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Merck

Accessing the Ene-Imine Motif in 1H-Isoindole, Thienopyrrole, and Thienopyridine Building Blocks.

ACS omega (2020-09-22)
Brandon C Fillmore, Jayden Price, Ryan Dean, Amy A Brown, Andreas Decken, Sara Eisler
RÉSUMÉ

A pathway to a range of diverse heterocycles was developed using a nucleophilic cyclization strategy. Lactams and ene-imines are accessed in a few steps from a common precursor, and these moieties are further elaborated to directly provide pyrroles or pyridines with extended conjugation. Reaction conditions are mild, and a broad range of structural types are available within a few steps.

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Sigma-Aldrich
4-Bromo-3-thiophenecarboxylic acid, 97%