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[11C]cyanogen bromide in the synthesis of 1,3-di(2-tolyl)-[11C]guanidine

✍ Scribed by Göran Westerberg; Wiebke Kärger; Hirotaka Onoe; Bengt Långström

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
253 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The title compound was ^11^C‐labelled in a one‐pot procedure using [^11^C]cyanogen bromide as the key intermediate. Synthesis time was 31–33 min counted from the end of bombardment, affording 1,3‐di(2‐tolyl)‐[^11^C]guanidine (6) in 87 % decay‐corrected radiochemical yield counted from [^11^C]cyanogen bromide. The specific radioactivity of the product at the end of synthesis was 118 GBq μmol^−1^ (3.2 Ci μmol^−1^). Autoradiographic studies on slide‐mounted rat brain sections showed specific binding of guanidine (6), but when injected intravenously into Rhesus monkey, brain uptake was very low, indicating that the 1,3‐di(2‐tolyl)‐[^11^C]guanidine did not cross the blood‐brain barrier.

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