Potassium Iodide → HCID 58529355, compound

Participants

Reaction Conditions

Reaction Steps

A solution of 5-(2-benzyl-2H-indazol-6-yl)-7-morpholin-2-ylpyrrolo[2,1-f][1,2,4]triazin-4-amine (247 mg, 0.521 mmol) in DMF (5 mL) was treated with 2-chloro-N,N-dimethylacetamide (115 mg, 0.94 mmol), potassium carbonate (658 mg, 4.8 mmol) and potassium iodide (19 mg, 0.12 mmol) and the mixture vigorously stirred at 60° C. for 18 h. Basic, aqueous workup and purification by column chromatography (CH2Cl2:MeOH:NH3) gave 312 mg (50%) of the desired compound. 1H NMR (300 MHz, DMSO-d6) δ 7.89 (s, 1 H), 7.76 (dd, 1 H, J=9, 1 Hz), 7.53 (s, 1H), 7.25 to 7.36 (m, 3H), 7.18-7.23 (m, 2H), 7.09 (d, 1 H, J=9 Hz), 6.60 (s, 1H), 5.63 (s, 2H), 3.14 (s, 2H), 3.03 (s, 3H), 2.89-2.94 (m, 2H), 2.80 (s, 3H), 2.62 (s, 3H), 2.12-2.24 (m, 2H), 1.93-2.03 (m, 2H), 1.63-1.79 (m, 2H); ES-MS m/z 523.2 [M+H]+, HPLC RT (min) 2.21.

Provenance & Evidence