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Reagents and conditions: (i) PdCl2(PPh3)2, LiHMDS, THF, 135 °C, 20 min, 19%–22%; or when X = CH(tBu3P)2Pd(0), NaOtBu, toluene, 80 °C, 2 h, 45%; (ii) amine, NMP, 145 °C, 20 min, (26–41%); (iii) amine, NMP, 145 °C, 20 min, followed by TFA, CH2Cl2, 1 h, rt, or HCl, dioxane, MP-TsOH column (3–63%).
