A Metal-Free Tandem Demethylenation/C(sp<sup>2</sup>)–H Cycloamination Process of <i>N</i>‑Benzyl-2-aminopyridines via C–C and C–N Bond Cleavage

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    Abstract

    A mild, metal-free synthesis of pyrido[1,2-<i>a</i>]benzimidazoles starting with <i>N</i>-benzyl-2-aminopyridines, which employs PhI(OPiv)<sub>2</sub> as a stoichiometric oxidant, has been developed. The process is initiated by an unusual PhI(OPiv)<sub>2</sub>-mediated <i>ipso</i> S<sub>E</sub>Ar reaction, followed by solvent-assisted C–C and C–N bond cleavage

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      Last time updated on 12/02/2018