Department of Process Chemistry, Merck & Co. Inc. , Rahway, New Jersey 07065, United States.
J Am Chem Soc. 2015 Nov 4;137(43):13728-31. doi: 10.1021/jacs.5b05934. Epub 2015 Oct 21.
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.
一种新型的通过钯催化 C-N 偶联与手性双膦单氧化物的半亚胺合成方法被描述。这种高效的新方法具有广泛的应用范围,为 HCV 药物候选物 elbasvir 的高效合成提供了可能,并已应用于手性 N,N-缩醛的合成。