With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.
103-76-4, Benzylchloroformate (4.72g, 27.69mmol) in acetonitrile (30mL) was added dropwise over 30min to a solution of 1-(2-hydroxyethyl)piperazine (3g, 23.08mmol) in water (30mL) via an isobar cylindrical funnel. The pH was maintained around 8-9 by addition of 4N NaOH. The reaction was stirred overnight at room temperature. The mixture was first extracted with dichloromethane (100mL) in order to remove the fully protected compound and then acidified with 4N HCl. The acidic aqueous phase was extracted twice with dichloromethane (2×100mL). The organic phase was washed with brine and dried over anhydrous Na2SO4. The solvent was removed in vacuum and the crude was purified by flash chromatography (0-8% of methanol in dichloromethane) to afford 22 (5.41g, 88.8%) as a colorless oil. 1H NMR (400MHz, DMSO-d6): delta 7.37-7.29 (m, 5H, CHarom.), 5.05 (s, 2H, CH2Phi), 4.41 (s, 1H, OH), 3.47 (m, 2H, HOCH2), 3.35 (m, 4H, (CH2)2NCO), 2.38-2.35 (m, 6H, CH2N, CH2NCH2). 13C NMR (100.6MHz, DMSO-d6): delta 155.04, 137.59, 129.09 (2C), 128.49, 128.22 (2C), 66.81, 60.82, 59.14, 53.51 (2C), 44.16 (3C). MS (ESI) m/z 265.02 (M+H)+.
103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.
Reference：
Article; Denoyelle, Severine; Chen, Ting; Yang, Hongwei; Chen, Limo; Zhang, Yingzhen; Halperin, Jose A.; Aktas, Bertal H.; Chorev, Michael; European Journal of Medicinal Chemistry; vol. 69; (2013); p. 537 – 553;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics