Some common heterocyclic compound, 175278-17-8, name is 2-Bromo-4-(trifluoromethoxy)aniline, molecular formula is C7H5BrF3NO, 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. category: ethers-buliding-blocks
According to route (C), 2-bromo-4-trifluoromethoxyaniline (2.3 mL, 15 mmoles, 1 eq.) was placed in l,4-dioxane (55 mL) with Pd(dppf)Cl2.CH2Cl2 (1.2 g, 1.5 mmole, 0.1 eq.). Upon addition of CS2CO3 (19.6 g, 60 mmoles, 4 eq.) and ethylboronic acid (3.3 g, 45 mmoles, 3 eq.), the reaction mixture was heated at l00C and stirred for 14 hours under an inert atmosphere of argon. The reaction mixture was then concentrated under reduced pressure and the resulting residue was purified by column chromatography on silica gel to afford 2-ethyl-4-(trifluoromethoxy)aniline (1.3 g, 42%). (0391) 6.93 (s, 1H), 6.90 (d, J = 8.5 Hz, 1H), 6.63 (d, J = 8.5 Hz, 1H), 3.64 (s, 2H), 2.49 (q, 7 = 7.5 Hz, 2H), 1.25 (t , J= 7.5 Hz, 3H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 175278-17-8, its application will become more common.
Reference:
Patent; ABIVAX; CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE; UNIVERSITE DE MONTPELLIER; INSTITUT CURIE; SCHERRER, Didier; TAZI, Jamal; MAHUTEAU-BETZER, Florence; NAJMAN, Romain; SANTO, Julien; APOLIT, Cecile; (0 pag.)WO2020/11810; (2020); A1;,
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