Synthesis
GENERAL STEPS: 3-(Piperazin-1-yl)propan-1-ol (1.44 g, 10 mmol), di-tert-butyl dicarbonate (3.3 g, 15 mmol), and N,N-diisopropylethylamine (1.80 g, 15 mmol) were dissolved in dichloromethane (100 mL) and stirred at room temperature until the reaction was complete. After the reaction was complete, the reaction mixture was diluted with dichloromethane (200 mL). The organic layer was washed with saturated saline, dried over anhydrous sodium sulfate, filtered and concentrated. The residue was purified by column chromatography (eluent: dichloromethane/methanol = 20:1) to afford tert-butyl 4-(3-hydroxypropyl)piperazine-1-carboxylate as a colorless oil (2.4 g, 97% yield).
References
[1] Patent: WO2015/120049, 2015, A1. Location in patent: Page/Page column 137
[2] Patent: WO2016/191172, 2016, A1. Location in patent: Page/Page column 83
[3] Journal of Medicinal Chemistry, 2017, vol. 60, # 15, p. 6516 - 6527
[4] Patent: WO2009/10491, 2009, A1. Location in patent: Page/Page column 56
[5] Patent: US2009/99172, 2009, A1. Location in patent: Page/Page column 29
