The H -antagonists, metiamide and cimetidine were labelled 2 with deuterium and tritium in the 2-position of the imidazole ring by the uncatalyzed exchange reaction with deuterium and tritium oxide at 100°C. The sulfur-35 labelled metiamide was prepared by an exchange reaction with elemental sulfur-
Synthesis of [14C]imidazole ring labeled metiamide, cimetidine and impromidine
✍ Scribed by A. J. Villani; L. Petka; D. W. Blackburn; D. Saunders; G. R. White; J. Winster
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 364 KB
- Volume
- 27
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
The radiosynthesis of imidazole ring labeled [14c]metiamide, [1k]cimetidine and ["k]impromidine are described involving the reaction of the key common intexmediate 2-[[(4methyl-lH-[2-14C]imidazol-5-yl)methyl]thio]ethanamine @ w i t h methyl isothiocyanate, dimethyldithiocyanoiminocarbonate/methylamine and the novel dihydroknidazdiazepine 0, res ectively. The ring labeled precursor @ was prepared in five steps from potassium mCi/mmol.
[ 1 B Clcyanide in an overall radiochemical yield of 63%, and having a specific activity of 9.3
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