ASYMMETRIC SYNTHESIS THROUGH MOLECULAR DIVERSITY

不对称手性配体组合库的合成 提出了过渡金属催化。 双齿配体将是 由非天然氨基酸和手性氨基醇组装而成。 的 模块化框架提供了多种结合几何形状和手性 螯合双次膦酸盐的环境。 图书馆将 在两个充分研究的反应中筛选不对称诱导：Pd- 催化的烯丙基酰胺化和Rh催化的烯酰胺氢化。 最后，将不对称配体库应用于先前的 非手性铑催化的二烯环化反应。 新的手性催化剂的发现对于扩大手性催化剂的应用具有重要意义。 制备对映体纯药物的合成方法。 如果 如果成功，所提出的战略将提供一种新的快速方法， 用于开发和合成不对称配体， 对映选择性催化过程。

Synthesis of a combinatorial library of chiral ligands for asymmetric transition metal catalysis is proposed. The bidentate ligands will be assembled from unnatural amino acids and chiral amino alcohols. The modular framework provides a variety of binding geometries and chiral environments for the chelating bisphosphinites. The library will be screened for asymmetric induction in two well studied reactions: Pd- catalyzed allylic amidation and Rh-catalyzed enamide hydrogenation. Finally, the asymmetric ligand libraries will be applied to a previously achiral Rh-catalyzed diene cyclization reaction. The discovery of new chiral catalysts is important in expanding the synthetic procedures for production of enantiomerically pure drugs. If successful, the proposed strategy would provide an new and rapid method for the development and synthesis of asymmetric ligands for enantioselective catalytic processes.