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Synthesis of radiocarbon labelled lidocaine (α‐diethylaminoacet‐[1‐ 14 C] ‐2′, 6′ ‐dimethylanilide)
Author(s) -
Mezö,
Teplán
Publication year - 1972
Publication title -
journal of labelled compounds
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0022-2135
DOI - 10.1002/jlcr.2590080302
Subject(s) - chemistry , diethylamine , yield (engineering) , chromatography , bromide , lidocaine , thin layer chromatography , aniline , sodium , nuclear chemistry , organic chemistry , anesthesia , materials science , medicine , metallurgy
Starting from sodium acetate‐1‐ 14 C, acetyl‐1‐ 14 C bromide was prepared and from this bromacetyl‐1‐ 14 C bromide. The latter was used to acylate 2, 6‐dimetyl‐aniline to α‐bromoacet‐(1‐ 14 C) ‐2′, 6′ ‐xylidide, with an activity yield of 31%. The labelled lidocaine and its hydrochloride were prepared from this product by refluxing with diethylamine, with yields of 84.5% and 74.3%, respectively. The molar activity of the radiocarbon‐labelled Lidocaine was found to be 3.48 mCi/mmole; thin‐layer chromatography showed the product to be homogeneous.