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Highly Enantioselective CuAAC of Functional Tertiary Alcohols Featuring an Ethynyl Group and Their Kinetic Resolution

Kui Liao, Yi Gong, Ren‐Yi Zhu, Cai Wang, Feng Zhou, Jian Zhou

2020Angewandte Chemie International Edition74 citationsDOI

Abstract

-catalyzed azide-alkyne cycloaddition (CuAAC) of tertiary alcohols and their kinetic resolution is reported. This approach allows facile access to multifunctional tertiary alcohols featuring an α-ethynyl or α-triazole moiety, and represents the first successful kinetic resolution of racemates with a tetrasubstituted carbon stereocenter via CuAAC. Newly developed pyridinebisoxazoline (PYBOX) ligands with a C4 phosphonate group play a key role.

Topics & Concepts

StereocenterEnantioselective synthesisKinetic resolutionMoietyCycloadditionChemistryPhosphonateCombinatorial chemistryAzideStereochemistryTertiary alcoholsCatalysisOrganic chemistryClick Chemistry and ApplicationsSynthesis and Catalytic ReactionsCyclopropane Reaction Mechanisms
Highly Enantioselective CuAAC of Functional Tertiary Alcohols Featuring an Ethynyl Group and Their Kinetic Resolution | Litcius