HIGHLIGHTS
SUMMARY
Arylation of carbon-(sp3) (pro)nucleophiles is most commonly achieved using transition metal-catalyzed reactions of aryl halides. But from a conceptual standpoint, a nucleophilic aromatic substitution (SNAr) reaction between a carbon (pro)nucleophile 12 and an aryl electrophile 11 also appears a viable strategy for the direct arylation of acidic C(sp3)-H bonds (Scheme 1, strategy 2a′). The electronic versatility of these reactions, which do not require electron-deficient aryl electrophiles, arises from substrate activation by an often underappreciated but crucial determiner of molecular reactivity: conformational control (Scheme 1, strategy 2a″). Conformational . . .
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