Abstract
The fast and efficient carbon-14 labelling of the three potent H3 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 [2-14C]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.
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