Electric Literature of 13438-65-8, 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 13438-65-8 as follows.
A mixture of 2-aminonicotinamide (0.85 g, 6.20 mmol), mono-tert-butyl succinate (1.620 g, 9.30 mmol), HATU (3.54 g, 9.30 mmol) and TEA (1.728 mL, 12.40 mmol) in DMF was stirred at 60C for 20 h. The mixture was poured into water and extracted with EtOAc. The combined organic layers were washed with brine, dried and concentrated. The residual material was absorbed onto a plug of silica gel and purified by chromatography through a Redi-Sep pre-packed silica gel column (40 g), eluting with a gradient of 0% to 60% 1M NH3-MeOH in DCM, to provide tert-butyl 4- ((3-carbamoylpyridin-2-yl)amino)-4-oxobutanoate (0.70 g, 2.386 mmol, 38.5 % yield) (including -30% unidentified compound) as a light-yellow solid.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,13438-65-8, its application will become more common.
Reference:
Patent; AMGEN INC.; BREGMAN, Howard; BUCHANAN, John L.; CHAKKA, Nagasree; DIMAURO, Erin F.; GUNAYDIN, Hakan; GUZMAN PEREZ, Angel; HUA, Zihao; HUANG, Xin; WO2014/36022; (2014); A1;,
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