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Highly Enantioselective Hydrogen-Transfer Reductive Amination: Catalytic Asymmetric Synthesis of Primary Amines


  • We thank Prof. A. Börner, Prof. K.-H. Drauz, Dr. J. Almena, Dr. A. Monsees, and Dr. V. I. Tararov for stimulating and helpful discussions.


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Ammonium formate is the hydrogen source in the catalytic asymmetric reductive amination of ketones presented here (Leuckart–Wallach-type reaction). The reaction proceeds smoothly in methanol in the presence of Ir, Rh, and Ru catalysts. Primary amines were obtained as products in good yields with high enantioselectivities after hydrolytic workup when [((R)-tol-binap)RuCl2] was used as the catalyst (see scheme). R1, R2=alkyl, aryl.

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