Synthesis
6-Methylquinazoline-2,4(1H,3H)-dione (550 mg, 3.12 mmol) was used as a starting material, which was dissolved in POCl3 (4.0 mL), followed by the addition of N,N'-diethylaniline (0.5 mL). The reaction mixture was heated to 135 °C and the reaction was stirred at this temperature for 3 hours. Upon completion of the reaction, the mixture was cooled to room temperature and carefully poured into ice water. The precipitated solid was collected by filtration and dried to afford 2,4-dichloro-6-methylquinazoline (590 mg, 89% yield), which could be used in subsequent steps without further purification.
References
[1] Bioorganic and Medicinal Chemistry Letters, 2012, vol. 22, # 1, p. 461 - 467
[2] Bioorganic and Medicinal Chemistry, 2009, vol. 17, # 1, p. 119 - 132
[3] Patent: WO2004/87680, 2004, A1. Location in patent: Page 162
[4] ACS Medicinal Chemistry Letters, 2015, vol. 6, # 3, p. 308 - 312
[5] Patent: WO2008/16666, 2008, A2. Location in patent: Page/Page column 49
