5-Amino-2-(trifluoromethyl)benzimidazole → [7-(3-Cyclopropylmethanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-(2-trifluoromethyl-3H-benzimidazol-5-yl)-amine

Beteiligte Stoffe

Reaktionsschritte

Following the synthetic and purification procedures described in Example 1293d, 7-(3-cyclopropylmethanesulfonyl-phenyl)-2-methylsulfanyl-pyrrolo[2,1-f][1,2,4]triazine (75 mg, 0.20 mmol) was coupled with 2-trifluoromethyl-3H-benzimidazol-5-ylamine (68.3 mg, 0.340 mmol) at 105° C. for 86 h to afford the title compound. Yield of TFA salt: 25 mg (22%) of brown powder; LC/MS: 513 (M+H); HPLC: 97% pure, RT=3.43 min; 1H NMR: (DMSO, δ) 9.60 (s, 1H), 8.97 (s, 1H), 8.53 (d, J=7.9, 1H), 8.41 (s, 1H), 7.90 (s, 1H), 7.81 (d, J=7.9, 1H), 7.70 (m, 2H), 7.60 (d, J=8.8, 1H), 7.21 (d, J=4.8, 1H), 6.91 (d, J=4.8, 1H), 3.20 (d, J=7.2, 2H), 0.77 (m, 1H), 0.32 (m, 2H), −0.01 (m, 2H).

Herkunft & Nachweise