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Publication in Organic Letters

TAKASAGO has published a paper entitled " Convincing Catalytic Performance of Oxo-Tethered Ruthenium Complexes for Asymmetric Transfer Hydrogenation of Cyclic α-Halogenated Ketones through Dynamic Kinetic Resolution " in Organic Letters.


Org. Lett. 2021, 23, 3070--3075.


The development of an efficient synthetic route for optically active halohydrin compounds is described. A highly efficient dynamic kinetic resolution of cyclic halohydrins was achieved by the asymmetric transfer hydrogenation of racemic α-haloketones using oxo-tethered Ru(II) complexes (DENEB®). By structural tuning of the catalyst, chiral alcohols having halogen, ester, carboxamide, and sulfone functions were obtained variably with excellent diastereo- and enantioselectivities, which provided a concise synthetic approach to a dopamine D3 receptor ligand, (+)-PHNO.