Reference of 878207-28-4, These common heterocyclic compound, 878207-28-4, name is Methyl 2-bromo-4,5-difluorobenzoate, its 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.
Methyl 4-(5-(benzyloxy)-1H-indol-1-yl)-2-bromo-5-fluorobenzoate [0220] A mixture of 5-benzyloxy indole (11.2g, 0.05 mmol), methyl 2-bromo-4,5-difluoro-benzoate (12.6g, 0.05 mol) and Cs2C03 (24.4g, 0.075 mol) in DMF (150 mL) was stirred at 100 C under N2 atmosphere overnight. The mixture was cooled to room temperature and then filtrated. The filtrate was poured into 150 mL water. A gradual formation of a cream-colored precipitate was observed. Filtration gave the desired intermediate product as a cream-colored solid which is pure enough for further reaction (Yield: 17g, 74.8%). 1HNMR (500 MHz, DMSO-d6) delta: 8.02 (d, J=7 Hz, IH), 7.98 (d, J=l lHz, IH), 7.60 (s, IH), 7.48 (d, J=7.5 Hz, 2H), 7.39 (t, J=7.5 Hz, 2H), 7.32 (t, J=7 Hz, IH), 7.26 (d, J=8.5 Hz, 2H), 6.96 (d, J=8.5 Hz, IH), 6.68 (s, IH), 5.14 (s, 2H) and 3.91 (s, 3H) ppm.
Statistics shows that Methyl 2-bromo-4,5-difluorobenzoate is playing an increasingly important role. we look forward to future research findings about 878207-28-4.
Reference:
Patent; ANACOR PHARMACEUTICALS, INC.; ZHANG, Yong-kang; ZHOU, Huchen; DING, Charles; PLATTNER, Jacob, J.; FREUND, Yvonne; WO2011/63293; (2011); A1;,
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