氘标色氨酸和氘标川芎哚的合成研究

Deuteration of tryptophan and perlolyrine

以色氨酸和氘水及色氨酸和氯化氘两种交换反应合成氘标色氨酸，其产率分别为95％和92％，氘标总丰度分别为96．2％和98．5％。以色氨酸和氘水反应合成的氘标色氨酸为原料，经环化、氧化脱羧及水解等反应合成氘标川芎哚，产率为11．6％，氘标总丰度约为90％。结果表明，合成的氘标川芎哚满足药物代谢研究的需要。

Deuterated tryptophan was prepared by simple exchange reactions in DC1 orD2O solution. The yield and abundance of deuterated tryptophan obtained from usingDC1 as the deuterium solute was 92% and 98.5% respectively, whereas that by usingD2O was 95% and 96.2% respectively. Deuterated perlolyrine was synthesizedstarting from deuterated tryptophan via acid-catalyzed ring-closure, aromatisationand hydrolysis, with a yield of 11.6% and abundance of about 95%. The labelledperlolyrine was suitable for studying drug metabolism.