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Synthesis of Azepane Derivatives via Formal 1,3-Migration of Hydroxy and Acyloxy Groups and Selective Annulation

Zijuan Feng, Hongjian Jiao, Zihang Ye, Ye Jie, Ze‐Feng Xu, Shengguo Duan, Chuan‐Ying Li

2022Organic Letters12 citationsDOI

Abstract

Formal 1,3-migration of hydroxy and acyloxy groups initiated by α-imino rhodium carbene was achieved, and the following selective annulations of the corresponding zwitterions could efficiently afford azepane derivatives. Benefiting from a time-saving procedure as well as a good functional group tolerance, this unique migration–annulation protocol could provide an efficient tool for synthesizing seven-membered N-heterocycles. The plausible mechanism is discussed.

Topics & Concepts

AnnulationChemistryRhodiumFormal synthesisCombinatorial chemistryCarbeneFunctional groupStereochemistryTotal synthesisOrganic chemistryCatalysisPolymerCyclopropane Reaction MechanismsCatalytic C–H Functionalization MethodsSynthetic Organic Chemistry Methods
Synthesis of Azepane Derivatives via Formal 1,3-Migration of Hydroxy and Acyloxy Groups and Selective Annulation | Litcius