基于手性三唑配体催化剂的合成及在借氢反应中的应用

Design and synthesis of novel, highly efficient and inexpensive chiral ligands is the key step to the realization of asymmetric borrowing hydrogen reaction, which has important academic significance and application prospect. This project will design and synthsize new types ligands of triazole amide alcohols, triazole cinchona alkaloid and triazole cyclohexanediamine skeleton through the use of strong coordination ability of triazole, which was easy to form stable metal π backbonding. With the catalysts based on the upper triazole ligands in hand, the project will focus on the following research areas: investigation the coordination of these two ligands and transition metals; synthesis of aromatic heterocyclic compounds, amine compounds and biologically active natural products through borrowing hydrogen strategy. The key problem is: synthesis of chiral amine derivatives with asymmetric borrowing hydrogen; solving the difficult problem of asymmetric borrowing hydrogen reaction. This provides a feasible route for industrial production of heterocyclic aromatic compounds and chiral amine compounds by using asymmetric hydrogenation strategy.

设计合成新颖、高效和廉价的手性配体是实现不对称借氢反应的关键，具有极其重要的学术意义和可观的工业价值。本课题利用三唑具有较强的配位能力，容易与金属形成稳定的反馈π键，拟设计合成新型骨架的三唑酰胺醇、三唑金鸡纳碱和三唑环己二胺骨架的配体，以制备活性较高和稳定性较好的三唑骨架催化剂；并将得到的催化剂应用于借氢反应和不对称借氢反应。研究以简单的醇作为原料，通过借氢策略催化合成芳香杂环化合物、胺类化合物、具有生物活性的天然产物和手性胺类衍生物；尤其是克服不对称借氢反应难题，为工业上采用不对称借氢反应策略生产芳香杂环化合物和手性胺类化合物提供了一种切实可行的路线。

设计合成新颖、高效和廉价的手性配体是实现不对称借氢反应的关键，具有极其重要的学术意义和可观的工业价值。本课题利用三唑具有较强的配位能力，设计合成了几类新型三唑骨架的配体以及相对应的催化剂；并将得到的催化剂成功应用于借氢反应和脱氢借氢反应中。研究以简单的醇作为原料，通过借氢策略催化合成了芳香杂环化合物、胺类化合物、具有生物活性的喹啉化合物等；为工业上采用不对称借氢反应策略生产芳香杂环化合物和胺类化合物提供了一种切实可行的路线。