Nickel-Catalyzed Amination of Aryl Chlorides and Sulfamates in 2-Methyl-THF.

Nickel-Catalyzed Amination of Aryl Chlorides and Sulfamates in 2-Methyl-THF.
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DOI:
10.1021/cs501045v
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发表时间:
2014-09-05
期刊:
影响因子:
12.9
通讯作者:
Garg, Neil K.
Garg, Neil K.
中科院分区:
化学1区
文献类型:
--
作者:
Nathel, Noah F. Fine;Kim, Junyong;Hie, Liana;Jiang, Xingyu;Garg, Neil K.

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本文报道了以镍为催化剂,用绿色溶剂2-甲基-四氢呋喃进行芳基O-氨基磺酸酯和氯化物的胺化反应。该方法使用市售的和空气稳定的预催化剂NiCl 2(DME),范围广,并且以合成有用的产率提供了获得芳基胺的途径。这种方法的实用性是强调的例子进行的催化剂负载低至1摩尔%的镍克规模的耦合。此外,所描述的镍催化的胺化耐受杂环,并且应该证明可用于合成药物候选物和其它含杂原子的化合物。
The nickel-catalyzed amination of aryl O-sulfamates and chlorides using the green solvent 2-methyl-THF is reported. This methodology employs the commercially available and air-stable precatalyst NiCl2(DME), is broad in scope, and provides access to aryl amines in synthetically useful yields. The utility of this methodology is underscored by examples of gram-scale couplings conducted with catalyst loadings as low as 1 mol % nickel. Moreover, the nickel-catalyzed amination described is tolerant of heterocycles and should prove useful in the synthesis of pharmaceutical candidates and other heteroatom-containing compounds.
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