Abstract: | Silymarin, the seed extract of milk thistle plant, Silybum marianum, has been used traditionally for the treatment of liver diseases and bile duct infection. Silybin 1 is the main bioactive components of silymarin, consisting a pair of diastereomers: Silybin A and Silybin B. In this article, we report the preparation of tritium‐labeled Silybin, which was accomplished by protection of Silybin as tritylated compound 2 and followed by oxidation of the primary alcohol to its corresponding aldehyde 3 . Subsequent reduction with NaB3H]4 and deprotection of the trityl group provided the tritium‐labeled Silybin 4 . Copyright © 2006 John Wiley & Sons, Ltd. |