2-~(15)N-川芎哚的全合成

    SYNTHESIS OF 2-~(15)N PERLOLYRINE FROM ~(15)N GLYCINE

    • 摘要: 为研究川芎哚在动物体内的代谢转化,以15N-甘氨酸为原料,铝镍合金作催化还原剂,首先合成[α-15N]-dl-色氨酸,进而合成[2-15N]-川芎哚。终产物经质谱(MS)、紫外光谱(UV)、薄层层析(TLC)等方法表征。总产率为7.3% ,15N 丰度为92% ,化学纯度为98% 。结果表明,合成的[2-15N]-川芎哚符合药理实验要求。

       

      Abstract: To study the metabolism of 2 15 N Perlolyrine in animals, α 15 N dl tryptophan and 2 15 N perlolyrine are designed and synthesized. α 15 N dl Tryptophan is first synthesized from 15 N glycine via many steps by the use of Al Ni alloy as a catalytic reduction agent, and then 2 15 N perlolyrine is synthesized from α 15 N dl tryptophan.The abundance of 15 N is determined by GC MS, the chemical purity is determined by TLC and the final product is confirmed by MS, UV and TLC. The overall yield of the final product is 7.3%, the abundance of 15 N is 92% and the chemical purity is 98%. The synthetic 2 15 N perlolyrine is suitable for pharmacological experiments.

       

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