With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.220641-87-2,N-Methyltetrahydro-2H-pyran-4-amine,as a common compound, the synthetic route is as follows.
To a solution of A2 (100 mg, 0.3 12 mmol) in DCM (4 mL) was added TEA (156 mg, 1.55 mmol) and HATU (112 mg, 0.468 mmol) at 25 C. After stirring at 25 C for 30 minutes, N-methyltetrahydro-2H- pyran-4-amine (57.4 mg, 0.499 mmol) was added. The mixture was stirred at 25 C for 16 hrs, quenchedwith water (4 mL) and extracted with DCM (2 x 4 mL). The organic layers were washed with brine (2 x5 mL), dried over Na2SO4 , filtered, concentrated in vacuo to give a crude product, which was purifiedby silica gel chromatography eluted with PE/EtOAc = 3/1 to afford the desired compound. Thecompound was lyophilized to give a solid (80 mg) that was further re-crystallized (85 C) from MeCN(2 mL) and water (20 mL) to give Compound 10 (66 mg, 51%) as a solid.1H NMR (400 MHz, CDCl3) delta 4.85-4.70 (m, 0.5H), 4.15-3.95 (m, 2H), 3.55-3.40 (m, 1.5H), 2.90-2.70 (m, 3H), 2.69-2.60 (m, 1H), 2.35-2.20 (m, 1H), 1.90-1.60 (m, 1OH), 1.59-1.16 (m, 18H),1.15-1.00 (m, 3H), 0.72 (s, 3H).LCMS Rt = 1.005 min in 2.0 mm chromatography, 30-90 AB, purity 100%, MS ESI calcd. for C26H44N03 [M+Hf?418, found 418.
220641-87-2, 220641-87-2 N-Methyltetrahydro-2H-pyran-4-amine 6991950, aTetrahydropyrans compound, is more and more widely used in various fields.
Reference£º
Patent; SAGE THERAPEUTICS, INC.; ROBICHAUD, Albert, J.; MARTINEZ BOTELLA, Gabriel; HARRISON, Boyd, L.; SALITURO, Francesco, G.; GRIFFIN, Andrew; BLANCO-PILLADO, Maria, Jesus; (296 pag.)WO2018/13613; (2018); A1;,
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