An efficient and expedient method for the synthesis of 11C-labeled a-aminoisobutyric acid: A tumor imaging agent potentially useful for cancer diagnosis

  • Kato Koichi
  • Tsuji Atsushi
  • Saga Tsuneo
  • Zhang Ming-Rong
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Publication date
April 2011
Journal
Bioorganic & Medicinal Chemistry Letters

Abstract

We describe the synthesis of 11C-labeled a-aminoisobutyric acid 2 from iodo[11C]methane and methyl N-(diphenylmethylen)-D,L-alaniate (5). The tetrabutylammonium fluoride (TBAF)-promoted a-[11C]methylation of sterically hindered analog 5 was a key step in our synthesis process. Total radiochemical conversion of 2 was high and a remote-controlled synthesis was carried out. A comparative tumor positron emission tomography (PET) imaging study using the same model mouse showed higher uptake of 2 than with 11C-labeled methionine and [18F] fluorodeoxyglucose (FDG)

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