Synthetic Route of 163263-91-0, 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 163263-91-0 as follows.
To a solution of 2,4-dichloro-6-(4-methoxyphenyl)pyrimidine (1.01 g, 3.96 mmol) and (+/-)-trans-methyl 3 -aminobicyclo[2 .2. 2]octane-2-carboxylate (871 mg, 4.75 mmol) in N,N-dimethylformamide (20 mL) was added potassium carbonate (0.81 g, 5.88mmol). The mixture was stirred at rt overnight. To the reaction mixture was added water (70 mL), and the mixture was extracted with EtOAc (100 mL x 3). The combined organic layers were washed with saturated brine (100 mL), dried over anhydrous sodium sulfate, and filtered. The filtrate was concentrated in vacuo to dry.The residue was purified by silica gel column chromatography (PE/EtOAc (v/v) = 20/1) to give the title compound as a white solid (1.01 g, 64%).MS-ESI: (ESI, pos.ion) m/z: 402.2 [M+Hfb;?H NIVIR (400 IVIFIz, CDC13) (ppm): 7.98 (d, J = 8.7 Hz, 2H), 6.98 (d, J = 8.9 Hz, 2H), 6.72 (s, 1H), 5.46 (d, J= 6.3 Hz, 1H), 4.32 (s, 1H), 3.88 (s, 4H), 3.74 (s, 3H), 2.39 (d, J= 5.1 Hz, 1H),2.08 (s, 1H), 1.90-1.84 (m, 1H), 1.78-1.56 (m, 8H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,163263-91-0, its application will become more common.
Reference:
Patent; SUNSHINE LAKE PHARMA CO., LTD.; REN, Qingyun; TANG, Changhua; YIN, Junjun; YI, Kai; ZHANG, Yingjun; (264 pag.)WO2018/33082; (2018); A1;,
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