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Synthesis of 1-([1-14C] cyclohexyloxycarbonyloxy) ethyl 7β-[2-(2-aminothiazol-4-YL)acetamido]-3-[[[1-(2-dimethylamino-ethyl)-1H-tetrazol-5-YL]thio]methyl]ceph-3-EM-4-carboxylate dihydrochloride ([14C]SCE-2174)

✍ Scribed by Masazumi Watanabe; Norio Tada; Masayuki Imanishi; Masayoshi Yamaoka

Publisher
John Wiley and Sons
Year
1988
Tongue
French
Weight
160 KB
Volume
25
Category
Article
ISSN
0022-2135

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✦ Synopsis

1-(Cyclohexyloxycarbony1oxy)ethyl 7P-[2-(2-aminothiazol-~-yl~acetamido]-3-[[[1-(2-dimethylaminoethyl~-1H-tetrazol-~-yl]thio]methyl]ceph-3-em-4-carboxylate dihydrochloride (SCE-2174), a new orally active cephalos orin, was labeled with carbon-14 starting from [l-lgC] c yc lohexanol (1) . 1 -Chloroe thy1 [ 1 -14C] c yc lohexyl carbonate (1) obtained by acylation of 1 with l-chloroethyl chloroformate (2) was converted to iodide (5) which was condensed with the potassium salt of Cefotiam (5). [14C]SCE-2174, having a specific activity of 672

MEq/mmol, was obtained in 13% overall radiochemical yield and had a radiochemical purity of 92%.

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