The Direct Asymmetric A-alkylation Reaction Of Ketones With3-hydroxy-3-indolyl Oxoindole By Chiral Phosphoric Acid Catalysis

Indole units are core structures in numerous biological active compounds and natural products.The development of asymmetric methodologies for synthesizing chiral indole derivatives is a longstanding project in organic synthesis. In this thesis, We disclosed the first highly enantioselective alkylation reaction of ketons with3-Hydroxy-3-indolyl Oxoindole by chiral phosphric acid. Under the optimal reaction conditions, the desired products were synthesized with up to99:1diastereoselectivity (d.r.) and97%enantioselectivity (ee). Our method provided an efficient way of preparing3-indoly compounds.