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Continuous Synthesis of Aryl Amines from Phenols Utilizing Integrated Packed-Bed Flow Systems.
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2020-07-09 , DOI: 10.1002/anie.202005109 Tomohiro Ichitsuka 1 , Ikko Takahashi 1 , Nagatoshi Koumura 1 , Kazuhiko Sato 1 , Shū Kobayashi 1
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2020-07-09 , DOI: 10.1002/anie.202005109 Tomohiro Ichitsuka 1 , Ikko Takahashi 1 , Nagatoshi Koumura 1 , Kazuhiko Sato 1 , Shū Kobayashi 1
Affiliation
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Aryl amines are important pharmaceutical intermediates among other numerous applications. Herein, an environmentally benign route and novel approach to aryl amine synthesis using dehydrative amination of phenols with amines and styrene under continuous‐flow conditions was developed. Inexpensive and readily available phenols were efficiently converted into the corresponding aryl amines, with small amounts of easily removable co‐products (i.e., H2O and alkanes), in multistep continuous‐flow reactors in the presence of heterogeneous Pd catalysts. The high product selectivity and functional‐group tolerance of this method allowed aryl amines with diverse functional groups to be selectively obtained in high yields over a continuous operation time of one week.
中文翻译：
利用集成床流系统从苯酚连续合成芳胺。
芳胺是其他众多应用中的重要药物中间体。在此，开发了在连续流动条件下使用苯酚与胺和苯乙烯的脱水胺化反应合成芳胺的环境友好途径和新方法。廉价且易于获得的苯酚在多相连续流反应器中，在多相钯催化剂的存在下，可与少量易除去的副产物（即H 2 O和烷烃）有效地转化为相应的芳基胺。这种方法的高产物选择性和官能团耐受性允许在一周的连续操作时间内以高收率选择性地获得具有各种官能团的芳基胺。
更新日期：2020-09-08
中文翻译：
利用集成床流系统从苯酚连续合成芳胺。
芳胺是其他众多应用中的重要药物中间体。在此，开发了在连续流动条件下使用苯酚与胺和苯乙烯的脱水胺化反应合成芳胺的环境友好途径和新方法。廉价且易于获得的苯酚在多相连续流反应器中，在多相钯催化剂的存在下，可与少量易除去的副产物（即H 2 O和烷烃）有效地转化为相应的芳基胺。这种方法的高产物选择性和官能团耐受性允许在一周的连续操作时间内以高收率选择性地获得具有各种官能团的芳基胺。
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