Synthetic Route of 2854-16-2 ,Some common heterocyclic compound, 2854-16-2, molecular formula is C4H11NO, its 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.
2,3-Difluoro-5-iodopyridine (500 mg, 2.07 mmol) was dissolved in NMP (500 mu) and pyridine (201 mu, 2.49 mmol, 1.2 equiv.) and l-amino-2-methylpropan-2-ol (555 mg, 6.22 mmol, 3 equiv.) were added at room temperature. The mixture was stirred for 16 hours at 100 °C. The reaction mixture was cooled and extracted with saturated NaHCOs solution and two times with a small volume of dichloromethane. The crude product was purified by flash chromatography by directly loading the dichloromethane layers onto a silica gel column and eluting with an ethyl acetate: heptane gradient 0: 100 to 100:0. The desired l-(3-fluoro-5-iodopyridin-2-ylamino)-2- methylpropan-2-ol (590 mg, 1.9 mmol, 91.7 percent yield) was obtained as a colorless oil, MS: m/e = 311.0 (M+H+).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,2854-16-2, its application will become more common.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GREEN, Luke; GUBA, Wolfgang; JAESCHKE, Georg; JOLIDON, Synese; LINDEMANN, Lothar; RICCI, Antonio; RUEHER, Daniel; STADLER, Heinz; VIEIRA, Eric; WO2011/128279; (2011); A1;,
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