Synthesis of 2-substituted piperazines via direct α-lithiation
Synthesis of 2-substituted piperazines via direct α-lithiation
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DOI：
10.1016/j.tetlet.2005.02.085
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发表时间：
2005-04-04
影响因子：
1.8
通讯作者：
van Maarseveen, JH
中科院分区：
文献类型：
--
作者：
Berkheij, M;van der Sluis, L;van Maarseveen, JH
描述了一种新的有效的合成路线朝向药学相关的2-取代哌嗪类。关键步骤包括N-Boc哌嗪的α-锂化，然后与几种亲电试剂反应。为了获得高产率，在某些情况下，需要在锂化步骤之后将金属过渡到铜。(c)2005爱思唯尔有限公司保留所有权利。
A novel efficient synthetic route towards the pharmaceutically relevant 2-substituted piperazine class is described. The key step involves alpha-lithiation of N-Boc piperazines, followed by reaction with several electrophiles. To obtain high yields, in some cases transmetallation to copper after the lithiation step is required. (c) 2005 Elsevier Ltd. All rights reserved.