反应详情

Following the same procedure as in step 3 of Example 121 using 1,3-benzothiazole-5-carbonitrile (56.1 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 mg, 0.19 mmol, 1.00 equiv), copper iodide (6.7 mg, 0.035 mmol, 0.18 equiv), cesium Carbonate (0.37 g, 6.00 equiv, 1.14 mmol) and Pd(PPh3)4 (40.4 mg, 0.035 mmol, 0.18 equiv) in DMF (6.0 mL). The crude product was purified by flash chromatography on silica gel, eluting with a mixture of 10-20% ethyl acetate in petroleum ether to give the title compound as a white solid. MS m/z [M+H]+ (ESI): 552.

1. customThe crude product was purified by flash chromatography on silica gel
2. washeluting with a mixture of 10-20% ethyl acetate in petroleum ether