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A New and Practical Synthetic Method for the Synthesis of 6-O-Methyl-scutellarein: One Metabolite of Scutellarin in Vivo
Authors:Hang Lin  Wei Zhang  Ze-Xi Dong  Ting Gu  Nian-Guang Li  Zhi-Hao Shi  Jun Kai  Cheng Qu  Guan-Xiong Shang  Yu-Ping Tang  Fang Fang  He-Min Li  Jian-Ping Yang  Jin-Ao Duan
Abstract: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.
Keywords:6-O-methyl-scutellarein  scutellarin  scutellarein  metabolite  synthesis
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