A simple synthesis of [11C]dihydrotetrabenazine (DTBZ).
[11C]Dihydrotetrabenazine (2-hydroxy-3-isobutyl-9-[11C]methoxy-10 -methoxy-1,2,3,4,6,7,- hexahydro-11bH-bezo[alpha]-quinolizine) ([11C]DTBZ) was synthesized by reacting the 9-hydroxy precursor in DMSO with gas-phase [11C]methyl iodide on a column of alumina impregnated with KOH. The reaction was instantaneous at room temperature. This column was then connected to the inlet of a short column containing basic alumina. Elution with cyclohexane removed radioactive contaminants. The radioactive product was then eluted with a few milliliters ether containing 1% ethanol. The [11C]DTBZ was obtained in isolated yields of > 200 mCi and specific activities > 1600 Ci/mmol.
Jewett
D M
DM
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109-0552, USA.
Kilbourn
M R
MR
Lee
L C
LC
D002250:Carbon Radioisotopes; D006847:Hydrocarbons, Iodinated; D007202:Indicators and Reagents; D007553:Isotope Labeling / Q000379:methods; D015394:Molecular Structure; D013747:Tetrabenazine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification
D002250:Carbon Radioisotopes; D006847:Hydrocarbons, Iodinated; D007202:Indicators and Reagents; C032811:dihydrotetrabenazine; C014055:methyl iodide; D013747:Tetrabenazine