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Bismuth-Catalyzed Direct Substitution of the Hydroxy Group in Alcohols with Sulfonamides, Carbamates, and Carboxamides


  • This work was supported by a Grant-in-Aid for Specially Promoted Research and a Grant-in-Aid for the Encouragement of Young Scientists (B) (for S.M.) from the JSPS and MEXT.


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No preactivation of the alcohol substrates is required in allylic, propargylic, and benzylic aminations catalyzed by a combination of commercially available Bi(OTf)3 and KPF6, mostly at room temperature (see scheme). The substitution reactions of readily accessible allylic, propargylic, and benzylic alcohols with sulfonamides, carbamates, and carboxamides give the desired amine products in up to 99 % yield.