Jewett D M, Kilbourn M R, Lee L C
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109-0552, USA.
Nucl Med Biol. 1997 Feb;24(2):197-9. doi: 10.1016/s0969-8051(96)00213-2.
[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.
[11C]二氢丁苯那嗪（2-羟基-3-异丁基-9-[11C]甲氧基-10-甲氧基-1,2,3,4,6,7-六氢-11bH-苯并[α]喹嗪）（[11C]DTBZ）通过使二甲基亚砜中的9-羟基前体与气相[11C]碘甲烷在浸渍有氢氧化钾的氧化铝柱上反应来合成。该反应在室温下瞬间完成。然后将此柱连接到装有碱性氧化铝的短柱的入口。用环己烷洗脱可除去放射性污染物。然后用几毫升含1%乙醇的乙醚洗脱放射性产物。得到的[11C]DTBZ的分离产率>200毫居里，比活度>1600居里/毫摩尔。
