Synthetic Route of 458-50-4,Some common heterocyclic compound, 458-50-4, name is 4-Bromo-3-fluoroanisole, molecular formula is C7H6BrFO, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
A degassed solution of 3-amino-furo[3,2-c]pyridine-2-carboxylic acid ethyl ester (206 g, 1.0 mmol), l-bromo-2-fluoro-4-methoxy-benzene (246 mg, 1.2 mmol), Pd2dba3 (46 mg, 0.050 mmol), Xantphos (58 mg, 0.10 mmol) and K3PO4 (254 mg, 1.2 mmol) in toluene (5 ml) was heated to 1100C then stirred for 18 hours. The reaction mixture was cooled to ambient temperature then diluted with EtOAc and filtered through a pad of celite. The filtrate was concentrated in vacuo to give a black oil. The oil was purified by flash chromatography (Si-SPE, MeOH: DCM, gradient 0: 100 to 10:90) to provide the title compound as a yellow oil (130 mg, 39percent). LCMS (method B): Rx = 2.93 min, M+H+ = 331.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Bromo-3-fluoroanisole, its application will become more common.
Reference:
Patent; GENENTECH, INC.; WO2008/24725; (2008); A1;,
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