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Synthesis of [11C]atipamezole, a potential PET ligand for the α2-adrenergic receptor in the brain

✍ Scribed by D. Roeda; H.T. Sipilä; Y. Bramoullé; J. D. Enas; F. Vaufrey; F. Dollé; C. Crouzel

Publisher
John Wiley and Sons
Year
2001
Tongue
French
Weight
119 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The α~2~‐adrenergic receptor antagonist atipamezole has been labelled with carbon‐11 using [^11^C]formaldehyde and 2‐ethyl‐2‐oxoacetylindane. Various routes are proposed for the synthesis of the latter: oxidation of 2‐acetyl‐2‐ethylindane, hydrolysis of 2‐diethoxy‐2‐indane and oxidation of 2‐diazoacetyl‐2‐ethylindane. The average radiochemical yield of [^11^C]atipamezole was 24% based on [^11^C]formaldehyde, and the synthesis time, including HPLC purification and formulation, was 45 min. Copyright © 2002 John Wiley & Sons, Ltd.

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