目的 吡唑啉酮和羟吲哚骨架是两类非常重要的药效团，在药物化学中占据了非常重要的地位。其中吡唑啉酮是一类含有N-N键的五元杂环类化合物，因其在药物化学和功能性材料中的广泛应用而成为杂环中最重要的含氮杂环之一。同时，羟吲哚衍生物以其独有的化学结构,使其具有独特的生理抗癌活性和阻胺镇痛的作用。靛红是靛蓝的氧化产物，存在于板蓝根属植物中，是人体肾上腺素的代谢衍生物。鉴于药效团组合策略在药物研发中的重要性，将这两种药效团进行有机结合将为药物研发奠定重要的分子基础。方法 考虑到SNV反应在C-C键偶联中的重要应用，本文从4-位单取代吡唑啉酮出发，通过其与靛红衍生硝基烯烃之间的SNV反应，得到了多种手性烯基吡唑啉酮加合物。通过对催化剂、溶剂及温度等影响因素的筛选，确定了最佳反应条件。在最佳反应条件下，实现了对结构多样的吡唑啉酮类化合物的底物扩展，所得产物均经过¹H NMR、¹³C NMR、HRMS等表征分析并确定结构。结果 该合成策略构筑了一系列含有带有一个羟吲哚部分的四取代立体异构中心的手性烯基，具有较高的收率（优异的区域选择性（E:Z >20:1）和较好的对映选择性（最高达 86% ee）。结论 这些新型烯基吡唑啉酮加合物有望为寻找新型先导化合物提供了物质支撑。

Objective Pyrazolone and hydroxyindole structures are two very important pharmacophore, which occupy a very important position in medicinal chemistry. Among them, pyrazolone is a kind of five membered heterocyclic compounds containing N-N bond. It has become one of the most important nitrogen heterocycles in heterocycles due to its wide application in medicinal chemistry and functional materials. At the same time, hydroxyindole derivatives have unique physiological anticancer activity and analgesic effects due to their unique chemical structure. Isatin is an oxidation product of indigo, found in plants of the genus Isatis, and is a metabolic derivative of adrenaline in the human body. In view of the importance of pharmacophore combination strategy in drug research and development, the organic combination of these two pharmacophore will lay an important molecular foundation for drug research and development. Methods Considering the important application of SNV reaction in C-C bond coupling, in this paper, starting from the 4-position monosubstituted pyrazolone, a variety of chiral alkenylpyrazolone adduct were obtained through the SNV reaction between it and the isatin-derived nitroalkenes. The optimal reaction conditions were determined by screening factors such as catalysts, solvents, and temperature. Under the optimal reaction conditions, substrate expansion of structurally diverse pyrazolone compounds was achieved, and the resulting products were characterized and analyzed by 1H NMR, 13C NMR, HRMS, and other methods to determine their structures. Results This synthesis strategy constructs a series of chiral alkenyls containing a tetrasubstituted stereoisomeric center with a hydroxyindole moiety, which have high yields (excellent regioselectivity (E: Z >20:1) and good enantioselectivity (up to 86% ee). Conclusion These new alkenylpyrazolone adduct are expected to provide material support for the search for new lead compound.