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Article Abstract

We have synthesized a series of sterically hindered ligands f-Amphbinol , which were successfully applied in the asymmetric hydrogenation of various ketones with excellent results (up to 63 examples, 95 → 99% yields, 90 → 99% ee, >20:1 dr). Ligand screening experiments demonstrated that the enantioselectivity of hydrogenation increases with the increase in the steric hindrance of substituents on P-aryl rings of the ligand. Besides, the key intermediates for API Ladostigil were successfully synthesized with this catalyst system, which hinted at the potential applications.

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http://dx.doi.org/10.1021/acs.joc.5c00943DOI Listing

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