Routine synthesis of N-[11C-methyl]scopolamine by phosphite mediated reductive methylation with [11C]formaldehyde
1988; Pergamon Press; Volume: 39; Issue: 5 Linguagem: Inglês
10.1016/0883-2889(88)90065-2
ISSN1878-1128
AutoresG. Keith Mulholland, Douglas M. Jewett, Steven A. Toorongian,
Tópico(s)Pharmacological Effects and Toxicity Studies
ResumoA synthesis of [11C]scopolamine capable of clinical delivery of this agent in high specific activity is described. The precursor [11C]formaldehyde was produced by catalytic oxidation of [11C]CH3OH over metallic silver and was used to N-11C-methylate norscopolamine using aqueous neutral potassium phosphite as the reducing agent. The labeling reaction was complete after 5 min at 75–80°C and the [11C]scopolamine (99% radiochemical purity) was isolated by preparative HPLC. Total synthesis time is less than 45 min. Decay corrected radiochemical yields from [11C]CO2 are presently 20–43%.
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