1383146-20-0, (R)-4-(2,4-Dimethoxybenzyl)-3-methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated
Method E is illustrated by the synthesis of intermediate (R)-l-(2,4-dimethoxybenzyl)-5- ethoxy-6-methyl-l,2,3,6-tetrahydropyrazine Ds-l(i.e. compound D wherein PG is DMB and R is Me). The corresponding DMB-protected ketopiperazine Cs is commercially available. 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-l (2.75 g, 10.40 mmol, 1 eq.) in anhydrous DCM (35 mL) was added, followed by freshly prepared triethyloxonium tetrafluoroborate (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-l 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, 1383146-20-0 (R)-4-(2,4-Dimethoxybenzyl)-3-methylpiperazin-2-one 56973619, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; EUROSCREEN SA; HOVEYDA, Hamid; DUTHEUIL, Guillaume; FRASER, Graeme; WO2014/154895; (2014); A1;,
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