Routine Synthesis of N-[“C-Methyl]Scopolamine by Phosphite Mediated Reductive Methylation
نویسندگان
چکیده
A synthesis of [“Qcopolamine capable of clinical delivery of this agent in high specific activity is described. The precursor [“Clformaldehyde was produced by catalytic oxidation of [“C]CH,OH over metallic silver and was used to N-“C-methylate norscopolamine using aqueous neutral potassium phosphite as the reducing agent. The labeling reaction was complete after 5min at 7580°C and the [“Clscopolamine (99% radiochemical purity) was isolated by preparative HPLC. Total synthesis time is less than 45 min. Decay corrected radiochemical yields from [“C]C02 are presently 2@43%.
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