Application of 257280-25-4, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.257280-25-4, name is 5-Bromo-2-phenoxypyrimidine, molecular formula is C10H7BrN2O, molecular weight is 251.08, as common compound, the synthetic route is as follows.
Synthesis of 2-(2-chloro-6-fluorophenyl)-5-(2-phenoxypyrimidin-5-yl)- lH-imidazole-4-carbonitrile (EX-43)[000265] A solution of 5-bromo-2-phenoxypyrimidine (1-28) (0.3 mmol) and hexamethylditin (0.3 mmol) in DME (3 mL) was degassed with nitrogen for 5 minutes. Pd(PPh3 )4 (0.015 mmol) was added and the reaction was heated at 80 0C for 12 hours. The reaction was subsequently cooled to room temperature and extracted with EtOAc. The organic layer was washed with brine, dried over MgSO4, filtered and reduced to dryness. The crude product was purified by flash column chromatography (hexanes : EtOAc = 9 : 1) to afford 5-(trimethylstannyl)-2-phenoxypyrimidine (1-29) as a clear oil. MS (m/z) (M+l)+: 335.0, 337.0. [000266] 5-(Trimethylstannyl)-2-phenoxypyrimidine (1-29) (0.16 mmol) and 5-bromo-2- (2-chloro-6-fluorophenyl)-lH-imidazole-4-carbonitrile (1-10) (0.083 mmol) were dissolved in DME (2 mL) and degassed for 5 minutes with nitrogen. Pd(PPh3)4 (0.0082 mmol) was added and the reaction was heated at 85 0C for 12 hours. The reaction was cooled to room temperature and partitioned with EtOAc and water. The organic layer was washed with brine, dried over MgSO4, filtered and reduced to dryness. The crude product was purified by flash column chromatography (hexanes : EtOAc = 3 : 1) to afford 2-(2-chloro-6- fluorophenyl)-5-(2-phenoxypyrimidin-5-yl)-lH-imidazole-4-carbonitrile (EX-43) as white glassy solid. 1U NMR (400MEtaz, d4-MeOO) delta 8.95 (s, 2H), 7.50 (m, IH), 7.37 (m, 3H), 7.21 (m, 2H), 7.14 (m, 2H). MS (m/z) (M+l)+: 392.5.
Statistics shows that 257280-25-4 is playing an increasingly important role. we look forward to future research findings about 5-Bromo-2-phenoxypyrimidine.
Reference:
Patent; IRM LLC; CHIANELLI, Donatella; MOLTENI, Valentina; ALBAUGH, Pamela A.; CHOI, Ha-Soon; LOREN, Jon; WANG, Zhicheng; MISHRA, Pranab; WO2010/127152; (2010); A2;,
Pyrimidine | C4H4N2 – PubChem,
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