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Pd(II)‐Catalyzed Tandem Enantioselective Methylene C(sp<sup>3</sup>)−H Alkenylation–Aza‐Wacker Cyclization to Access β‐Stereogenic γ‐Lactams

Yi Ding, Ye‐Qiang Han, Le‐Song Wu, Tao Zhou, Qi‐Jun Yao, Ya‐Lan Feng, Ya Li, Ke‐Xin Kong, Bing‐Feng Shi

2020Angewandte Chemie International Edition71 citationsDOI

Abstract

Abstract Herein, we describe an unprecedented cascade reaction to β‐stereogenic γ‐lactams involving Pd(II)‐catalyzed enantioselective aliphatic methylene C(sp 3 )−H alkenylation–aza‐Wacker cyclization through syn ‐aminopalladation. Readily available 3,3′‐substituted BINOLs are used as chiral ligands, providing the corresponding γ‐lactams with broad scope and high enantioselectivities (up to 98 % ee ).

Topics & Concepts

StereocenterEnantioselective synthesisMethyleneChemistryStereochemistryTandemCatalysisCascade reactionCombinatorial chemistryMedicinal chemistryOrganic chemistryComposite materialMaterials scienceCatalytic C–H Functionalization MethodsSynthesis and Catalytic ReactionsAsymmetric Hydrogenation and Catalysis
Pd(II)‐Catalyzed Tandem Enantioselective Methylene C(sp<sup>3</sup>)−H Alkenylation–Aza‐Wacker Cyclization to Access β‐Stereogenic γ‐Lactams | Litcius