新型NN2 pincer配体的研制及其促进烷基胺/醇类衍生物的Sonogashira反应研究

炔烃是有机化学中最重要的官能团之一，广泛应用于化学生物学、制药和材料科学等领域中。近年来，发展简捷、高效的炔烃构筑方法得到了化学家的广泛关注和浓厚的研究兴趣。过渡金属催化的芳基或烯基亲电试剂的Sonogashira反应是合成取代炔烃最有效和便捷的方法之一，但是非活化烷基亲电试剂的Sonogashira偶联仍然是一个巨大的挑战且研究的很少，主要局限于环境不友好、价格昂贵的卤代烷烃参与的交叉偶联反应。因此，发展新型、廉价易得的烷基化试剂的Sonogashira反应尤为迫切和需要。本项目拟通过设计和开发新型、高活性的NN2 pincer配体，将廉价易得、来源广泛的烷基胺和醇类化合物作为新的烷基化试剂应用到Sonogashira反应中，发展高效、高选择性的镍催化的Sonogashira反应及其挑战性的不对称反应，为合成重要的烷基取代炔烃提供新颖和实用的方法。

Alkynes are amongst the most valuable functional groups in organic chemistry and widely used in chemical biology, pharmacy, and materials science. Recently, developing straightforward and efficient methods for the construction of alkynes has attracted lots of attentions and intense interests. Although transition-metal catalyzed Sonogashira coupling of aryl or vinyl electrophiles has proven to be one of the most efficient and convenient method for the synthesis of substituted alkynes, the coupling of non-activated alkyl electrophiles is still a formidable challenge, and the few reports were largely restricted to the use of environment-unfriendly, expensive alkyl halides. Therefore, it is highly urgent and desirable to develop such coupling with new alternatives that are cheap and easily available reagents. This project will enable the utilization of readily available, naturally abundant alkyl amines and alcohols as new alkylating agents in Sonogashira reactions based on the design and development of novel, highly active NN2 pincer ligands, and develop the highly effective and selective nickel-catalyzed Sonogashira coupling as well as challenging asymmetric reactions, providing novel and practical approaches for the synthesis of important alkyl substituted alkynes.