利用分子内去芳构化环化策略合成螺环吡咯[2,1-b]喹唑酮化合物的反应研究

由于结构的刚性影响，螺环化合物的合成一直是有机合成的研究热点和最富有挑战性的前沿课题之一。有关吡咯[2,1-b]喹唑酮的合成方法已有许多报道，但通过分子内去芳构化环化反应构建含螺环的吡咯[2,1-b]喹唑酮化合物，目前成功的例子很少。本课题拟发展以炔基喹唑酮通过分子内去芳构化环化策略高效构建螺环吡咯[2,1-b]喹唑酮化合物的方法。根据底物的设计调控反应的选择性，并进一步研究反应的普适性，揭示去芳构化环化构建螺环骨架的规律。在此基础上，利用发展的催化体系和方法学实现若干螺环喹唑酮生物碱的合成。上述工作将为合成螺环喹唑酮骨架提供一条新的途径，为进一步研究含螺环喹唑酮骨架药物提供物质基础。

Due to the influence of rigid structure, the synthesis of spirocyclic compounds has been one of the most challenging and hot topics in organic synthesis. There have been many reports on the synthetic methods of pyrrolo[2,1-b]quinazolone, but few successful examples have been reported on the construction of spiropyrrolo[2,1-b]quinazolone compounds through the intramolecular dearomatization and cyclization reaction. This project intends to develop an efficient method for the construction of spironolpyrrolo[2,1-b]quinazolone compound by means of intramolecular dearomatization and cyclization strategy. According to the design of the substrate, the selectivity of the reaction was regulated, and the reaction scope and limintation were further studied to reveal the regularities of the construction of spirocyclic skeleton by dearomatization and cyclization. Then, several spirocycloquinazolone alkaloids were synthesized by using the developed catalytic system and methodology. This work will provide a new approach for the synthesis of spirocycloquinazolone skeletons and provide a material basis for the further study of drugs containing spirocycloquinazolone skeletons.