[2-^(15)N]-川芎哚的合成研究

Synthesis of [2-^(15)N] -perlolyrine

以糠醛为起始原料，经乙酰化、甲酰化后，与中间原料[α－15N]－dl－色氨酸发生氧化（芳香化）、脱羧、水解等反应生成[2－15N]－川芎哚。终产物经MS、UV、TLC等证实。产率为15．5％，15N的丰度为92％。结果表明，合成的[2－15N]－川芎哚符合药理实验要求。

The synthesis of [2-15N]-perlolyrine is described. Furfuryl alcohol was first acetylated and formacylated, and then reacted with [α -15N]-dl-tryptophan to form the ring-closed product, which was oxidated and hydrolyzed to give the final product. The product was confirmed by MS, UV and TLC. Its yield from [α -15N]-dl-tryptophan was 15.5%, and the abundance of 15N was 92%. The synthetic [2- 15N]-perlolyrine is therefore suitable for pharmacologic experiments.