With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10261-82-2,1,5-Naphthyridin-2(1H)-one,as a common compound, the synthetic route is as follows.
To a suspension of Intermediate 3 (5.9 g) in dry DME (180 ml) and dry DMF (45 ml) at O0C under argon was added in portions NaH (60% w:w dispersion in mineral oil, 3.2 g). After stirring for 45 minutes, the mixture was treated with lithium bromide (8.8 g) and the suspension was allowed to warm to room temperature. After stirring for 45 minutes, the mixture was treated with allyl bromide (7 ml) and then stirred at 650C for 3 h. The mixture was cooled to room temperature and concentrated under reduced pressure, then t- BuOMe (300 ml) was added and the mixture was then washed with 1 N NH4CI (200 ml).The combined aqueous phases were extracted with f-BuOMe (2 x 100 ml). The organic phases were combined, washed with brine (200 ml), dried over Na2SO4, filtered and evaporated under reduced pressure. The residue was purified by column chromatography on silica gel using a EtOAc and hexane gradient (50-75%) to give the desired product (4.29 g, 57%). To obtain an additional amount of the desired compound, the combined aqueous phases were extracted exhaustively with CH2CI2. Then, the organic extracts were combined, dried over MgSO4, filtered and evaporated under reduced pressure. Theresidue was purified by column chromatography on silica gel using a EtOAc and hexane gradient (50-75%) to give the desired product (1.5 g, 20%). [ES MS] m/z 187 (MH+).
The synthetic route of 10261-82-2 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; GLAXO GROUP LIMITED; ALEMPARTE-GALLARDO, Carlos; BARROS-AGUIRRE, David; CACHO-IZQUIERDO, Monica; FIANDOR-ROMAN, Jose Maria; LAVANDERA DIAZ, Jose Luis; REMUINAN-BLANCO, Modesto Jesus; WO2010/81874; (2010); A1;,
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