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New Chiral Reagent for Installation of Pharmacophoric (S)‐ or (R)‐2‐(Alkoxyphosphono)‐1‐amino‐2,2‐difluoroethyl Groups
Authors:Chen Xie  Lijun Zhang  Dr. Haibo Mei  Dr. Romana Pajkert  Dr. Maksym Ponomarenko  Dr. Yi Pan  Prof. Dr. Gerd‐Volker Röschenthaler  Prof. Dr. Vadim A. Soloshonok  Dr. Jianlin Han
Affiliation:1. School of Chemistry and Chemical Engineering, State Key Laboratory of Coordination Chemistry, Nanjing University, Nanjing, P. R. China;2. Department of Life Sciences and Chemistry, Jacobs University Bremen gGmbH, Bremen, Germany;3. Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, San Sebastián, Spain;4. IKERBASQUE, Basque Foundation for Science, Bilbao, Spain
Abstract:A new chiral reagent has been developed for generalized installation of pharmacophoric (S)‐ or (R)‐2‐(alkoxyphosphono)‐1‐amino‐2,2‐difluoroethyl group into organic compounds. The original synthetic application of this new reagent is exemplified by Friedel–Crafts reactions with indoles, which proceed efficiently with excellent diastereoselectivity to give enantiomerically pure products.
Keywords:asymmetric synthesis  Friedel–  Crafts  imine  indoles  synthetic methods
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