Abstract An asymmetric para‐ C(sp 2 )−H bond functionalization of alkyl benzene derivatives was successfully developed via cooperative catalysis of gold and chiral phosphoric acid (CPA), leading to synthetically useful chiral 1,1‐diaryl motifs. Chiral phosphoric acid, ligand, and molecular sieves were found to be crucial for enantioselectivity control of this transformation. The salient features of this protocol include mild conditions, high efficiency, commercially available starting materials, highly chemo‐ and site‐ as well as enantioselective aromatic C−H functionalization, broad substrate scope, and extensive applications of the chiral products. The mechanistic studies suggested that two CPAs might be involved in chiral induction.
Abstract The direct conversion of CH bond into CX bond has been emergent as an efficient approach for the construction of complex molecules. In this area, gold‐catalyzed C(sp 2 )H bond functionalization has attracted great interest over the past two decades as a synthetic toolbox for the construction of complex molecules and late‐stage modification of bioactive compounds. This article summarizes the evolution of gold‐catalyzed C(sp 2 )H bond functionalization and exhibits the different chemo‐ and site‐selectivities under various reaction conditions.
Abstract An asymmetric para‐ C(sp 2 )−H bond functionalization of alkyl benzene derivatives was successfully developed via cooperative catalysis of gold and chiral phosphoric acid (CPA), leading to synthetically useful chiral 1,1‐diaryl motifs. Chiral phosphoric acid, ligand, and molecular sieves were found to be crucial for enantioselectivity control of this transformation. The salient features of this protocol include mild conditions, high efficiency, commercially available starting materials, highly chemo‐ and site‐ as well as enantioselective aromatic C−H functionalization, broad substrate scope, and extensive applications of the chiral products. The mechanistic studies suggested that two CPAs might be involved in chiral induction.
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