Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. Application In Synthesis of 2-Bromobenzo[b]thiophene, C8H5BrS. A document type is Article, introducing its new discovery., Application In Synthesis of 2-Bromobenzo[b]thiophene
A palladium-catalyzed asymmetric carbon-carbon cleavage for the preparation of functionalized axially chiral molecules was reported. Increasing ring distortion not only enhanced the reactivity but also improved the chemoselectivity for different carbon-carbon bonds. This protocol enabled the quick synthesis of ketone-containing axially chiral biaryls in high yields and enantioselectivities.Development of new synthetic strategies for enantioselective carbon-carbon and carbon-heteroatom bond formation is one of the pillars of modern organic chemistry. Whereas significant advances have been achieved in center chirality construction, catalytically asymmetric construction of axial chirality is still under development. Moreover, axially chiral molecules constructed through carbon-carbon and carbon-heteroatom bond cleavage are extremely limited. Here, we report an asymmetric synthesis of biaryl atropisomers via palladium-catalyzed chemoselective carbon-carbon cleavage of 9-aryl-9H-fluoren-9-ols. The reaction demonstrated broad substrate scope and produced the atropisomers in high yields and enantioselectivity. The ring-opening reactivity was considerably accelerated by the torsional strain created by the steric repulsion between two ortho-substituents of the biaryl skeleton in the substrates. The high enantiocontrol hinges on the evolvement of a new TADDOL-based phosphoramidite as ligand. These findings set up a new platform for the development of novel synthetic methods via asymmetric carbon-carbon cleavage.Rapid generation of chirality to increase the complexity of molecules is pivotal for organic synthesis, material chemistry, and drug discovery. By taking advantage of ring strain, we developed a palladium-catalyzed asymmetric carbon-carbon bond cleavage reaction for facile access to a series of axially chiral biaryls in an atom-economical fashion. High functional group tolerance, yields, and enantioselectivities were achieved. The method set up a new platform toward axially chiral biaryl units found in many biologically active natural products, drugs, and catalysts. The present work also showcased a promising strategy for the activation of other non-activated molecules via increasing the ring strain by molecular distortion.
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Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem