含哒嗪酮结构的L-缬氨酸取代去甲斑蝥素衍生物的制备与应用

Preparation and Application of L-valine Substituted Norcantharidin Derivatives Containing Pyridazine Ketone

采用1,3-偶极环加成方法,在L-缬氨酸取代去甲斑蝥素结构中的C5和C6位引入吡唑环,进而与含哒嗪酮结构的色酮醛腙反应导入哒嗪酮结构,生成含哒嗪酮结构的L-缬氨酸取代去甲斑蝥素衍生物.该衍生物具有多种生物活性,可用于潜在药物的开发研究.

In this paper,the pyrazole ring was introduced into the structure of L-valine replaced norcantharidin in C5 and C6positions by 1,3-dipolar ring addition method;,the structure of pyridazine was then introduced into the structure of pyridazine through reaction with tryptoprozone containing azone structure; the Lvalrine containing pyridazine ketone was generated to replace the derivatives of norcantharidin. This derivative has a variety of biological activities,thus used in the development and research of potential drugs.