中文摘要
本项目着重探讨了汇聚式合成在发现新型（杂环）骨架的有机化合物方面应用，在合成新骨架的过程中，出于对绿色化学要求的思考，尽可能使用了环境友好的条件，比如绿色溶剂的使用，用有机小分子催化剂代替重金属催化剂，催化剂的循环使用以减少排放等。研究结果表明汇聚式合成相比传统的分步反应而言，可以以最为简单的步骤，较高的产率合成具有新颖骨架的杂环化合物，而且一些反应经常表现出良好的选择性。在项目实施的过程中，我们针对不同生理、药理活性化合物骨架的特点，设计、合成了羟吲哚螺环骨架，吲哚联吡啶骨架，吡啶桥联双吲哚骨架，吲哚联呋喃骨架，咪唑并噻唑骨架，1，4－二氢喹啉骨架，双联吡啶骨架等。这些都为化合物的活性筛选提供了更多的选择，并且我们还发现部分化合物可以在配位化学，有机小分子光电材料方面得到应用。拓宽了合成方法的应用价值。
英文摘要
This program has been mainly focused on the application of multicomponent reactions on the construction of novel heterocyclic skeletons. As the green chemistry has been taken into consideration, more environmental benign conditions were chosen during the construction of the target molecules. For instance, the green solvent were utilized in some cases, the metal catalysts were replaced by more environmental friendly organocatalysts, the catalysts were recycled and reused which would avoid the production of the unnecessary wastes. Our results have disclosed that, compared with the conventional multi-step procedure, the multicomponent procedure could afford classes of novel heterocyclic systems in a more convenient and efficient way. Moreover, a number of multicomponent reactions have exhibited splendid selectivity. In our program, a large number of heterocyclic systems such as the spirooxindoles, the indole-containing bipyridines, the bis(3’-indolyl)pyridines, the indole-containing furan derivatives, the 1,4-dihydroquinoline derivatives were devised and synthesized based on their potential biological and pharmacological activities. These compounds have furnished tremendous convenience in the context of generating libraries of molecules for the optimization of potent drug candidates. In addition, some of our products might find their application on coordination chemistry as well as the development of the organic light-emitting devices.
结题摘要
本项目着重探讨了汇聚式合成在发现新型（杂环）骨架的有机化合物方面应用，在合成新骨架的过程中，出于对绿色化学要求的思考，尽可能使用了环境友好的条件，比如绿色溶剂的使用，用有机小分子催化剂代替重金属催化剂，催化剂的循环使用以减少排放等。研究结果表明汇聚式合成相比传统的分步反应而言，可以以最为简单的步骤，较高的产率合成具有新颖骨架的杂环化合物，而且一些反应经常表现出良好的选择性。在项目实施的过程中，我们针对不同生理、药理活性化合物骨架的特点，设计、合成了羟吲哚螺环骨架，吲哚联吡啶骨架，吡啶桥联双吲哚骨架，吲哚联呋喃骨架，咪唑并噻唑骨架，1，4－二氢喹啉骨架，双联吡啶骨架等。这些都为化合物的活性筛选提供了更多的选择，并且我们还发现部分化合物可以在配位化学，有机小分子光电材料方面得到应用。拓宽了合成方法的应用价值。