手性催化不对称 Pictet-Spengler 型反应合成具有光学活性的吲哚并[3,4-cd][1]苯并氮杂卓。
Catalytic asymmetric Pictet-Spengler-type reaction for the synthesis of optically active indolo[3,4-cd][1]benzazepines.
机构信息
Joint Laboratory of Green Synthetic Chemistry, Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, China.
出版信息
Org Lett. 2011 Oct 21;13(20):5636-9. doi: 10.1021/ol202361t. Epub 2011 Sep 26.
A new strategy has been introduced to develop a catalytic asymmetric Pictet-Spengler-type reaction by replacing the aldehyde with an imine. A range of 4-(2-aminoaryl)indoles smoothly undergo the chiral phosphoric acid catalyzed asymmetric Pictet-Spengler-type reaction with imines at room temperature to give structurally diverse indolo[3,4-cd][1]benzazepines in good to excellent yields and ee.
一种新的策略被引入，通过用亚胺取代醛，来开发催化不对称的Pictet-Spengler 型反应。一系列 4-(2-芳基氨基)吲哚在室温下与亚胺在手性磷酸的催化下顺利地进行不对称的 Pictet-Spengler 型反应，以良好至优异的收率和对映选择性得到结构多样的吲哚并[3,4-cd][1]苯并氮杂卓。
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