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Carbon-14 labelling of selective H3 receptor antagonists

✍ Scribed by Steen K. Johansen

Publisher: John Wiley and Sons
Year: 2005
Tongue: French
Weight: 88 KB
Volume: 48
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1018

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✦ Synopsis

The fast and efficient carbon-14 labelling of the three potent H 3 antagonists NNC 38-1202, NNC 38-1384, and NNC 38-1401 is reported. The two-step synthetic sequence, which included a Knoevenagel reaction, provided the carbon-14-labelled compounds in 38-55% overall yield starting from [2-14 C]malonic acid. The compounds were all obtained in high radiochemical purity (>99%) and with high specific activity (55.8 mCi/mmol).

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