Tetrafluoro-m-phenylenediamine dihydrochloride → (6-{7-[3-(Morpholine-4-sulfonyl)-phenyl]-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino}-1H-benzoimidazol-2-yl)-methanol

Participants

Reaction Steps

(6-{7-[3-(Morpholine-4-sulfonyl)-phenyl]-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino}-1H-benzoimidazol-2-yl)-methanol was prepared from 7-[3-(morpholine-4-sulfonyl)-phenyl]-pyrrolo[2,1-f][1,2,4]triazin-2-ol and (6-amino-1H-benzoimidazol-2-yl)-methanol; dihydrochloride in an analogous manner to Example 1052a. Product isolated as a yellow solid (31 mg, 21%). m.p.=232-237° C.; LCMS (m/e) 506 (M+H); 1H-NMR (d6-DMSO, 400 MHz) δ 12.05 (bs, 1H), 9.40 (s, 1H), 9.03 (s, 1H), 8.72 (d, 1H, J=7.8 Hz), 8.28 (s, 1H), 7.86-7.74 (m, 2H), 7.72 (d, 1H, J=7.8 Hz), 7.55 (d, 1H, J=8.7 Hz), 7.46 (d, 1H, J=8.7 Hz), 7.29 (d, 1H, J=4.8 Hz), 6.97 (d, 1H, J=4.8 Hz), 4.66 (s, 2H), 3.62-3.55 (m, 4H), 2.93-2.86 (m, 4H).

Provenance & Evidence