Enantioselective Synthesis of Hemiaminals via Pd-Catalyzed C–N Coupling with Chiral Bisphosphine Mono-oxides

A novel approach to hemiaminal synthesis via palladium-catalyzed C–N coupling with chiral bisphosphine mono-oxides is described. This efficient new method exhibits a broad scope, provides a highly efficient synthesis of HCV drug candidate elbasvir, and has been applied to the synthesis of chiral N,N-acetals.

本研究报道了一种通过钯催化C-N偶联、以手性双膦单氧化物为配体的半缩胺（hemiaminal）合成新方法。该高效新方法底物适用范围广泛，可高效合成丙型肝炎病毒（HCV）候选药物艾尔巴韦（elbasvir），并已应用于手性N,N-缩醛（N,N-acetals）的合成。