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Reagents and conditions: (i) NaH, NCCH2CO2Et, DMF, 0 °C to rt and then 40 or 41, 2 h, rt, 48%; (ii) Zn/AcOH, 95 °C, 1 h 15 min, 88%; (iii) formamide, ammonium formate, 170 °C, 18 h, 45%; (iv) POCl3, 75 °C, 18 h, 100%; (v) amine, TEA, DMF, 120 °C, 1 h, microwave and then 4 M HCl, dioxane/MeOH, 2.5 h, 3–46%; (vi) amine, TEA, NMP, 140 °C, microwave and then MP-TsOH column, 29%.
