对映选择合成
立体中心
动力学分辨率
催化作用
化学
配体(生物化学)
组合化学
二胺
立体化学
有机化学
受体
生物化学
作者
Jie Kang,Kang Ding,Si‐Mu Ren,Wen-Jun Yang,Bo Su
标识
DOI:10.1002/anie.202415314
摘要
P‐stereogenic phosphorus compounds are essential across various fields, yet their synthesis via enantioselective P‐C bond formation remains both challenging and underdeveloped. We report the first copper‐catalyzed enantioselective hydrophosphorylation of alkynes, facilitated by a newly designed chiral 1,2‐diamine ligand. Unlike previous methods that rely on kinetic resolution with less than 50% conversion, our approach employs a distinct dynamic kinetic asymmetric transformation mechanism, achieving complete conversion of racemic starting materials. This reaction is compatible with a broad range of aromatic and aliphatic terminal alkynes, producing products with high yields (up to 95%), exclusive cis selectivity, and exceptional regio‐ and enantioselectivity (> 20:1 r.r. and up to 96% ee). The resulting products were further transformed into a diverse array of enantioenriched P‐stereogenic scaffolds. Preliminary mechanistic studies were conducted to elucidate the reaction details.
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