Details

Autor(en) / Beteiligte

• Yang, Pengtao
• Song, Dingguo
• Chen, Lingxin
• Zhao, Xianghua
• Chen, Yirui
• Shen, Feiyang
• Ling, Fei
• Zhong, Weihui

Titel

Dynamic kinetic resolution of α-F-β-ketone amides (esters) via Ir/f-diaphos-catalyzed asymmetric hydrogenation

Ist Teil von

• Organic Chemistry Frontiers, 2024-04, Vol.11 (8), p.2201-2207

Ort / Verlag

London: Royal Society of Chemistry

Erscheinungsjahr

2024

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Chiral fluorine stands as a widespread building unit, demonstrating favorable pharmacological activity in numerous drugs and intermediates. In this study, we describe an Ir/f-diaphos-catalyzed asymmetric hydrogenation of α-F-β-ketone amides (esters) via dynamic kinetic resolution, conducted under mild conditions. The resulting products exhibited exceedingly high enantioselectivities and diastereoselectivities, surpassing 99% ee and 99/1 dr, respectively, with their absolute configuration confirmed through XRD analysis. Additionally, we showcase the successful execution of this methodology on a gram scale and explore further transformations of the obtained products.