| Dynamic kinetic resolution (DKR) is an efficient method to obtain optically pure compounds from racemic substrates. Recently, increasing attention has been given to the discovery of DKR reactions, which can, theoretically, result in quantitative yield with enantiomeric excess (ee) approaching 100%. A few examples about DKRs have been reported via asymmetric transfer hydrogenation. After consulting a lot of literatures, this dissertation, we describe the design and synthesis of a series ofβ–keto sulfones, and the realization of DKR of these substrates via asymmetric transfer hydrogenation reaction.1. The synthesis of a series ofβ–keto sulfones with good yield. All products was well confirmed with data of 1H NMR.2. Dynamic kinetic resolution of a series ofβ–keto sulfones was achieved by their asymmetric transfer hydrogenation using HCOOH : Et3N = 5 : 2 as the hydrogen source and (S,S)-TsDPEN based Ru (II) catalyst, providing the corresponding chiralβ–hydroxyl sulfones with good yield, high dr and ee. |
