反应详情

温度

90 °C

N-(3-bromo-5-{[4-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)acetamide (150 mg, 0.400 mmol), 2-(trimethylsilyl)-5-(trimethylstannanyl)-1,3-thiazole (141 mg, 0.440 mmol) (prepared using literature procedure: Dondoni, A.; Mastellari, A. R.; Medici, A.; Negrini, E.; Pedrini, P. Synthesis 1986, 9, 757-760) and Pd(Ph3P)4 (46.2 mg, 0.040 mmol) were placed in a nitrogen purged microwave vial. Dioxane (2 mL) was added and the resultant solution was purged for 10 minutes with nitrogen gas. The reaction mixture was heated to 90° C. for 15 h. Note: Under the reaction conditions the TMS group is removed. The reaction mixture was concentrated and directly purified by column chromatography to yield 130 mg of N-[3-(1,3-thiazol-5-yl)-5-{[4-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl]acetamide (0.343 mmol, 86%) as a yellow powder.

1. customthe resultant solution was purged for 10 minutes with nitrogen gas
2. customUnder the reaction conditions the TMS group
3. customis removed
4. concentrationThe reaction mixture was concentrated
5. customdirectly purified by column chromatography