Regiochemical control in the amination reaction of phenanthridine-7,10-quinones
Regiochemical control in the amination reaction of phenanthridine-7,10-quinones
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DOI：
10.1016/j.tetlet.2009.05.042
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发表时间：
2009-07-29
影响因子：
1.8
通讯作者：
Andrea Ibacache, J.
中科院分区：
文献类型：
--
作者：
Valderrama, Jaime A.;Andrea Ibacache, J.
描述了取代的菲啶-7,10-醌与胺反应构建新型氨基菲啶醌衍生物作为抗肿瘤剂。胺化反应的区域化学根据醌环上远程取代基的诱导和空间效应进行讨论，这些效应控制胺穿过醌双键的共轭加成方向。据报道，一些获得的氨基醌具有显着的体外抗肿瘤活性。 (C) 2009 Elsevier Ltd. 保留所有权利。
The reaction of substituted phenanthridine-7,10-quinones with amines to construct novel aminophenanthridinequinone derivatives as antitumor agents is described. The regiochemistry of the amination reaction is discussed in terms of inductive and steric effects of remote substituents to the quinone ring, which Control the direction of the conjugate addition of the amines across the quinone double bond. Evidences on the significant in vitro antitumor activities of some of the obtained aminoquinones, are reported. (C) 2009 Elsevier Ltd. All rights Reserved.