Methoxyacetic Acid → N-[(2R)-2-({4-[3-chloro-4-hydroxyanilino]quinazolin-5-yl}oxy)propyl]-2-methoxyacetamide

Participants

Reaction Steps

4-({5-[(1R)-2-Amino-1-methylethoxy]quinazolin-4-yl}amino)-2-chlorophenol was reacted with methoxyacetic acid using an analogous process to that described in Example 3 (preparation of starting materials) to give N-[(2R)-2-({4-[3-chloro-4-hydroxyanilino]quinazolin-5-yl}oxy)propyl]-2-methoxyacetamide in 83% yield; NMR spectrum (DMSO-d6) 1.4 (d, 3H), 3.1 (s, 3H), 3.35-3.45 (m, 1H), 3.72-3.85 (m, 3H), 4.95-5.05 (m, 1H), 7.05 (d, 1H), 7.31 (d, 1H), 7.4 (dd, 1H), 7.48 (d, 1H), 7.81 (m, 1H), 7.95 (t, 1H), 8.25 (t, 1H), 8.8 (s, 1H), 10.39 (s, 1H), 10.74 (s, 1H) Mass spectrum MH+ 417.

Provenance & Evidence