Sinensetin is one of the polymethoxyflavones existed in citrus peels. The effective antioxidant, inhibitory effect of inflammation, anti-diabetic and anti-cancer activity of sinensetin has been revealed recently. However, the amount of sinensetin isolated from the nature source is extremely low relating to the needs for its in vivo and efficacy study. Herein we summarized the alternative routes, i.e. the organic synthesis of sinensetin and its associated derivatives to provide a complete but concise reference in the preparation of this class of compounds as an effective source for in-depth study of sinensetin and related molecules.
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