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Lewis Acid Catalyzed Ring-Opening 1,3-Aminothiolation of Donor–Acceptor Cyclopropanes Using Sulfenamides

Avishek Guin, Thukaram Rathod, Rahul N. Gaykar, Tony Roy, Akkattu T. Biju

2020Organic Letters64 citationsDOI

Abstract

catalyzed mild and regioselective ring-opening 1,3-aminothiolation of donor-acceptor (D-A) cyclopropanes using sulfenamides has been demonstrated. The insertion of the C-C σ-bond of D-A cyclopropanes into the S-N σ-bond of sulfenamides allows the synthesis of diverse γ-aminated α-thiolated malonic diesters in moderate to good yields (up to 87%) with good functional group compatibility. The stereospecificity of the reaction was demonstrated using enantiomerically pure D-A cyclopropane.

Topics & Concepts

ChemistryCyclopropaneRegioselectivityRing (chemistry)CatalysisLewis acids and basesAcceptorStereospecificityMedicinal chemistryOrganic chemistryPhysicsCondensed matter physicsCyclopropane Reaction MechanismsSulfur-Based Synthesis TechniquesCatalytic Alkyne Reactions
Lewis Acid Catalyzed Ring-Opening 1,3-Aminothiolation of Donor–Acceptor Cyclopropanes Using Sulfenamides | Litcius