Synthesis of high specific activity [ethyl‐1,2‐3H]‐labeled chlorpyrifos oxon and diazoxon
Synthesis of high specific activity [ethyl‐1,2‐3H]‐labeled chlorpyrifos oxon and diazoxon
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高比活性[乙基-1,2-3H]标记毒死蜱氧磷和重氮磷的合成
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发表时间：
2000
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通讯作者：
J. Casida
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作者：
Nanjing Zhang;H. Morimoto;P. Williams;J. Casida
通过在 Pd/C 上催化氚化相应的单乙烯基类似物，合成了比活度分别为 79 和 58 Ci/mmol 的[乙基-1,2-3H]毒死蜱和[乙基-1,2-3H]重氮酮。提供的直接证据表明，高比活性是由双键饱和之前末端乙烯基质子的同位素交换产生的。该放射合成程序适用于许多商业 O-O-二乙基硫代磷酸酯农药的毒理学上重要的氧磷代谢物。
[Ethyl-1,2-3H] Chlorpyrifos oxon and [ethyl-1,2-3H] diazoxon were synthesized at a specific activity of 79 and 58 Ci/mmol, respectively, by catalytic tritiation of the corresponding monovinyl analogs over Pd/C. Direct evidence is provided that the high specific activity results from isotope exchange of the terminal vinylic protons prior to saturation of the double bond. This radiosynthesis procedure is applicable to the toxicologically-important oxon metabolites of many commercial O-O-diethyl phosphorothioate pesticides.