Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371170 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
We describe the synthesis of 11C-labeled α-aminoisobutyric acid 2 from iodo[11C]methane and methyl N-(diphenylmethylen)-d,l-alaniate (5). The tetrabutylammonium fluoride (TBAF)-promoted α-[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).
Graphical abstractWe describe the synthesis of 11C-labeled α-aminoisobutyric acid 2 from iodo[11C]methane and methyl N-(diphenylmethylen)-d,l-alaniate (5). The tetrabutylammonium fluoride (TBAF)-promoted α-[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).Figure optionsDownload full-size imageDownload as PowerPoint slide