Acetic Acid → HCID 57974325, compound

Participants

Reaction Steps

A mixture of HATU (197 mg), diisopropylethylamine (90 μl), acetic acid (22 μl) and N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(methylamino)ethoxy]quinazolin-4-amine (150 mg) in DCM (20 ml) was stirred for 2 hours. The solution washed with water, then brine and concentrated in vacuo. The residue was purified by chromatography using DCM—5% methanol as eluent to give the title compound as a white solid (114 mg, 69%); NMR spectrum (DMSO-d6) 1.95 (s, 3H), 3.00 (s, 3H), 3.89 (t, 2H), 4.48 (m, 2H), 5.29 (s, 2H), 7.18 (d, 1H), 7.24 (d, 1H), 7.35 (m, 2H), 7.59 (m, 2H), 7.72 (dd, 1H), 7.85 (dt, 1H), 7.96 (d, 1H), 8.46 (s, 1H), 8.58 (m, 1H), 9.70 (bs, 1H); Mass spectrum MH+ 478.5.

Provenance & Evidence