The invention discloses a synthetic method of a C1-
triazole oridonin derivative and an anti-tumor application of the C1-
triazole oridonin derivative. The invention provides a synthetic method of the C1-
triazole oridonin derivative, which comprises the following steps: carrying out four-step reaction to obtain an oridonin analogue containing an
azide group at the C1 site, and catalyzing by cuprous
iodide to obtain the C1-triazole oridonin derivative with the
azide group at the C1 site, thereby obtaining the C1-triazole oridonin derivative with the
azide group at the C1 site and the oridonin analogue with the azide group at the C1 site. According to the method,
alkyne compounds containing different
substituent groups react with C1-triazole oridonin to synthesize the C1-triazole oridonin derivative, the method is mild in condition and rapid in reaction, large-scale preparation of the C1-triazole oridonin derivative can be achieved, and the method is suitable for large-scale production of the C1-triazole oridonin derivative. Meanwhile, the C1-triazole oridonin derivative synthesized by the invention can be used for effectively inhibiting the
proliferation activity of
tumor cells and has a relatively good inhibition effect on MCF-7 cells and A549 cells.