Preparation Of 5,8-Dimethoxyl-1,4-Naphthoquinone-6-Formic Acid Derivatives And Studies On Their Antitumor Activities

Shikonin as a traditional Chinese medicine, exhibit a wide variety of pharmacological effects, including antibacterial, anti-inflammatory, antiviral and antioncogenic activities. Shikonin and its derivatives are the main active component. Now shikonin is mainly isolated from the natural Zicao. The research on the anti-inflammatory, anti-cancer and anti-virus activity of the shikonin has become a hot topic in this area. Besides, shikonin is also a good natural pigment and has been used in food and cosmetic industry, the demand quantity of shikonin is very high. The method of total synthesis is an effective means to meet the demand of natural product.There have been many reports about the total synthesis of shikonin since shikonin was synthesized by using 1,4,5,8-tetramethoxynaphthalene-2 -carboxaldehyde as starting material by Japanese scholar in 1980s. We optimized the synthetic technologies of key intermediates, 1,4,5,8-Tetramethoxy-naphthalene-2-carbaldehyde. 1,4,5,8-tetramethoxy -naphthalene was prepared from the oxidation of 1,5-dinitronaphthalene and the reaction product naphthazarin was directly methylated without been purified. The 1,4,5,8-Tetramethoxy -naphthalene -2-carbaldehyde was...