氚标记阿片受体配基N-烯丙基-6,14-内乙烯撑基-7α-二(β-氯乙基)胺甲基四氢奥利文的制备

PREPARATION OF TRITIUM NARCOTIC LIGAND N-ALLY-7α-BIS (β-CHLOROETHYL) AMINOMETHYL-6, 14-ENDOETHENOTETRAHYDROORIPAVINE

N-烯丙基-6,14-内乙烯撑基-7α-二(β-氯乙基)胺甲基四氢奥利文(简称A-α-CMO)是新设计合成的阿片受体不可逆配基。本文以蒂巴因为原料通过八步有机合成反应制得A-α-CMO的炔丙基前体(Ⅵ),然后通氚气部分还原反应制备~3H-A-α-CMO,经氚核磁共振测定,氚标记位置在N-烯丙基上。纯化后,~3H-A-α-CMO的放化纯度为96％以上,放射性比度为1.332TBq/mmol,初步放射受体分析显示,特异结合与非特异结合之比为5.6:1。

N-ally-7α-bis (β-chlcoroethyl) aminomethyl-61,4-endoethenotetrahydrooripa-vine(A-α-CMO)is an irreversible narcotic ligand. The N-propagyl precursor of A-α-CMO was first designed and synthesized through eight organic reactions, then the precursor was reduced with tritium gas in the presence of a catalyst. The position of tritium labelling in N-ally was determined by tritium-NMR. After purification, the radiochemical purity of 3H-A-α-CMO was above 96% and specific activity was 1.332 TBq/mmol. RRA showed that the ratio of specific binding to non-specific binding was 5.6:1.