With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
To a solution of (lambda)-3-hydroxymethyl-piperazine-l-carboxylic acid tert-butyl ester (795 mg, 3.68 mmol) in DCM (20 mL) was added triethylamine (1.53 mL, 11.04 mmol). The resulting mixture was cooled to 0 C before the dropwise addition of chloroacetyl chloride (325 muL, 4.05 mmol). The mixture was warmed to RT and stirred for 5 h. The reaction mixture was partitioned between a saturated aqueous solution OfNaHCO3 and DCM. The organic layer was separated and the aqueous layer extracted with DCM. The combined organic fractions were dried (Na2SO4) and concentrated in vacuo. The resulting residue was purified by column chromatography to give the title compound as a colourless oil which was a mixture of rotamers (710 mg, 66%).1H NMR (400 MHz, CDCl3): delta 1.48 (s, 9H), 2.80-2.92 (m, IH), 2.95-3.10 (m, 2H), 3.34-3.44 (m, 1AH), 3.60-3.74 (m, 21Z2H), 3.96-4.16 (m, 31AH), 4.22-4.30 (m, V2Yi), 4.32-4.40 (m, VJS) and 4.63 (bs, V2H)., 278788-66-2
As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.
Reference：
Patent; F. HOFFMANN-LA ROCHE AG; WO2009/53715; (2009); A1;,
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