The first reverse regioselective intermolecular annulation of aryl substituted 2-acetylenic ketones with O-substituted N-hydroxybenzamides or acrylamides followed by tandem cyclization via ruthenium-catalyzed C–H activation, is reported. Excellent reverse selectivity of alkyne insertion was induced by the weak coordination between the carbonyl group and ruthenium complex. This highly efficient and practical reaction has a broad range of substrate scope with excellent functional-group tolerance. The tandem reaction provides a wide range of polycyclic products that have an indozilidine structural motif, and are found to potentially be synthetically and pharmaceutically valuable.
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机译:芳基取代的2-炔酮与 O em>-取代的 N em>-羟基苯甲酰胺或丙烯酰胺的第一次区域选择性分子间环化,然后通过 em>钌-进行串联环化据报道催化了CH的活化。羰基和钌配合物之间的弱配位作用导致了炔烃插入的优异反向选择性。这种高效,实用的反应具有广泛的底物范围,具有出色的官能团耐受性。串联反应提供了具有吲唑烷结构基序的多种多环产物,并且发现它们具有潜在的合成和药学价值。
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