[11C]octopamine synthesis using [11C]cyanide: chemical and enzymatic approaches for the [11C]cyanohydrin synthesis.
[11C]-p- and m-octopamine hydrochloride were synthesized from [11C]HCN in a two-step sequence. Chemical and enzymatic approaches were used for the formation of the [11C]cyanohydrin intermediates as the key step. Isolated radiochemical yields of 0.7-2.3% at the end-of-synthesis were obtained with an overall preparation time of 40-60 min. The enantiomeric purity of the [11C]-p-octopamine obtained through the enzymatic process was 92% e.e. in the (S)-enantiomer, whereas that of the [11C]-m-octopamine was 42% e.e. in the (R)-enantiomer, as determined by HPLC without any derivatization.
Maeda
M
M
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Koga
Y
Y
Fukumura
T
T
Kojima
M
M
D002250:Carbon Radioisotopes; D007553:Isotope Labeling; D009570:Nitriles / Q000138:chemical synthesis*; D009655:Octopamine / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D009570:Nitriles; D009655:Octopamine; C005310:norfenefrine