摘要/Abstract

发展高效实用的不对称催化反应对手性药物的简洁合成具有重要的意义，而手性配体和催化剂对于发展高效的不对称催化反应尤为关键.综述了基于苯并氧杂膦烷结构的P-手性单膦和双膦配体的设计理念以及它们在手性药物合成中的应用.这类配体具有P-手性、刚性，大位阻和富电子等结构特征，物理化学性质稳定，并且易于衍生化，在过渡金属催化的不对称氢化、偶联、环化和加成反应中表现出优异的催化性能.这些不对称催化反应的发展促进了一系列重要药物分子的高效不对称合成.
关键词: 手性膦配体, 苯并磷氧杂环, 不对称氢化, 不对称偶联, 手性药物
Development of efficient and practical asymmetric catalytic reactions plays a pivotal role for the concise syntheses of chiral drugs. Chiral ligands and catalysts are crucial for the selectivity and reactivity of the catalytic reactions. In this account, the design and development of a series of P-chiral mono- and bis-phosphorus ligands were summarized based on a benzooxaphosphane backbone and their applications in the synthesis of chiral drugs. Beside their P-chirality, these ligands are structurally rigid, sterically bulky, and electron-rich, providing good physical properties and tunabilities. Facilitated by these chiral ligands, a series of efficient and practical reactions including asymmetric hydrogenation, asymmetric cross-coupling, asymmetric cyclization, and asymmetric nucleophilic additions have been developed. The excellent conversions, yields, regioselectivities, enantioselectivities, and broad substrate scope have enabled concise and efficient syntheses of a series of chiral drugs.
Key words: chiral phosphorus ligands, transition metal catalysis, asymmetric synthesis, enantioselectivity, chiral drugs


PDF全文下载地址:

点我下载PDF