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Routine synthesis of N-[11C-methyl]scopolamine by phosphite mediated reductive methylation with [11C]formaldehyde

✍ Scribed by G.Keith Mulholland; Douglas M. Jewett; Steven A. Toorongian

Book ID
103920098
Publisher
Elsevier Science
Year
1988
Weight
608 KB
Volume
39
Category
Article
ISSN
0883-2889

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✦ Synopsis

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 7580Β°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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