Asymmetric synthesis of 2-arylpiperazines
Asymmetric synthesis of 2-arylpiperazines
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DOI：
10.1016/j.bmcl.2014.10.047
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发表时间：
2014-12-15
影响因子：
2.7
通讯作者：
Tanaka, Hiroshi
中科院分区：
文献类型：
--
作者：
Yokoshima, Satoshi;Watanabe, Kazutoshi;Tanaka, Hiroshi
建立了以苯基溴化物为起始原料的2-芳基哌嗪的不对称合成方法，该方法种类繁多，易于获得。该合成的特征在于苯基溴的CBS还原以提供光学富集物，1，2，3-恶唑烷2-氧化物与构型颠倒的叠氮阴离子的S(N)2反应，以及通过哌嗪-2，3-二酮的还原构建哌嗪环。(C)2014爱思唯尔有限公司。保留所有权利。
An asymmetric synthesis of 2-arylpiperazines starting from phenacyl bromides, a variety of which are easily available, has been established. The synthesis features a CBS reduction of phenacyl bromide to provide optically enriched compounds, an S(N)2 reaction of 1,2,3-oxathiazolidine 2-oxides with an azide anion with invert of configuration, and construction of the piperazine ring via reduction of piperazine-2,3-diones. (C) 2014 Elsevier Ltd. All rights reserved.