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Carbon‐14 labelling of selective H 3 receptor antagonists
Author(s) -
Johansen Steen K.
Publication year - 2005
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1018
Subject(s) - chemistry , labelling , malonic acid , knoevenagel condensation , yield (engineering) , carbon 14 , carbon fibers , stereochemistry , specific activity , organic chemistry , biochemistry , catalysis , algorithm , materials science , physics , quantum mechanics , composite number , computer science , metallurgy , enzyme
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). Copyright © 2005 John Wiley & Sons, Ltd.