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Divergent Synthesis of β‐Hydroxy Amides (Esters) and γ‐Amino Alcohols via Ir/f‐Diaphos Catalyzed Asymmetric Hydrogenation

Xianghua Zhao, Zehui Yang, Yuqi Cheng, An Huang, Fangyuan Hu, Fei Ling, Weihui Zhong

Advanced Synthesis & Catalysis, 2022

13 citations

Abstract

Abstract The iridium/f‐diaphos L2 or L9 catalyzed asymmetric hydrogenation of β‐aryl β‐keto amides (esters), and β‐amino ketones to afford two enantiomers of the desired chiral alcohols was realized with 90%‐99% yield and 73%‐99% ee. This protocol could be easily conducted on gram scale in the presence of low catalyst loading (up to 9900 TON). Moreover, the hydrogenated products are versatile building blocks for a variety of biologically active molecules and drugs, such as Fluoxetine, Dapoxetine and so on. magnified image

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