Synthetic Route of 1000577-58-1,Some common heterocyclic compound, 1000577-58-1, name is 1-Bromo-2,3-dichloro-5-fluorobenzene, molecular formula is C6H2BrCl2F, 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.
l-Bromo-2,3-dichloro-5-fluorobenzene (1.0401 g, 4.27 mmol) was dissolved in toluene (30 mL), and then the solvent was removed under reduced pressure. The residue was dried under high vacuum for a few minutes. Anhydrous THF (15 mL) was added to dissolve the starting material. And then sodium methanoxide (0.9873 g, 17.36 mmol) was added. The mixture was heated at 75 C for 4.5 h, cooled to room temperature. The mixture was quenched with saturated ammonium chloride solution, concentrated to remove THF. The remaining mixture was extracted with ethyl acetate (4 x 150 mL). The organic solution was washed with brine, dried over anhydrous sodium sulfate, concentrated to dryness to afford 1.0188 g of product as white solid in 93% yield. -NMR (500MHz, CDC13): 7.109 (d, J = 3.0 Hz, 1H), 6.988 (d, J= 3.0 Hz, 1H), 3.786 (s, 3H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1-Bromo-2,3-dichloro-5-fluorobenzene, its application will become more common.
Reference:
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
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