Pharmaceutically acceptable salt of benzocoumarin derivative, and preparation method and application thereof

• Main Authors: LIU JIACHUN, ZHAO ZHANCHAO, MAO HUIJUAN, ZHANG WEN
• Format: Patent
• Language: Chinese; English
• Published: 19.04.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention provides a pharmaceutically acceptable salt of a benzocoumarin derivative, and a preparation method and an application thereof, belonging to the field of medicinal chemistry. According to the invention, the preparation method has the advantages of simplicity, easily available raw materials and convenient aftertreatment; and the target compound provided by the invention has high synthetic yield and purity, wherein the purity is up to 98% or above, and the structure of the compound passes verification of nuclear magnetism and mass spectrometry. Pharmacological activity screening experiment results show that the compound with a novel structure displays extremely strong cytotoxic activity on human hepatoma cell line HepG2, and the compound has a minimum IC50 value reaching 7.85 [mu]M and provides important values for further development of benzocoumarin antitumor drugs. 苯并香豆素类衍生物药学上可接受的盐及其制备方法和应用，属于药物化学领域。本发明提供了类苯并香豆素类衍生物药学上可接受的盐及其制备方法和应用，其制备方法简单、原料简易，后处理方便，所发明的目标化合物合成收率和纯度高，其纯度高达98％以上，其结构均通过核磁和质谱验证