Journal of Medicinal Materials, 2023, Vol. 28, No. 6 (pp. 357 - 360)
THE PREPARATION OF DIOSMIN FROM HESPERIDIN VIA THREE STEPS
Nguyen Thi Ha1,*, Hoang Thi Ngoc Anh2, Nguyen Minh Khoi1, Pham Hai Long1, Nguyen Thi Thuy Loan3
1National Institute of Medicinal Materials, Hanoi, Vietnam; 2Dai Nam University, Vietnam;
3Edupharm International Joint Stock Company, Hanoi, Vietnam
*Corresponding author: nguyenthihavdl2005@gmail.com
(Received May 19th, 2023)
Summary
The Preparation of Diosmin from Hesperidin via three Steps
Diosmin (diosmetin 7-O-rutinoside), the natural flavonoids mainly found in Citrus fruits, is used for the treatment of hemorrhoids or chronic venous diseases. In this report, we studied the semi-synthesis of diosmin from hesperidin through three steps. In the first step, hydroxyl functional groups of hesperidin were protected, then acetyl-hesperidin (1) was continuously oxidized on the C-3 position, diosmin was obtained by deacetylation reaction. The structure of compounds 1-3 was confirmed by 1D, 2D-NMR, and LC-ESI MS spectrum.
Keywords: Diosmin, Diosmetin 7-O-rutinoside, Hesperidin, Oxidation, Deacetylated.
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