反应详情

Following the same procedure as in step 3 of Example 337 using 7-chloro-1,3-benzothiazole (58.8 mg, 0.35 mmol, 1.80 equiv), tert-butyl (3R)-3-[[5-iodo-6-methoxy-2-(morpholin-4-yl)pyrimidin-4-yl]amino]piperidine-1-carboxylate (100.0 mg, 0.19 mmol, 1.00 equiv), cesium carbonate (371.4 mg, 6.00 equiv), tetrakis(triphenylphosphine)palladium (40.4 mg, 0.03 mmol, 0.18 equiv) and copper (I) iodide (6.7 mg, 0.04 mmol, 0.18 equiv) in N,N-dimethylformamide (4.0 mL). The crude product was purified through a silica gel column, eluting with ethyl acetate/petroleum ether (1:10-1:3) to provide the title compound as a white solid.

1. customThe crude product was purified through a silica gel column
2. washeluting with ethyl acetate/petroleum ether (1:10-1:3)