7-Amino-5,5-dimethyl-1,3,4,5-tetrahydro-benzo[b]azepin-2-one → 2-[5-Chloro-2-(5,5-dimethyl-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-7-ylamino)-pyrimidin-4-ylamino]-N-methyl-4-nitro-benzamide

Participants

Reaction Steps

2-[5-Chloro-2-(5,5-dimethyl-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-7-ylamino)-pyrimidin-4-ylamino]-N-methyl-4-nitro-benzamide was prepared from 2-(2,5-Dichloro-pyrimidin-4-ylamino)-N-methyl-4-nitro-benzamide and 7-Amino-5,5-dimethyl-1,3,4,5-tetrahydro-benzo[b]azepin-2-one in an analogous manner to Example 1221d. The product was isolated as an orange-yellow solid. 88% HPLC purity, LCMS 510.21, MP 247-248, 1H-NMR (CDCl3, 400 MHz) δ: 11.19 (s, 1H), 9.57 (s, 1H), 8.20 (s, 1H), 7.88 (d, J=6.6 Hz, 1H), 7.66 (d, J=8.3 Hz, 1H), 7.59 (d, J=8.8 Hz, 1H), 7.37 (s, 1H), 7.06 (s, 1H), 6.97 (s, 1H), 6.84 (d, J=8.3 Hz, 1H), 6.30 (m, 1H), 3.10 (d, J=4.8 Hz, 3H), 2.41 (t, J=6.8 Hz, 2H), 2.10 (t, J=7.1 Hz, 2H), 1.40 (s, 6H).

Provenance & Evidence