钯催化的手性阴离子联萘酚-磷酸配体促进的脂肪族伯胺的对映选择性 C-H 活化。
Palladium-Catalyzed Enantioselective C-H Activation of Aliphatic Amines Using Chiral Anionic BINOL-Phosphoric Acid Ligands.
机构信息
Department of Chemistry, University of Cambridge , Lensfield Road, Cambridge CB2 1EW, United Kingdom.
出版信息
J Am Chem Soc. 2017 Feb 1;139(4):1412-1415. doi: 10.1021/jacs.6b12234. Epub 2017 Jan 18.
PMID:28064488
Abstract
The design of an enantioselective Pd(II)-catalyzed C-H amination reaction is described. The use of a chiral BINOL phosphoric acid ligand enables the conversion of readily available amines into synthetically valuable aziridines in high enantiomeric ratios. The aziridines can be derivatized to afford a range of chiral amine building blocks incorporating motifs readily encountered in pharmaceutically relevant molecules.
摘要
本文描述了一种对映选择性 Pd(II)-催化的 C-H 胺化反应的设计。使用手性 BINOL 磷酸配体，可将易得的胺转化为具有高对映选择性的合成有价值的氮丙啶。氮丙啶可以衍生化，得到一系列包含药物相关分子中常见结构单元的手性胺砌块。
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