SYNTHESIS OF [H-3] NALTRINDOLE
SYNTHESIS OF [H-3] NALTRINDOLE
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DOI：
10.1002/jlcr.2580310506
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发表时间：
1992-05-01
影响因子：
1.8
通讯作者：
PITZELE, BS
中科院分区：
文献类型：
--
作者：
DORN, CR;MARKOS, CS;PITZELE, BS
制备[H-3]纳曲吲哚（[H-3] 1）用作δ阿片受体的选择性放射性标记配体。由纳洛酮和2，4-二溴苯肼的Fischer吲哚合成产生二溴化物前体2，其用无载体氚气催化脱卤，以45.8%的产率在39.5 Ci/mmol的比活度下得到[H-3] 1。
[H-3]Naltrindole ([H-3] 1) was prepared for use as a selective radiolabeled ligand for delta opioid receptors. The Fischer indole synthesis from naltrexone and 2,4-dibromophenylhydrazine produced dibromide precursor 2, which was catalytically dehalogenated with carrier free tritium gas to afford [H-3] 1 in 45.8% yield at a specific activity of 39.5 Ci/mmol.