Abstract: 6,7-diacetoxylbaicalein has been synthesized in 67.7% yield by the CH3COOK/Py catalyzed direct acetylation of baicalin, the main active component of Chinese herb Scutellaria baicalensis Georgi, with acetic anhydride at reflux, the monoacetylated derivative 6-acetoxyl baicalein or the mono-O-methylated derivative 6-acetoxy-7-methoxylbaicalein has been prepared in excellent yields from 6,7-diacetoxylbaicalein through the high selective hydrolysis reaction in the presence of K2CO3/acetone-H2O or methoxylation reaction at the C-7 position with Me2SO4 .

Key words: baicalin, 6,7-diacetoxylbaicalein, selective hydrolysis, methoxylation