8-Amino-1,3,4,5-tetrahydro-2H-1-benzazepin-2-one → 2-[5-Chloro-2-(2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-8-ylamino)-pyrimidin-4-ylamino]-3-fluoro-N-methyl-benzamide

Participants

Reaction Steps

2-[5-Chloro-2-(2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-8-ylamino)-pyrimidin-4-ylamino]-3-fluoro-N-methyl-benzamide was prepared from 8-amino-1,3,4,5-tetrahydro-benzo[b]azepin-2-one and 2-(2,5-dichloro-pyrimidin-4-ylamino)-3-fluoro-N-methyl-benzamide in an analogous manner to Example 308c. Product isolated as a yellow solid (67 mg, 32%). m.p.=180-190° C.; LCMS (m/e) 455 (M+H); 1H-NMR (d6-DMSO, 400 MHz) δ 9.35-9.22 (m, 3H), 8.56-8.47 (m, 1H), 8.17 (s, 1H), 7.50-7.42 (m, 2H), 7.40-7.31 (m, 1H), 7.23 (d, 1H, J=8.3 Hz) 7.09 (s, 1H), 6.93 (d, 1H, J=8.3 Hz), 2.72 (d, 3H, J=4.4 Hz), 2.56 (t, 2H, J=6.2 Hz), 2.12-1.97 (m, 4H).

Provenance & Evidence