Synthesis
5-Bromo-2-fluorobenzaldehyde (10 g, 49.2 mmol) and guanidine carbonate (13.3 g, 74 mmol) were dissolved in N,N-dimethylacetamide (50 mL). The reaction mixture was heated to reflux temperature with continuous stirring for 5 hours. Upon completion of the reaction, it was cooled to room temperature, water (120 mL) was added and stirring was continued for 2 hours at room temperature. The resulting 6-bromo-2-quinazolinamine was collected by filtration and subsequently dried under vacuum to give the final product (5.0 g, 60% yield).
References
[1] Patent: WO2017/46739, 2017, A1. Location in patent: Page/Page column 49
[2] European Journal of Medicinal Chemistry, 2017, vol. 141, p. 506 - 518
[3] Journal of Organic Chemistry, 2006, vol. 71, # 10, p. 3959 - 3962
[4] Journal of Medicinal Chemistry, 2006, vol. 49, # 19, p. 5671 - 5686
[5] Journal of Medicinal Chemistry, 2008, vol. 51, # 11, p. 3065 - 3068
