4-methylsulfonyl-3-morpholin-4-ylaniline

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 7-(3-Chloro-phenyl)-2-methanesulfinyl-pyrrolo[2,1-f][1,2,4]triazine (126.9 mg, 0.0004350 mol), N,N-Diisopropylethylamine (0.114 mL, 0.000652 mol) and 4-Methanesulfonyl-3-morpholin-4-yl-phenylamine (223 mg, 0.000870 mol) were dissolved in 2-Methoxyethanol (3.05 mL) and The reaction was microwaved on 300 watts, 180° C. for 40 minutes or until HPLC showed consumption of starting material. LC/MS and NMR data showed that the solvent underwent addition to the sulfoxide rather than the aniline. The reaction mixture was then reduced en vacuo and 7.48 mg of 7-(3-Chloro-phenyl)-2-(2-methoxy-ethoxy)-pyrrolo[2,1-f][1,2,4]triazine was isolated and purified by Gilson prep HPLC. The product was then lyophilized to a powder. (M+H)=304.08. 1H NMR (400 MHz, DMSO, d6) δ 9.09 (s, 1H), 8.36 (s, 1H), 8.19 (d, 1H, J=7.88 Hz), 7.55 (t, 1H, J=7.97 Hz), 7.45 (m, 2H), 7.10 (d, 1H, J=4.84 Hz), 4.47 (m, 2H), 3.75 (m, 2H), 3.64 (s, 3H). The reaction was microwaved on 300 watts, 180° C. for 40 minutes or until HPLC consumption of starting material LC/MS and NMR data showed that the solvent underwent addition to the sulfoxide rather than the aniline