Reference of 142808-15-9, These common heterocyclic compound, 142808-15-9, name is 4-Bromo-2-fluorobenzotrifluoride, 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.
Example 80A2-[3-Fluoro-4-(trifluoromethyl)phenyl]-4,4,5,5-tetramethyl-1,3,2-dioxaborolane A mixture of 25 g (99.8 mmol) of 4-bromo-2-fluoro-1-(trifluoromethyl)benzene in 500 ml of dioxane was admixed under argon at RT with 27.8 g (109.8 mmol) of 4,4,4′,4′,5,5,5′,5′-octamethyl-2,2′-bis-1,3,2-dioxaborolane, 2.91 g (3.99 mmol) of 1,1-bis(diphenylphosphine)-ferrocenedichloropalladium(II) dichlormethane complex and with 29.38 g (299.4 mmol) of potassium acetate. The reaction mixture was stirred below 100 C. for several hours until conversion was substantially complete. The mixture was filtered through Celite and admixed with water. After addition of ethyl acetate and phase separation, the organic phase was dried over magnesium sulphate, filtered and concentrated under reduced pressure. The crude product is purified by flash chromatography (silica gel-60, eluent: cyclohexane/ethyl acetate 3:1). This gave 18.22 g of crude product in 73% purity (LC-MS), which was reacted without any further purification steps.1H NMR (400 MHz, DMSO-d6): delta=7.82 (dd, 1H), 7.67 (d, 1H), 7.59 (d, 1H), 1.32 (s, 12H).
The synthetic route of 142808-15-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; US2011/21489; (2011); A1;,
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