反应详情

温度

100 °C

Ethereal hydrogen chloride (2.0M; 0.57 ml, 1.14 mmol) was added to a solution of 5-bromo-2-chloro-4-(4-methoxyphenoxy)pyrimidine (Method 1, 200 mg, 0.63 mmol) and 4-[3-(isobutylamino)-2-hydroxypropoxy]aniline (Method 10, 136 mg, 0.57 mmol) in NMP (4 ml). The solution was heated at 100° C. for 6 hours and silica (1 g) was added. Volatile material was removed by evaporation and the residue was purified by column chromatography, eluting with 0-10% 2.0M methanolic ammonia solution in DCM, to give the product as a colourless solid (76 mg, 26%). MS (MH+): 517, 519; HPLC (RT): 6.48.

1. additionsilica (1 g) was added
2. customVolatile material was removed by evaporation
3. customthe residue was purified by column chromatography
4. washeluting with 0-10% 2.0M methanolic ammonia solution in DCM