With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.
Synthesis of methyl (3R)-4-[6-(4,4-difluoropiperidin-l-yl)-2-(methylsulfanyl)pyrimidin- 4-yl]-3-methylmorpholine: Into a 40-mL microwave and maintained with an inert atmosphere of nitrogen, was placed (3R)-4-[6-chloro-2-(methylsulfanyl)pyrimidin-4-yl]-3-methylmorpholine (1 g, 3.85 mmol, 1 equiv), 4,4-difluoropiperidine (932.7 mg, 7.70 mmol, 2.0 equiv), Pd2(dba)3 (352.5 mg, 0.38 mmol, 0.10 equiv), XantPhos (445.5 mg, 0.77 mmol, 0.20 equiv), Cs2C03 (2.5 g, 7.70 mmol, 2.00 equiv), dioxane(10 ml). The resulting solution was stirred for 1 hr at 90 ¡ãC. The solids were filtered out. The combined organic layer was concentrated. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (1 :3). This resulted in 180 mg (13.57 percent) of (3R)-4-[6-(4,4-difluoropiperidin- l-yl)-2-(methylsulfanyl)pyrimidin-4-yl]-3- methylmorpholine as a white solid. LC-MS-BLV-CY-232-2: (ES, m/z): 345 [M+H]+. H-NMR- BLV-CY-232-2: (300 MHz, d6-DMSO, ppm): delta 5.73 (s, 1H), 4.42-4.31 (m, 1H), 3.97-3.87 (m, 2H), 3.71-3.68 (m, 5H), 3.56 (dd, 7 = 11.4, 2.9 Hz, 1H), 3.41 (td, 7 = 11.8, 2.8 Hz, 1H), 3.04 (td, 7 = 12.8, 3.6 Hz, 1H), 2.38 (s, 3H), 2.02-1.89 (m, 4H), 1.13 (d, 7 = 6.7 Hz, 3H)., 21987-29-1
The synthetic route of 21987-29-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; BLUEVALLEY PHARMACEUTICAL LLC; LI, Xiang; (99 pag.)WO2019/50889; (2019); A1;,
Piperidine – Wikipedia
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