With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1383146-20-0,(R)-4-(2,4-Dimethoxybenzyl)-3-methylpiperazin-2-one,as a common compound, the synthetic route is as follows.
Synthesis of (R)-l-(2,4-dimethoxybenzyl)-5-ethoxy-6-methyl-l,2,3, 6- tetrahydropyrazine D. Oven dried (115C) sodium carbonate (2.48 g, 23.40 mmol, 2.25 eq.) was placed in a round-bottom flask. The round-bottom flask was backfilled with Ar and then capped with a rubber septum. A solution of (R)-4-(2,4-dimethoxybenzyl)-3-methylpiperazin-2- one C (2.75 g, 10.40 mmol, 1 eq.) in anhydrous DCM (35 mL) was added, followed by freshly prepared triethyloxoniumtetrafluoroborate (2.48 g, 13.05 mmol, 1.25 eq.) in one portion. Thereafter the reaction mixture was stirred further at RT for 45 min to 1 hour, whereupon the reaction mixture was diluted with saturated aqueous NaHC03 (100 mL). The aqueous layer was extracted with DCM (3 x 200 mL). The organic layers were combined, dried over MgS04, filtered and concentrated under reduced pressure to afford 3.1 g of yellow oil. The crude compound was then purified on silica gel (EtOAc/MeOH: 99/1) to afford the desired product D as a pale yellow oil. Yield: 1.44 g, 48 %. LCMS: P = 95 , retention time = 1.8 min, (M+H20+H)+: 311 ; chiral HPLC retention time = 12.3 min, ee > 97 %. 1H-NMR (CDC13): delta 7.23 (d, J= 8.8, 1H), 6.48 (d, J= 8.8, 1H), 6.44 (s, 1H), 4.02 (m, 2H), 3.92 (s, 6H), 3.86 (d, JAB= 14.0, 1H), 3.46 (d, JAB= 14.0, 1H), 3.44 (m, 2H), 3.10 (m, 1H), 2.79 (m, 1H), 2.32 (m, 1H), 1.35 (d, J= 6.8, 3H), 1.24 (t, J= 6.0, 3H)., 1383146-20-0
As the paragraph descriping shows that 1383146-20-0 is playing an increasingly important role.
Reference£º
Patent; EUROSCREEN SA; HOVEYDA, Hamid; DUTHEUIL, Guillaume; FRASER, Graeme; WO2014/154897; (2014); A1;,
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