Synthesis of 11C-Labelled Symmetrical Ureas via the Rapid Incorporation of [11C]CO2 into Aliphatic and Aromatic Amines

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Abstract

An efficient method to radiolabel symmetrical [11C]ureas using 1,8-diazabicycloundec-7-ene (DBU) and cyclotron-produced [11C]CO2 has been developed. [11C]urea derivatives were obtained when aliphatic and aromatic amines were used with excellent radiochemical yields (RCYs) of over 70%. The mechanism of the reaction is proposed on the basis of control experiments. This simple and robust methodology provides a powerful tool to prepare 11C-labelled ureas previously inaccessible by existing methods and enable their utilisation for in vivo molecular imaging applications.

Original languageEnglish
Article numberst-2015-d0366-l
Pages (from-to)2257-2260
Number of pages4
JournalSYNLETT
Volume26
Issue number16
DOIs
Publication statusPublished - 2015

Keywords

  • carbon dioxide
  • carbon-11
  • DBU
  • Mitsunobu reaction
  • symmetrical urea

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