Synthesis of substituted isoquinolines utilizing palladium-catalyzed α-arylation of ketones

Synthesis of substituted isoquinolines utilizing palladium-catalyzed α-arylation of ketones
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DOI:
10.1073/pnas.1206532109
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发表时间:
2012-07-17
影响因子:
11.1
通讯作者:
Bassuto, Jose A.
Bassuto, Jose A.
中科院分区:
综合性期刊1区
文献类型:
--
作者:
Donohoe, Timothy J.;Pilgrim, Ben S.;Bassuto, Jose A.

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利用连续的钯催化的α-芳基化和环化反应提供了一系列异喹啉及其相应的N-氧化物的一般方法。该方法允许以区域选择性方式和优异的总产率收敛组合容易获得的前体。这种强大的多取代异喹啉路线,不限于富电子部分,也允许快速获得生物活性化合物的类似物。
The utilization of sequential palladium-catalyzed alpha-arylation and cyclization reactions provides a general approach to an array of isoquinolines and their corresponding N-oxides. This methodology allows the convergent combination of readily available precursors in a regioselective manner and in excellent overall yields. This powerful route to polysubstituted isoquinolines, which is not limited to electron rich moieties, also allows rapid access to analogues of biologically active compounds.