3-(2-Methoxyethyl)-2,3,4,5-tetrahydro-1h-3-benzazepin-7-amine → 5-Chloro-N(4)-[2-fluoro-6-(tetrahydro-furan-3-ylmethoxy)-phenyl]-N(2)-[3-(2-methoxy-ethyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl]-pyrimidine-2,4-diamine

関与物質

反応手順

5-Chloro-N(4)-[2-fluoro-6-(tetrahydro-furan-3-ylmethoxy)-phenyl]-N(2)-[3-(2-methoxy-ethyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl]-pyrimidine-2,4-diamine was prepared from 3-(2-Methoxy-ethyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ylamine and (2,5-Dichloro-pyrimidin-4-yl)-[2-fluoro-6-(tetrahydro-furan-3-ylmethoxy)-phenyl]-amine in an analogous manner to Example 1221d. Title compound was isolated as a white solid (90 mg, 62%) HPLC purity=99%, LCMS=542.21 (M+H), 1H-NMR (DMSO-d6, 400 MHz) δ 9.63 (bs, 1H), 9.28 (s, 1H), 8.49 (s, 1H), 8.09 (s, 1H), 7.40-7.34 (m, 1H0, 7.26 (s, 1H), 7.13 (d, J=7.7 Hz, 1H), 7.02-6.93 (m, 2H), 6.85 (d, J=8.5 Hz, 1H), 3.92-3.85 (m, 2H), 3.71-3.69 (m, 1H), 3.63-3.52 (m, 6H), 3.41-3.23 (m, 7H), 3.12-2.82 (m, 6H), 1.82-1.77 (m, 1H), 1.50-1.46 (m, 1H).

情報源と証拠