jo0c01438_si_002.cif (2.48 MB)

Asymmetric Transfer Hydrogenation: Dynamic Kinetic Resolution of α‑Amino Ketones

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posted on 19.08.2020, 21:05 by Shweta K. Gediya, Guy J. Clarkson, Martin Wills
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.