With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1403898-64-5,(2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
Tert-butyl (2R,5R)-5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate (770 mg, 3.34 mmol), 181 tert-butylchlorodimethylsilane (756 mg, 5.02 mmol), 132 triethylamine (677 mg, 6.69 mmol) and 182 N,N-dimethylpyridin-4-amine (41 mg, 0.33 mmol) were dissolved in 63 DCM (6 ml) and the mixture was stirred at room temperature for 2 hours. The reaction was quenched with saturated 152 aqueous NH4Cl and extracted with DCM (3×30 ml). The organic phase was washed with brine and dried. The solvent was removed under reduced pressure and the crude product was purified by flash chromatography on a silica gel, eluting from 0-30% (57 EtOAc in 148 petroleum ether). The fractions containing the desired product were evaporated to dryness to afford 183 tert-butyl (2R,5R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-2-methylpiperazine-1-carboxylate (1.04 g, 90%) as a colourless oil. 1H NMR (Chloroform-d, 400 MHz) 0.08 (6H, d), 0.91 (9H, s), 1.30 (3H, d), 1.47 (9H, s), 2.56 (1H, dd), 2.96-3.05 (1H, m), 3.10 (1H, dd), 3.30 (1H, dd), 3.55 (1H, dd), 3.68-3.82 (2H, m), 4.15-4.25 (1H, m), (1 exchangeable proton not seen). m/z (ES+), [M+H]+=345., 1403898-64-5
The synthetic route of 1403898-64-5 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); A1;,
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