Application of 259809-79-5 , The common heterocyclic compound, 259809-79-5, name is tert-Butyl 7,8-dihydro-2-(methylsulfonyl)pyrido[4,3-d]pyrimidine-6(5H)-carboxylate, molecular formula is C13H19N3O4S, 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.
Under nitrogen atmosphere, 2,2-difluoroethanol (65.5 mg, 0.80 mmol) dissolved in DMF (2 mL) was cooled with ice. To the solution was added sodium hydride (60 wt percent, 31.9 mg, 0.80 mmol) portionwise. The mixture was stirred at 0° C. for 1 hour. To the mixture was added a compound 27 (50 mg, 0.16 mmol) portionwise. Then, the mixture was stirred at 0° C. for 2 hours. Ice water was added to the reaction mixture. The mixture was extracted with ethyl acetate. The organic layer was washed by brine, and then dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure. The obtained residue was purified by silica-gel column chromatography (hexane-ethyl acetate) to give a compound 28 (28.8 mg, yield 57percent).1H-NMR (CDCl3) delta: 1.50 (s, 9H), 2.89 (s, 2H), 3.73 (s, 2H), 4.53-4.61 (m, 4H), 6.14 (t, J=55.4 Hz, 1H), 8.27 (s, 1H).
The synthetic route of 259809-79-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Shionogi & Co., Ltd.; TOBINAGA, Hiroyuki; MASUDA, Koji; KASUYA, Satoshi; INAGAKI, Masanao; YONEHARA, Mitsuhiro; MASUDA, Manami; (289 pag.)US2019/161501; (2019); A1;,
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