Method for the synthesis of flavonoid nitrogen mustard derivatives

• Main Authors: Jinglei Song, Meixuan Yu, Xi Yan, Haijun Hao
• Format: Article
• Language: English
• Published: Elsevier 2020-01-01
• Series: MethodsX
• Subjects: Chlorination; Organic synthesis; Yield
• Online Access: http://www.sciencedirect.com/science/article/pii/S2215016120301229

We have prepared a kind of new type of flavonoid nitrogen mustard derivatives with broad-spectrum antitumor activity, which have not been reported in the literature. In the process of preparing intermediate (the flavonoid diethanolamine derivatives) of the target compound, we found that the reasonable separation method is silica gel column chromatography with eluent (MeOH/CH2Cl2, 1:40). The experimental results show that the composition of eluent is an important factor to get high yield of the intermediate, which will directly affect the final yield of the target compound. Acetonitrile is the suitable solvent in the reaction system, and the optimized reaction condition is reaction under reflux condition for 48 hours. Several new flavonoid nitrogen mustard derivatives were synthesized with high yield using the above method. • A method for the synthesis of flavonoid nitrogen mustard derivatives was introduced. • The reasonable purification conditions and the optimized reaction time were recommended.