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General procedure for the synthesis of 7-(benzyloxy)-N-(4-bromo-2-fluorophenyl)-6-methoxyquinazolin-4-amine from 4-bromo-2-fluoroaniline and 7-benzyloxy-4-chloro-6-methoxyquinazoline: 6.5 M hydrogen chloride (2.54 mL) was added to a 2-propanol (160 mL) solution containing 4-bromo-2-fluoroaniline (4.51 g, 15.0 mmol) and 7-benzyloxy-4- chloro-6-methoxyquinazoline (2.40 g, 16.5 mmol) in a solution of 2-propanol (160 mL). Subsequently, the reaction mixture was heated to reflux and kept for 2 hours. Upon completion of the reaction, the mixture was cooled to room temperature and the precipitated solid product was collected by filtration. The solid was washed sequentially with 2-propanol and ether and finally dried under vacuum overnight to afford the target compound 7-(benzyloxy)-N-(4-bromo-2-fluorophenyl)-6-methoxyquinazolin-4-amine (7.9 g, 94% yield) as a white solid.

[1] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 11, p. 3222 - 3226
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[3] Patent: US2010/75916, 2010, A1. Location in patent: Page/Page column 16
[4] Patent: WO2005/97134, 2005, A2. Location in patent: Page/Page column 16-17; figure 2
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