The invention provides a novel method for synthesizing a 9-O-
aryl substituted
berberine derivative 5 and a 9-O-phenyl bridged
berberine dimer 7. The method comprises the steps: removing methyl of
a site 9 from
berberine 1, which serves as a
raw material, so as to obtain berberrubine 2, and subjecting the berberrubine 2 to
protonation and reduction, so as to prepare tetrahydro berberrubine 3; subjecting the tetrahydro berberrubine 3 and iodo
aromatic hydrocarbon to a C-O cross-
coupling reaction under
nitrogen protection so as to obtain a product 4, and then, carrying out oxidation, so as to obtain the target 9-O-
aryl substituted berberine derivative 5;
coupling the tetrahydro berberrubine 3 and 4o, and carrying out oxidation, thereby obtaining the berberine
dimer 7. The berberine derivatives synthesized by the method have the advantages of good
fat solubility, simple preparation method, high yield and the like. Discovered by in-vitro experiments, this kind of berberine derivatives havea relatively good inhibiting action on
staphylococcus aureus, thereby having a potential application value in the field of antibacterial drugs.