Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) → 4-chloro-N-cyclopentyl-2-fluoro-5-[4-(3-fluorophenyl)-4-[2-[(1R,5S)-3-(2-methylbenzimidazol-1-yl)-8-azabicyclo[3.2.1]octan-8-yl]ethyl]piperidine-1-carbonyl]benzenesulfonamide

関与物質

反応手順

0.103 g (0.23 mmol) 1-((1R,5S)-8-{2-[4-(3-fluorophenyl)piperidin-4-yl]ethyl}-8-azabicyclo[3.2.1]oct-3-yl)-2-methyl-1H-benzimidazole and 0.148 g (0.46 mmol) 2-chloro-4-fluoro-5-[(cyclopentylamino)sulfonyl]benzoic acid were combined following the HATU general procedure in Example 5. This compound was purified by reverse phase chromatography on a 0-100% gradient of 0.1% TFA in water in acetonitrile. 0.068 g obtained (40% yield). 1H NMR (300 MHz, DMSO-d6) δ 9.32-9.49 (br, 1H), 8.13-8.25 (m, 2H), 7.73-7.91 (m, 3H), 7.39-7.56 (m, 2H), 7.08-7.30 (m, 3H), 5.00-5.15 (m, 1H), 4.03-4.16 (m, 2H), 3.83-4.02 (m, 1H), 3.35-3.58 (m, 2H), 3.19-3.33 (m, 2H), 3.16 (s, 1H), 2.94-3.08 (m, 2H), 2.67-2.80 (m, 6H), 2.54-2.65 (m, 1H), 2.02-2.26 (m, 8H), 1.72-2.01 (m, 2H), 1.47-1.67 (m, 4H), 1.26-1.44 (m, 4H)

情報源と証拠