唑类化合物的反应特性及其在活性天然产物全合成中的应用研究

含氮杂环特别是唑类化结构广泛存在于大量的天然产物和小分子中，大部分化合物都表现出较好的生理活性，对于含氮杂环化学研究一直是有机化学研究的热点之一。本项目拟在课题组前期工作基础上，以五元含氮杂环特别是唑类化合物为研究对象，系统开展其金属催化反应特性以及在活性分子中的合成应用研究，我们将从以下四个方面入手：1）首次利用环境友好的氧化反应高效合成唑类化合物；2）首次系统探索基于金属催化C-H断裂特别是双C-H键断裂的偶联反应实现唑类化合物的C4/C5-位官能团化反应，考查C/4/C5位的反应调控规律；3）利用本组发展金属催化偶联反应方法学以及调控规律，开展若干唑类小分子化合物的合成以及唑类、吡咯类等活性天然产物的全合成研究。期望通过本课题的实施，系统阐明唑类化合物的反应特性，拓展方法学在唑类化合物多样性合成以及其他含氮杂环天然产物全合成的应用，从而为开发以含氮杂环为模板的药学研究奠定化学基础。

Heterocycles containing nitrogen atom such as azoles (thiazole, oxazole or imidazole) are prevalent scaffolds found in a variety of natural products and pharmacophores, many of which possess very attractive bioactivities, such as antiviral, antifungal, antibacterial and anti-tumor activities. The interesting biactivities of these moieties have attracted much attention from synthetic cmmunity in the past several decades. In this project, we wish to systematically conduct the reseaches on the chemisty of azoles and other related heterocycles and synthetic application to several bioactive compounds. This work is expected to pave an avenue to the synthesis of heterocyclic boactive molecules for drug development. Systematic investigation will be performed as followed:.1) Preparation of azoles and other heterocyle using molecular oxygen as a sole oxidant in various solvents will be conducted..2) Transition-metal-catalyzed reactions through double C-H cleavage and decarboxylative cross-coupling reactions will be investigated to demonstrate the reactivity and regioselectivity of the selected heterocyles..3) Synthetic application of the transition-metal-catalyzed cross-coupling reactions to several bioactive compounds and natural products will be performed.