β–Amino sulfone compounds have received great attention because of its applications to natural products, drugs, and functional materials. In addition, β-amino sulfones are important intermediates in the preparation of cyclic or acyclic nonproteinogenic α-amino acids, amines, and alkaloids, taking advantage of the fact that sulfones can be involved in synthetic transformations. The carbon-nitrogen bond forming reaction is an interesting topic for synthesizing numerous functionalized amines. In particular, metal-catalyzed hydroamination is one of the most efficient and straightforward methods. Among the numerous metal-catalyzed hydroamination reactions, copper-catalyzed amination to alkenes is attractive due to the use of cheap and easy-to-handle copper catalyst and the use of readily available alkenes. Herein, we described an efficient and regioselective hydroamination of heterocycles with allylic sulfones promoted by an NHC-Cu catalyst. The amination was carried out in the presence of NHC-CuCl and KO<i><sup>t</sup></i>Bu under mild reaction conditions, providing a broad range of β-amino sulfones in high yields with excellent regioselectivity.

Synthesis of β-amino sulfones through copper-catalyzed hydroamination of allylic sulfones

2019 Fall National Meeting

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