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A Facile Synthesis of N-Aryl Substituted Piperidones
Authors:GENG  Qian  ZHANG  Hui  CAO  Weiguo  CHEN  Yalia
Institution:1. Department of Chemistry,Shanghai University,99 Shangda Lu,Shanghai 200444,China.
2. Department of Chemistry,Shanghai University,99 Shangda Lu,Shanghai 200444,China;State Key Laboratory of Organometallic Chemistry,Shanghai Institute of Organic Chemistry,Chinese Academy of Science,Shanghai 200032,China; Key Laboratory of Organofluorine Ch
Abstract:A general and efficient procedure for the synthesis of N‐aryl‐substituted 4‐piperidones was developed. The two step syntheses proceeded with an overall yield of 60%‐83% using L‐proline as the ligand for the Cu(I)‐catalyzed Ullmann amination followed by subsequent hydrolysis of resulting ketals.
Keywords:N-aryl 4-piperidone  Ullmann amination  ligand  copper(I) iodide
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