Some common heterocyclic compound, 309721-44-6, name is 2-Bromo-1-chloro-3-fluorobenzene, molecular formula is C6H3BrClF, 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. Computed Properties of C6H3BrClF
To a mixture of sodium tert-butoxide (138 mg, 1 .4 mmo) in THF (1.0 mL) was added I ,1 ,1 -trifiuoro-2-propano (0.14 mL, 1.5 mmo) and 2-bromo-1-choro-3-fluorobenzene (200 mg, 0.96 mmofl n DMF (2.0 rnL). The reacfion mxture was heated at 80 C for 24 h. After coohng to rt, EtOAc (5.0 mL) was added to the reacton rnxture and washed sequentaHy with 1 M HC (2.5 mL), saturated aqueous NaHCO3, and brine. The aqueous ayers were extractedw[th EEtOAc, and the combined organic extracts were dred (Na2SO4), ifitered and concentrated. Purflcaton by FCC (0 -10% EtOAc I hexanes) afforded the tWe compound as an o (87 rng, 30% yed). ?H NMR (400 MHz, CDC3) oe 7.23 (rn, 2H), 6.86 (dd, J = 7.3, 2.4 Hz, I H), 4.72 4.58 (m, 1 H), 1.62 – 1.49 (m, 3H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 309721-44-6, its application will become more common.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; RAVULA, Suchitra; SWANSON, Devin M.; SAVALL, Bradley M.; AMERIKS, Michael K.; (250 pag.)WO2016/176449; (2016); A1;,
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