Kiesewetter D O, Finn R D, Rice K C, Monn J A
Department of Nuclear Medicine, Warren Grant Magnuson Clinical Center, National Institutes of Health, Bethesda, MD 20892.
Int J Rad Appl Instrum A. 1990;41(2):139-42. doi: 10.1016/0883-2889(90)90098-2.
The synthesis of C5 labeled (+-)-5-[11C]methyl-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten- 5,10-imine [(+-)-[11C]MK801] has been accomplished via alkylation of (+-)-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-5,10-imine-N-t- butylformamidine [(+-)-5-des-methyl MK801 formamidine). The 11C labeling is accomplished by reaction of the anion of (+-)-5-des-methyl MK801 formamidine, generated with s-butyllithium, and [11C]methyl iodide.
通过对(±)-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺-N-叔丁基甲脒[(±)-5-去甲基MK801甲脒]进行烷基化反应,已完成C5标记的(±)-5-[11C]甲基-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺[(±)-[11C]MK801]的合成。11C标记是通过用仲丁基锂生成的(±)-5-去甲基MK801甲脒的阴离子与[11C]碘甲烷反应来实现的。