Asymmetric Transfer Hydrogenation: Dynamic Kinetic Resolution of α-Amino Ketones.,The Journal of Organic Chemistry

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Asymmetric Transfer Hydrogenation: Dynamic Kinetic Resolution of α-Amino Ketones.
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2020-08-07 , DOI: 10.1021/acs.joc.0c01438
Shweta K Gediya ₁ , Guy J Clarkson ₁ , Martin Wills ₁

Affiliation

A series of α-amino ketones were reduced using asymmetric transfer hydrogenation (ATH) through a dynamic kinetic resolution (DKR). The protecting group was matched to the reducing agent, and following optimization, a series of substrates were investigated, giving products in high diastereoselectivity, over 99% ee in several cases and full conversion. The methodology was applied to the enantioselective synthesis of an MDM2–p53 inhibitor precursor.

中文翻译：

不对称转移加氢：α-氨基酮的动态动力学拆分。

使用不对称转移氢化（ATH）通过动态动力学拆分（DKR）还原了一系列α-氨基酮。使保护基与还原剂匹配，并在优化后对一系列底物进行了研究，从而获得了具有高非对映选择性的产品，在某些情况下具有超过99％ee的产物并实现了完全转化。该方法应用于MDM2-p53抑制剂前体的对映选择性合成。

更新日期：2020-09-05

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