Litcius/Paper detail

Nickel-Catalyzed Enantioselective C(sp<sup>3</sup>)–C(sp<sup>3</sup>) Cross-Electrophile Coupling of <i>N</i>-Sulfonyl Styrenyl Aziridines with Alkyl Bromides

Yun Lan, Qiaoying Han, Pingyong Liao, Ruijia Chen, Fan Fei, Xuejun Zhao, Wenbin Liu

2024Journal of the American Chemical Society33 citationsDOI

Abstract

Herein, we report the first example of a highly enantioselective alkylative aziridine ring opening. Under the catalysis of a chiral nickel/pyridine-imidazoline complex, asymmetric C(sp 3 )–C(sp 3 ) cross-electrophile coupling between racemic N -sulfonyl styrenyl aziridines and readily available primary alkyl bromides furnishes a variety of highly enantioenriched phenethylamine derivatives with complete regiocontrol and good functional group tolerance. Preliminary mechanistic studies support a reaction pathway consisting of regioselective iodolysis of aziridines in situ and subsequent enantioconvergent coupling of the generated β-amino benzyl iodides with alkyl bromides.

Topics & Concepts

ChemistryEnantioselective synthesisAziridineNickelCatalysisElectrophilePyridineSulfonylMedicinal chemistryAlkylStereochemistryRing (chemistry)Organic chemistrySynthesis and Catalytic ReactionsCatalytic C–H Functionalization MethodsAsymmetric Synthesis and Catalysis