Abstract

Abstract1‐(Cyclohexyloxycarbonyloxy)ethyl 7β‐[2‐(2‐amino‐thiazol‐4‐yl)acetamido]‐3‐[[[1‐(2‐dimethylaminoethyl)‐1H‐tetrazol‐5‐yl]thio]methyl]ceph‐3‐em‐4‐carboxylate dihydrochloride (SCE‐2174), a new orally active cephalosporin, was labeled with carbon‐14 starting from [1‐14C]cyclohexanol (1). 1‐Chloroethyl [1‐14C]cyclohexyl carbonate (3) obtained by acylation of 1 with 1‐chloroethyl chloroformate (2) was converted to iodide (4) which was condensed with the potassium salt of Cefotiam (5). [14C]SCE‐2174, having a specific activity of 672 MBq/mmol, was obtained in 13% overall radiochemical yield and had a radiochemical purity of 92%.

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