1H-indol-3-yl)(naphthalene-1-yl)methanone ([(11)C]3), 1-butyl-7-[(11)C]methoxy-3-(naphthalene-1-ylmethyl)-1H-indole ([(11)C]5), and 1-butyl-7-[(11)C]methoxy-3-(naphthalene-2-yl)-1H-indole ([(11)C]8) were prepared by O-[(11)C]methylation of their corresponding precursors with [(11)C]CH3OTf under basic condition (2N NaOH) and isolated by a simplified solid-phase extraction (SPE) method in 50-60% radiochemical yields based on [(11)C]CO2 and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 23min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 185-555GBq/μmol.
Copyright © 2014 Elsevier Ltd. All rights reserved.

KEYWORDS:

Alcohol abuse; Cannabinoid receptor; Carbon-11-labeled aminoalkylindole derivatives; Positron emission tomography (PET); Radiosynthesis

PMID:

 

25466179

 

[PubMed – in process]
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