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

Int J Rad Appl Instrum A. 1988;39(5):373-9. doi: 10.1016/0883-2889(88)90065-2.

Abstract

A 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 degrees 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%.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Carbon Radioisotopes*
  • Formaldehyde
  • Humans
  • Isotope Labeling / methods
  • N-Methylscopolamine
  • Parasympatholytics / chemical synthesis*
  • Phosphites*
  • Phosphorous Acids
  • Potassium Compounds*
  • Receptors, Muscarinic
  • Scopolamine Derivatives / chemical synthesis*
  • Tomography, Emission-Computed

Substances

  • Carbon Radioisotopes
  • Parasympatholytics
  • Phosphites
  • Phosphorous Acids
  • Potassium Compounds
  • Receptors, Muscarinic
  • Scopolamine Derivatives
  • potassium phosphite
  • Formaldehyde
  • N-Methylscopolamine