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

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Reaction Steps

2-[5-Chloro-2-(1-methyl-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-7-ylamino)-pyrimidin-4-ylamino]-N-prop-2-ynyl-benzamide was prepared from 7-amino-1-methyl-1,3,4,5-tetrahydro-1-benzazepin-2-one and 2-(2,5-dichloro-pyrimidin-4-ylamino)-N-prop-2-ynyl-benzamide in an analogous manner to Example 308c. Product isolated as a white solid (79 mg, 48%). m.p.=193-194° C.; LCMS (m/e) 475 (M+H); 1H-NMR (CDCl3, 400 MHz) δ 10.97 (s, 1H), 8.66 (d, 1H, J=8.4 Hz), 8.14 (s, 1H), 7.57 (d, 1H, J=7.8 Hz), 7.54-7.42 (m, 3H), 7.19-7.09 (m, 2H), 6.95 (s, 1H), 6.34 (bs, 1H), 4.33-4.27 (m, 2H), 3.36 (s, 3H), 2.74-2.64 (m, 2H), 2.38-2.30 (m, 3H), 2.22-2.12 (m, 2H).

Provenance & Evidence