Reference of 203302-95-8,Some common heterocyclic compound, 203302-95-8, name is 4-Bromo-3,5-difluoroaniline, molecular formula is C6H4BrF2N, 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 mixture of 4-bromo-3,5-difluoroaniline (23.0 g, 110 mmol), 4,4,4′,4,,5,5,5′,5′- octamethyl-2,2′-bi(l ,3,2-dioxaborolane) (30.9 g, 122 mmol), dppf (3.0 g, 5.5 mmol), Pd(dppf)Cl2(4.5 g, 5.5 mmol) and KOAc (32.0 g, 331 mmol) in dioxane (230 mL) was heated at 80 C under N2atmosphere for 18 h. The reaction mixture was cooled and filtered. The filtrate was concentrated, and the residue was purified by column chromatography (Si02, petroleum ethenEtOAc = 20: 1) to give the title compound as a light yellow solid. NMR (400 MHz, CDC13): delta 6.13-6.11 (m, 2H), 4.04 (br s, 2H), 1.35 (s, 12H).
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-3,5-difluoroaniline, its application will become more common.
Reference:
Patent; MERCK SHARP & DOHME CORP.; CROWLEY, Brendan; FRALEY, Mark; POTTEIGER, Craig; GILFILLAN, Robert; PATEL, Mehul; ARRINGTON, Ken; MITCHELL, Helen; SCHIRRIPA, Kathy; MCWHERTER, Melody; BIFTU, Tesfaye; NAIR, Anilkumar; WANG, Cheng; YANG, De-Yi; ZHU, Cheng; KAR, Nam Fung; HUANG, Xianhai; CHEN, Lei; ZHOU, Wei; LIU, Qingsheng; CAI, Jiaqiang; WO2015/161011; (2015); A1;,
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