High reactivity of [11C]CH3I with thiol group in the synthesis of C-11 labeled radiopharmaceuticals.
High reactivity of [11C]-methyl iodide ([11C]CH3I) with the thiol group was demonstrated with cysteamine and other compounds containing a thiol and another functional groups in each structure. The methylation of the thiol group in cysteamine with [11C]CH3I was very rapid at 0 degree C with no catalyst, and gave a high radiochemical yield and purity without any detectable by-product. Moreover, this reaction was not disturbed by the other functional groups, such as -NH2, -OH and -COOH in the same structure. This S-methylation reaction is very useful for producing a new radiopharmaceutical labeled with the short lived positron emitting nuclide C-11.
Magata
Y
Y
Department of Nuclear Medicine, Faculty of Medicine, Kyoto University, Japan.
Saji
H
H
Tokui
T
T
Ohmomo
Y
Y
Yamada
Y
Y
Hirata
M
M
Konishi
J
J
Yokoyama
A
A
D002250:Carbon Radioisotopes; D006847:Hydrocarbons, Iodinated / Q000737:chemistry*; D007553:Isotope Labeling; D013438:Sulfhydryl Compounds / Q000737:chemistry*
D002250:Carbon Radioisotopes; D006847:Hydrocarbons, Iodinated; D013438:Sulfhydryl Compounds; C014055:methyl iodide