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Phosphorylation Organocatalysts Highly Active by Design

Amit Fallek, Mor Weiss-Shtofman, M. S. Kramer, Roman Dobrovetsky, Moshe Portnoy

2020Organic Letters17 citationsDOI

Abstract

The activity of nucleophilic organocatalysts for alcohol/phenol phosphorylation was enhanced through attaching oligoether appendages to a benzyl substituent on imidazole- or aminopyridine-based active units, presumably because of stabilizing n–cation interactions of the ethereal oxygens with the positively charged aza-heterocycle in the catalytic intermediates, and was substantially higher than that of known benchmark catalysts for a range of substrates. Density functional theory calculations and the study of analogues having a lower potential for such stabilizing interactions support our hypothesis.

Topics & Concepts

ChemistrySubstituentNucleophileImidazoleCatalysisPhosphorylationCombinatorial chemistryDensity functional theoryStereochemistryOrganic chemistryComputational chemistryBiochemistryChemical Synthesis and AnalysisAsymmetric Synthesis and CatalysisOrganophosphorus compounds synthesis
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