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Bi(OAc)<sub>3</sub>/Chiral Phosphoric Acid-Catalyzed Enantioselective 1,2- and Formal 1,4-Allylation Reaction of β,γ-Unsaturated α-Ketoesters

Xiang-Shuai Liu, Yao Li, Xin Li

2021Organic Letters17 citationsDOI

Abstract

A highly efficient asymmetric 1,2-allylation reaction of β,γ-unsaturated α-ketoesters was realized by using a Bi(OAc)3/chiral phosphoric acid catalyst system under mild conditions. Meanwhile, using this combined strategy of enantioselective 1,2-allylation and subsequent anionic oxy-Cope rearrangement, the asymmetric formal 1,4-allylation reaction was achieved by a one-pot process. These reactions offer rapid access to an array of homoallylic tertiary alcohols and γ-allyl-α-ketoesters with good yields and excellent enantioselectivities. Density functional theory calculations were conducted to interpret the high enantioselectivity.

Topics & Concepts

Enantioselective synthesisPhosphoric acidChemistryCatalysisFormal synthesisReaction conditionsCombinatorial chemistryOrganic chemistryMedicinal chemistryAsymmetric Synthesis and CatalysisSynthetic Organic Chemistry MethodsChemical Synthesis and Analysis