New downstream synthetic route of 1000577-58-1

According to the analysis of related databases, 1000577-58-1, the application of this compound in the production field has become more and more popular.

Related Products of 1000577-58-1, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 1000577-58-1 as follows.

l -Bromo-2,3-dichloro-5-fluorobenzene (1,4618 g, 5.99 mmol) and mPEG3-OH (1.1097g, 6.76 mmol) was mixed with toluene (25 mL) and removed the solvent. The remaining material was dried under high vacuum for a few minutes. The mixture was dissolved in anhydrous THF (20 mL). 60% Sodium hydride (0.3549 g, 8.87 mmol) was added. The resulting mixture was heated at 75 C for 3 h. The mixture was cooled to room temperature. Saturated ammonium chloride aqueous solution was added to quench the reaction. The mixture was concentrated to remove the organic solvent. The remaining mixture was extracted with dichloromethane (3 x 20 mL). The combined organic solution was washed with brine, dried over anhydrous sodium sulfate, concentrated. The residue was purified with biotage flash column using 15-100% ethyl acetate/hexane to afford the product (2.057 g, yield: 88%). NMR (500 MHz, Chloroform-i/) delta 7.17 (d, J = 2.9 Hz, 1 H), 7.05 (d, J= 2.8 Hz, IH), 4.16 – 4.07 (m, 2H), 3.89-3.83 (m, 2H), 3.77-3.65 (m, 6H), 3.60-3.55 (m, 2H), 3.41 (s, 3H).

According to the analysis of related databases, 1000577-58-1, the application of this compound in the production field has become more and more popular.

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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