Electric Literature of 145255-19-2, 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 145255-19-2 as follows.
[1144] 40 mg (0.098 mmol) of 2-[4-(5-chioro-2-cyano- phenyl)-5-methoxy-2-oxopyridin-i (2H)-yl] -3-(i ,3-oxazol- 2-yl)propanoic acid (racemate) and 20mg (0.147 mmol, 1.5 eq.) of 5-aminopyridine-2-carboxamide were initially charged in 0.8 ml of pyridine, 93 j±1 (0.392 mmol, 50% in ethyl acetate, 4.0 eq.) of T3P were added and the mixture was stirred at 50 C. for 2 h. The reaction mixture was cooled, 6 ml of saturated aqueous sodium hydrogencarbonate solution were added and the mixture was stirred for 15 mm. The crystals formed were filtered oil with suction and washed with water, 500 j±1 of isopropanol and then pentane. The residue was dried under high vacuum. Yield: 29 mg (57% of theory).11145] LCMS [Method 1]: R=0.79 mm; MS (ESIpos):mlz=5 19 (M+H), j1146] ?H-NMR (400 MHz, DMSO-d5): oe [ppm]=i0.91(s, 1H), 8.84 (d, 1H), 8.20 (dd, 1H), 8.07-7.95 (m, 4H), 7.73 (dd, 1H), 7.68 (d, 1H), 7.52 (s, 2H), 7.12 (s, 1H), 6.51 (s, 1H), 6.00 (t, 1H), 3.78 (d, 2H), 3.64 (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,145255-19-2, its application will become more common.
Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; ROeHRIG, Susanne; JIMENEZ-NUNEZ, Eloisa; SCHLEMMER, Karl-Heinz; TERSTEEGEN, Adrian; TELLER, Henrik; HILLISCH, Alexander; HEITMEIER, Stefan; SCHMIDT, Martina Victoria; ACKERSTAFF, Jens; STAMPFUss, Jan; (87 pag.)US2017/291892; (2017); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem