Iridium-Catalyzed Diastereoselective Amination Of Alcohols With Chiral Tert-Butanesulfinamide

Chiral amines exist in natural products,drug molecules and bioactive molecules and are widely used in the synthesis of pesticides,pharmaceuticals and other organic molecules and so on.Therefore,it is of great importance to develop highly effective and enantioselective method to produce chiral amines.In recent years,with the introduction of green chemistry,the development of a highly efficient and environmentally friendly method has also been concerned by chemists.In this paper,the formation of chiral amines is promoted by the iridium catalyst.Chiral amines are produced from racemic alcohols and chiral t-butyl sulfinamides via the borrowing hydrogen process.The amine derivatives have been obtained in higher yields(50%-94%)and diastereoselective(>19:1),and the only by-product are water.Chiral amine derivatives derived from this methodology have undergone a series of reactions and have been transformed into(S)-Rivastigmine and NPS R-568 for the treatment of Alzheimer’s disease and primary and secondary hyperparathyroidism.