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Stereoselective Sulfa-Michael/Aldol Reaction Promoted by an Axially Chiral Styrene-Based Organocatalyst

Hao Yu, Zihao Li, Peng-Fei Lian, Quan‐Zhe Li, Yuan She, Zhi‐Gang Ma, Shu‐Yu Zhang

2023Organic Letters14 citationsDOI

Abstract

Herein, we describe a stereoselective sulfa-Michael/aldol cyclization reaction promoted by a rationally designed novel axially chiral styrene-based organocatalyst. A variety of highly substituted tetrahydrothiophenes featuring an alkyne-substituted quaternary stereogenic center are obtained in good yields, excellent stereoselectivities, and exclusive trans selectivities. This process tolerates a broad range of alkynyl-substituted acrylamides under mind conditions. The utility of this approach is highlighted in its excellent asymmetric introduction, scalability, and attractive product diversification.

Topics & Concepts

StereocenterChemistryAldol reactionStereoselectivityStyreneAlkyneCombinatorial chemistryOrganic chemistryCatalysisEnantioselective synthesisCopolymerPolymerAxial and Atropisomeric Chirality SynthesisSulfur-Based Synthesis TechniquesAsymmetric Synthesis and Catalysis
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