With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.
To a solution of(s)-i -boc-2-(hydroxymethyl)piperazine (5.0 g, 23.12 mmol) in i,2-dichloroethane (100 mL) was added benzaldehyde (7.04 mL, 69.4mmol). The resulting mixture was then stirred at room temperature for 30 mm, and then sodium triacetoxyborohydride (6.85 mL, 46.2 mmol) was added. The resulting mixture was then stirred at room temperature overnight. Then, the mixture was quenched with saturated NaHCO3 (20 mL) and was stirred at room temperature for 10 mm. The organic layer was collected and aqueous layer wasextracted with EtOAc (1 x 30 mL). The combined organic extracts were then dried over Mg504 and concentrated in vacuo. Chromatographic purification of the residue (silica gel, 0% to 100% EtOAc/heptane) provided (5)-tert-butyl 4- benzyl-2-(hydroxymethyl)piperazine- 1 -carboxylate (5.86 g, 19. 13 mmol, 83% yield) as an oil. MS (ESI, +ve ion) m/z 307.3 (M+H)., 1030377-21-9
The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; AMGEN INC.; HARRINGTON, Paul E.; ASHTON, Kate; BROWN, Sean P.; KALLER, Matthew R.; KOHN, Todd J.; LANMAN, Brian Alan; LI, Kexue; LI, Yunxiao; LOW, Jonathan D.; MINATTI, Ana Elena; PICKRELL, Alexander J.; STEC, Markian M.; TAYGERLY, Joshua; (991 pag.)WO2018/183418; (2018); A1;,
Piperazine – Wikipedia
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