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Asymmetric Synthesis of Nortropanes <i>via</i> Rh-Catalyzed Allylic Arylation

Yan Zhang, F. Wieland Goetzke, Kirsten E. Christensen, Stephen P. Fletcher

2022ACS Catalysis12 citationsDOIOpen Access PDF

Abstract

an unexpected kinetic resolution, and the resolved enantiopure allyl chloride can undergo highly enantiospecific reactions with N-, O-, and S-containing nucleophiles. The method was applied in a highly stereoselective formal synthesis of YZJ-1139(1), a potential insomnia treatment that recently completed Phase II clinical trials. Our report represents an asymmetric catalytic method for the synthesis of YZJ-1139(1) and related compounds.

Topics & Concepts

Enantiopure drugAllylic rearrangementChemistryEnantioselective synthesisCatalysisKinetic resolutionArylNucleophileAllyl chlorideStereoselectivityCombinatorial chemistryTropaneChlorideStereochemistryOrganic chemistryAlkylChemical synthesis and alkaloidsCyclopropane Reaction MechanismsCatalytic C–H Functionalization Methods
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