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.
Highlights
Ischemic cerebrovascular disease is a frequently-occurring disease, and it has been one of the leading causes of death and disability worldwide that seriously endangers human health [1].Traditional Chinese medicines have been used clinically for thousands years and can be regarded as potential rich sources for drug lead compound discovery
6-O-methyl-scutellarein (3) (Figure 1), which is one of the circulating metabolite of scutellarin in vivo, might be responsible for the therapeutic effects of scutellarin (1). This interesting scutellarin metabolite (3) is not commercially available, as a result, synthetic methods for this metabolite will be very important for further study
With an aim to provide a solution to the material supply issue we recently reported a synthetic route to 6-O-methyl-scutellarein (3) (Figure 2) [14]
Summary
Hang Lin 1,2,3, Wei Zhang 1,2,3, Ze-Xi Dong 1,2,3, Ting Gu 1,2,3, Nian-Guang Li 1,2,3,*, Zhi-Hao Shi 4, Jun Kai 1,2,3, Cheng Qu 1,2,3, Guan-Xiong Shang 1,2,3, Yu-Ping Tang 1,2,3,*, Fang Fang 1,2,3, He-Min Li 1,2,3, Jian-Ping Yang 1,2,3 and Jin-Ao Duan 1,2,3. Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210023, Jiangsu, China
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