Abstract:

Using baicalin, the main active component of a traditional Chinese herb Scutellaria baicalensis, and one of its derivative, 6,7-diacetoxylbaicalein, as precursors, a series of C₈-substituted and di or tri-O-methylated baicalein derivatives was synthesized in good yields by iodination, nitration, reductive amination and selective methoxylation or hydrolysis of 6,7-diacetoxylbaicalein. The structures of these producrs were characterized. They featured with a broad spectrum of biological activities, notably anti-oxidant.

Key words: baicalin, diacetoxylbaicalein, selective methoxylation, structural modification