Novel, One-Pot Procedure for the Synthesis of 2-Arylethanol Derivatives

Novel, One-Pot Procedure for the Synthesis of 2-Arylethanol Derivatives
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合成 2-芳基乙醇衍生物的新型一锅法

DOI:
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发表时间:
2008
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通讯作者:
B. Wünsch
B. Wünsch
中科院分区:
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文献类型:
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作者:
T. Schläger;C. Oberdorf;B. Tewes;B. Wünsch

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描述了使用硫酸乙烯酯作为C 2 结构单元的2-芳基乙醇衍生物的有效一锅法合成。通过捕获通过卤素-金属交换或用硫酸乙烯酯直接金属化产生的芳基锂中间体,可以获得高产率。所得杂芳基或苯基乙醇衍生物代表了通过 oxa-Pictet-Spengler 反应合成环状吡喃衍生物的通用结构单元。
An efficient one-pot synthesis of 2-arylethanol derivatives using ethylene sulfate as a C 2 building block is described. High yields are obtained upon trapping of aryllithium intermediates generated by halogen-metal exchange or directed metalation with ethylene sulfate. The resulting heteroaryl or phenylethanol derivatives represent versatile building blocks for the synthesis of annulated pyran derivatives by oxa-Pictet-Spengler reaction.