Improved synthesis of [11C]SA4503, [11C]MPDX and [11C]TMSX by use of [11C]methyl triflate.

Kazunori Kawamura, Kiichi Ishiwata

Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Tokyo, Japan. kawamura@pet.tmig.or.jp

Annals of nuclear medicine 2004 Apr

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Recently we have clinically used three new radioligands, [11C]SA4503, [11C]MPDX, and [11C]TMSX, for mapping sigma1, adenosine A1, and adenosine A2A receptors, respectively, in the human brain by positron emission tomography. These radioligands are synthesized by methylation of the respective demethyl precursor with [11C]methyl iodide. Here we demonstrate the improved syntheses of these compounds by use of [11C]methyl triflate, a highly reactive alternative to [11C]methyl iodide.

Citation

Kazunori Kawamura, Kiichi Ishiwata. Improved synthesis of [11C]SA4503, [11C]MPDX and [11C]TMSX by use of [11C]methyl triflate. Annals of nuclear medicine. 2004 Apr;18(2):165-8