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Citation: JIANG Ming-Zhong, LEI Ze, MU Xiao-Yun, FU Zheng-Qi, WEN Xiao-Jiang, KONG Lan-Fen, ZHU Hong-You. One-step Synthesis,Selective Hydrolysis and Methoxylation of 6,7-Diacetoxylbaicalein[J]. Chinese Journal of Applied Chemistry, ;2009, 26(7): 845-847. shu

One-step Synthesis,Selective Hydrolysis and Methoxylation of 6,7-Diacetoxylbaicalein

1.
a Key Laboratory of Medicinal Chemistry for Natural Resource of Ministry of Education, Yunnan University, Kunming 650091;
2.
b Yunnan Police Officer Academy, Kunming;
3.
c Yunnan University Medical Development Co., Ltd, Kunming 650222

Corresponding author: ZHU Hong-You,
Received Date: 16 July 2008
Available Online: 15 October 2008
Fund Project: 云南省自然科学基金(2003C009M)资助项目 (2003C009M)

6,7-Diacetoxylbaicalein was synthesized in a yield of 67.6% by direct acetylation of baicalin,the main active component of a traditional Chinese herb Scutellaria baicalensis Georgi,with acetic anhydride catalyzd using CH₃COOK/Py under reflux.The monoacetylated derivative 6-acetoxyl baicalein or mono-O-methylated derivative 6-acetoxy-7-methoxylbaicalein was prepared in an excellent yield from 6,7-diacetoxylbaicalein via a high selective hydrolysis reaction in the presence of K₂CO₃/acetone-H₂O or a methoxylation reaction at the C-7 position with Me₂SO₄,respectively.
- baicalin,
- diacetoxylbaicalein,
- selective hydrolysis,
- methoxylation
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