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Dynamic Kinetic Asymmetric Reductive Amination: Synthesis of Chiral Primary β-Amino Lactams.

A new interesting article has been published in Angew Chem Int Ed Engl. 2018 Oct 22;57(43):14193-14197. doi: 10.1002/anie.201809719. Epub 2018 Oct 2. and titled:

Dynamic Kinetic Asymmetric Reductive Amination: Synthesis of Chiral Primary β-Amino Lactams.

Authors of this article are:

Lou Y, Hu Y, Lu J, Guan F, Gong G, Yin Q, Zhang X.

A summary of the article is shown below:

A highly efficient ruthenium-catalyzed asymmetric reductive amination (ARA) of racemic β-keto lactams with molecular hydrogen and ammonium salts is disclosed for the synthesis of enantiomerically pure primary amino lactams through dynamic kinetic resolution (DKR). By this approach, a range of syn primary β-amino lactams were obtained in high yields with high chemo-, enantio-, and diastereoselectivity (up to 98 % yield, 99 % ee, >20:1 d.r., syn products). The utility of the products has been demonstrated by rapid access to a key synthetic intermediate towards biologically active drug molecules. Meanwhile, mechanistic studies and control experiments indicate that the reaction may proceed through the hydrogenation of an iminium intermediate.

Check out the article’s website on Pubmed for more information:



This article is a good source of information and a good way to become familiar with topics such as:

asymmetric catalysis;asymmetric hydrogenation;chiral lactams;primary amines;reductive amination

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