氘标记川芎嗪的合成

SYNTHESIS OF DEUTERIUM-LABELED TETRAMETHYLPYRAZINE

为深入研究川芎嗪的代谢,制备了它的氘标记物。以丁酮和氘水在无水K_2CO_3存在下经多次交换反应得到氘代丁酮,后者和亚硝酸乙酯反应生成肟经Zn粉还原及脱水环缩合制成氘标记川芎嗪。GCMS测定结果表明标记产物具特征性的同位素峰簇,氘标记丰度高,能满足药物代谢研究之所需。

Tetramethylpyrazine(TMP) ,an active principle isolated from the traditional Chinese herb, Ligusticum Wallichii Franch,has been widely used in the treatment of patients with cerebral ischemic diseases in China, In order to investigate its metabolism, we synthesized deuterium-labeled TMP from deuterated butanone which was obtained by the exchange of butanone with deuterium oxide in the presence of potassium carbonate. The resulting deuterium-labeled TMP exhibited characteristic isotopic clus ters in its CI ma...