反应详情

N-[3-Chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(ethylamino)ethoxy]quinazolin-4-amine (58 mg) in DCM (3 ml) was treated with acetyl chloride (15 mg) and DIPEA (39 mg) and stirred overnight. The solution was purified by chromatography using DCM to 10% 7N ammonia in methanol in DCM to give after trituration with diethyl ether N-{2-[(4-{[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino}quinazolin-5-yl)oxy]ethyl}-N-ethylacetamide (39 mg, 61%); NMR spectrum (DMSO-d6) 1.12 (t, 3H), 1.98 (s, 3H), 3.37-3.42 (m, 2H), 3.87 (t, 2H), 4.39 (t, 2H), 5.31 (s, 2H), 7.16 (d, 1H), 7.22-7.28 (m, 1H), 7.33-7.39 (m, 2H), 7.55-7.61 (m, 2H), 7.71-7.75 (m, 1H), 7.87-7.91 (m, 1H), 7.94 (d, 1H), 8.45 (s, 1H), 8.61 (d, 1H), 9.80 (s, 1H); Mass spectrum MH+ 492.

1. customThe solution was purified by chromatography