Abstract:
The main crystalline princiiple "Baicalein" from the root of the Chinese drug Huang-Chin (
Scutellaria baicalensis Georg.) of Labiatae has been proved to be effective in lowering blood pressure without any toxic effect, even when large doses are administered as shown by pharmacological and clinical tests The method for extracting, Baicalin has been improved, and as much as twothirds of the time required by the old procedure (Shibata et aL Acta Phytochim. (1922-23) I, 105) were saved by using the improved method. The maximum yield of the improved method could be as high as 5.4 per cent. A monomethyl ether of Baicalin was obtained by using the ordinary amount of diazomethane for methylation while a dimethyl ether was formed with an excess of the reagent. The following six derivatives have been prepared and all of them are considered as new compotmds. 1) 6-Methyl ether Baicalein methyl ester C
23H
22O
11, m.p. 218-220℃. 2) 5,6-Dimethyl ether Baicalein methyl ester C
24H
24H
2O, m.p. 198℃. 3) 6-Methyl ether Baicalein methyl ester tetra-acetate C
23H
18O
11 (COCH
3)
4,m.p. 190℃. 4) 5,6 Dimethyl ether Baicalein methyl ester tri-acetate C
24H
21O
11 (COCH
3)
3,m.p. 220℃. 5) 5,6-Dimethyl ether Baicalein C
17H
14O
5, m.p. 209--208℃. 6) 5,6-Dimethyl ether-7-acetyl Baioalein C
19H
16O
6, m.p. 156--158℃. (m.p. are uncorrected)