Sodium 7~-Cyanomethylthioacetamido-7a-14C-methoxy- 3-[ (1-methyl-1H-tetrazol-5-yl) thiomethyl) -3-cephem-4-carboxylate (CS-1170), a new cephamycin derivative was prepared for metabolic studies, The key reaction involves the methoxylation o f t'he diphenylmethyl 7-( 3 , 4 -d i -~-b u t y l -4 -o x 0
Synthesis of 14C-labeled 7α-methoxycephalosporin derivative (14C-cefotetan)
✍ Scribed by Kazuharu Tamazawa; Hideki Arima
- Publisher
- John Wiley and Sons
- Year
- 1982
- Tongue
- French
- Weight
- 295 KB
- Volume
- 19
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
[Caboxamido‐^14^C]Cefotetan, 7α‐[4‐(carbamoyl carboxymethylene)‐1,3‐dithietan‐2‐yl] [^14^C]carboxamido‐7α‐methoxy‐3‐(1‐methyl‐1H‐tetrazol‐5‐yl)thiomethyl‐y1)thiomethyl‐3‐cephem‐4‐carboxylic acid (IX), a new cephamycin derivative, was synthesized from bromo[1‐^14^C]acetic acid for metabolic studies. The results of duplicate preparation of ^14^C‐Cefotetan are described. In the second synthesis, a new improved method was adopted. The overall radiochemical yields were 21.5 % and 26.7 %, at specific activity of 44.5 μCi/mg and 53.3 μCi/mg respectively.
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