873-38-1, name is 2-Bromo-4-chloroaniline, belongs to chlorides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Application In Synthesis of 2-Bromo-4-chloroaniline
4-chloro-2-bromo-aniline (206 mg, 0.01 mmol) was dissolved in dimethylsulfoxide (20 mL). Under a nitrogen atmosphere, bis(pinacolato)diboron (3.8 g, 15 mmol), potassium acetate (2.5 g, 25.7 mmol) and [1,1?-bis(diphenylphosphino)ferrocene]dichloropalladium (218 mg, 0.3 mmol) were added thereto, and the temperature was raised to 80 C. to allow the reaction to proceed for 24 hours. Water (100 ml) was added to the reaction solution, which was extracted with ethyl acetate (80 ml¡Á2). The organic phases were combined, washed with saturated brine (100 mL), dried over anhydrous sodium sulfate, and concentrated. The residue was purified by silica gel column chromatography (ethyl acetate:petroleum ether=1:100 to 1:30) to give the title compound 4-chloro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline (2i) as a white solid (2.0 g, yield 79%). 1H NMR (400 MHz, CDC3) delta 7.54 (s, 1H), 7.19-7.08 (m, 1H), 6.55 (d, 1H), 4.86 (s. 2H), 1.34 (s, 12H). LCMS m/z=254.0 [M+1].
The synthetic route of 873-38-1 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Sichuan Haisco Pharmaceutical Co., Ltd.; Wei, Yonggang; QIU, Guanpeng; ZHENG, Suxin; LEI, Bolin; YU, Yan; CHEN, Yashu; (29 pag.)US2017/29423; (2017); A1;,
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