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Public Documents
1
Rhodium-Catalyzed Asymmetric Transfer Hydrogenation of Heterocyclic Diaryl Ketones: F...
Li Wang
and 6 more
August 21, 2023
Transition metal-catalyzed asymmetric transfer hydrogenation has been proved to be a powerful approach for the synthesis of chiral alcohols. Herein, A highly efficient and enantioselective transfer hydrogenation of dibenzoheptaheterocyclic ketones catalyzed by an arene-tethered TsDPEN-based Rh(III) catalyst has been successfully developed, and a variety of dibenzoheptaheterocyclic ketones were reduced by a 1/1 mixture of formic acid and DBU (1,8-diazabicyclo[5.4.0]undec-7-ene) with high yields and enantioselectivities. With this method, the asymmetric reduction of 7,8-difluorodibenzo[b,e]thiepin-11(6H)-one has been realized, providing the key intermediate of baloxavir marboxil with >99% yield and >99% ee at a substrate/catalyst molar ratio of 1000.