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aReagents and conditions: (a) 3-carboxyphenylboronic acid, 1 mol% Pd2(dba)3, 2 mol% PCy3, K3PO4, dioxane, 100 °C (microwave), 1 h, then aq. HCl, 99%; (b) pentafluorophenyl trifluoroacetate, N(i-Pr)2Et, CH2Cl2, 0 °C to rt, 1 h, 81%; (c) primary amines, N(i-Pr)2Et, CH2Cl2, rt, 1 h; (d) TFA, CH2Cl2, rt, 30 min., 100 ~ 56% (over 2 steps).
