Wiehn Matthias S, Fürniss Daniel, Bräse Stefan
Institut fur Organische Chemie, Karlsruhe Institute of Technology, Fritz-Haber-Weg 6, 76131 Karlsruhe, Germany.
J Comb Chem. 2009 Nov-Dec;11(6):982-1006. doi: 10.1021/cc9000899.
Three small compound biaryl libraries featuring a novel fluorinating cleavage strategy for preparation of a difluoromethyl group were assembled on solid supports. The average reaction yield per step was up to 96% in a synthetic sequence over five to six steps. Key features were Suzuki coupling reactions, transesterification with potassium cyanide and amidation reaction with trimethyl aluminum on solid supports.
在固体载体上构建了三个具有用于制备二氟甲基的新型氟化裂解策略的小型复合联芳基文库。在五到六个步骤的合成序列中,每步的平均反应产率高达96%。关键特征包括在固体载体上进行的铃木偶联反应、与氰化钾的酯交换反应以及与三甲基铝的酰胺化反应。