O-Xylene → 5-Allyl-4-(4-bromo-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-ol

Participants

Reaction Steps

A solution of (6-allyloxy-7-methoxy-quinazolin-4-yl)-(4-bromo-2-fluoro-phenyl)-amine (0.46 g, 1.13 mmol) (from Example 19, Step C, supra) in o-xylene (75 mL) was heated at 150° C. for 4 hours. At the end of this period, TLC analysis indicated almost complete consumption of the starting material and the formation of desired product as the major spot. The solution was concentrated to a small volume and filtered. The solid was collected and dried in vacuo to give the desired 5-allyl-4-(4-bromo-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-ol as an off white solid. (Yield 0.35 g, 76%).

Provenance & Evidence