Cefclidin (E1040), a new injectable cephalosporin with potent antipseudomonal activity, was synthesized labelled with carbon‐14, starting from bromo[1‐14C]acetic acid according to the method illustrated in Scheme 1, 2. [14C] Cefclidin, having a specific activity of 3.43 MBq/mg (water content 15.3%, which was based on water content of non labelled compound prepared by the same procedure), was obtained in 2% overall radiochemical yield, with a radiochemical purity of more than 99.1%.
Synthesis of (6R,7R)-7-[2-(5-amino4-carboxylate hydrochloride (IV) was acylated with the above acid chloride using the PC15 method, to afford the title compound (V); [14C]E1040, having a specific activity of 3.74 MBq/mg (as its anhydride) , was obtaind in 47% overall radiochemical yield, with a radiochemical purity of more than 98.1%.
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