Convenient Access to Di‐ and Trifluoroethylamines for Lead Structure Research (Eur. J. Org. Chem. 5/2016). Issue 5 (February 2016) - Deutsch, Amrei
Abstract : The cover picture shows an easy and reliable approach towards the synthesis of novel carboxamide surrogates for lead structure research. Di‐ or trifluoroethylamines might represent missing puzzle pieces in the search for hydrolytically stable amide bioisosteres, and their convenient preparation is reported starting from di‐ and trifluoromethylated N ‐aryl N, O ‐acetal precursors. Nucleophilic addition of Grignard reagents or heteroatom nucleophiles allows a flexible, yet simple access to various functionalized di‐ and trifluoromethylated amines. Details are discussed in the article by C. Deutsch, A. Hoffmann‐Röder et al. on p.930 ff .