N-[11C]methyl-3,4-methylenedioxyamphetamine (Ecstasy) and 2-methyl-N-[11C]methyl-4,5-methylenedioxyamphetamine: Synthesis and biodistribution studies
作者： M. Patt , D. Gündisch , U. Wüllner , A. Blocher , K. -A. Kovar
DOI: 10.1007/BF02349410
关键词: Methylation 、 Radiochemistry 、 MDMA 、 Yield (chemistry) 、 Biodistribution 、 Stereochemistry 、 Ecstasy 、 Chemistry 、 Amphetamine
摘要: In order to evaluate the neurobiological mechanism causing psychogenic effects of methylenedioxy-derivatives amphetamine, carbon-11 labeled analogues 3,4-methylenedioxymethamphetamine (MDMA),2 and 2,N-dimethyl-4,5-methylenedioxyamphetamine (MADAM-6)4 were prepared for application in in-vivo PET studies by methylation 3,4-methylenedioxyamphetamine (MDA)1 2-methyl-4,5-methylenedioxyamphetamine3 with [11C]CH3I. The radiochemical yield was determined dependence on time, temperature amount precursor. best conditions a fast labeling reaction preparative scale found be time 10 min using 1 mg corresponding dimethyl-precursors1 or3, thus obtaining yields 60% (based produced [11C]CH3I). Biodistribution performed rats, high brain blood ratio 7.5 observed [11C]MDMA contrast 3.7 [11C]MADAM-6.
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