Abstract
An efficient synthesis of 1,3-/1,1-dialkoxy 1,2-dihydroisoquinolines from o-ethynylbenzacetals and sulfonyl azides via a cascade process combining copper-catalyzed alkyne-azide cycloaddition (CuAAC), Dimroth rearrangement, 1,5-OR shift/1,5-H shift, and 6Ï-electrocyclic ring closure (6Ï-ERC) is described. Extension of the produced 1,3-dialkoxy-1,2-dihydroisoquinolines to isoquinolium salts is also disclosed.
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