Tryptanthrin possesses remarkable antitumor, anti-inflammatory and antibacterial activity as one of the active ingredients in medicinal plants Strobilanthes cusia, Polygonum tinctorum Lour and Isatis Einetorial. However, despite a variety of synthesis methods had been developed, the yield was low, and the cost was high due to the use of isatoic anhydride. Furthermore, not a single current synthesis method is efficacious and sim-ple enough to meet the requirement for the use in lab and industry. Our previous study on the distribution of tryptanthrin in Isatis Einetorial demonstrated that tryptanthrin was a product resulted from the reaction between isatin and anthranilic acid in the leaves during a drying process instead of a constitutive component within the plant. In order to develop an efficient and simple method, a biomimetic synthesis of tryptanthrin was carried out using isatin and anthranilic acid existing naturally in the medical plants as reaction agents, with THF and toluene as solvents in the presence of catalyst POCl3 . A high yield of 40. 3% was obtained, and the product showed a structure characterization same to that of standard sample. After the first trial, total other 14 deriva-tives of tryptanthrin were synthesized using the same method with relatively reasonable yields. Moreover, the raw materials used in this study were readily available and much cheaper than those in conventional methods, and the reaction conditions were relatively mild. It implied that the synthesis method reported could be applied widely.%以药用植物体内存在的生物合成前体吲哚醌和邻氨基苯甲酸为反应物，用POCl3作催化剂，仿生合成了天然产物色胺酮(1)，结构表征结果与标准品一致。该反应所用原料易得，避免了使用较昂贵的靛红酸酐，适合实验室小规模简便合成。采用此方法合成了14个色胺酮衍生物，可见其具有广泛的适应性。
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