Yield:103505-49-3 98%

Reaction Conditions:

with hydrogenchloride in ethanol;water at 20 - 82; for 79 h;

Steps:

1-(1A-1)a 5-amino-4, 6-dichloropyrimidine (5.00 g, 29 MMOL) and 4-chloroaniline (4. 71 g, 36 MMOL) were suspended in 80 ml H20 and 12 ML ETHANOL. Concentrated HCI (1.2 ML, 14.5 MMOL) was added at room temperature followed by warming reaction to 82 °C. After stirring for 19 hours the reaction was cooled to room temperature and stirred for 60 hours. The precipitate was collected on a sintered glass funnel and rinsed with water followed by hexanes. After drying under vacuum, 1-(1A-1 a was obtained as an off-white solid (7.38 g, 98%): +ESI MS (M+1) 255.3 ; H NMR: (400 MHz, CD30D) : No. 7.87 (s, 1 H), 7.66 (d, J = 8.7 Hz, 2 H), 7.30 (d, J = 8.7 Hz, 2 H).

References:

WO2004/37823,2004,A1 Location in patent:Page 63-64