A New and Practical Synthetic Method for the Synthesis of 6-O-Methyl-scutellarein: One Metabolite of Scutellarin in Vivo

作者:Lin, Hang; Zhang, Wei; Dong, Ze-Xi; Gu, Ting; Li, Nian-Guang*; Shi, Zhi-Hao; Kai, Jun; Qu, Cheng; Shang, Guan-Xiong; Tang, Yu-Ping; Fang, Fang; Li, He-Min; Yang, Jian-Ping; Duan, Jin-Ao
来源:International Journal of Molecular Sciences, 2015, 16(4): 7587-7594.
DOI:10.3390/ijms16047587

摘要

Scutellarin (1) has been used for the treatment of angina pectoris, cerebral infarction and coronary heart disease with a large market share in China. Pharmacokinetic studies on scutellarin showed that scutellarin (1) is readily converted into its metabolites in vivo. In this paper, a new and practical synthetic method for the synthesis of 6-O-methyl-scutellarein (3) (one metabolite of scutellarin in vivo) is reported. The benzyl bromide was firstly used to selectively replace the acetyl group at C-7 in 7, and was then used to protect the hydroxy groups at C-4' in 10, 6-O-methyl-scutellarein (3) is obtained in high yield through these methods.