26 Sep 2021 News Downstream synthetic route of 1-Methylpiperazine

109-01-3, As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

4-Bromobenzonitrile 52a (1.00 mmol) was placed in a reaction tube. Toluene (10 mL), Cs2CO3 (2.50 mmol), Pd2dba3 (0.03 mmol), Xphos (0.12 mmol) and piperazine (2.50 mmol) were added. The tube was sealed and the suspension was warmed to 110 C and stirred for 12 h. After this time, water was added and the mixture was extracted with EtOAc, washed with brine, dried over Na2SO4 and concentrated. The residue waxs purified by flash chromatography (hexanes/EtOAc 3:1). White solid. M.p. 186-188 C. Yield: 78%. 1H-NMR (delta, ppm): 7.44 (d, 2H, J=8.8 Hz), 6.82 (d, 2H, J=8.8 Hz), 3.31-3.29 (m, 4h), 2,53-2,51 (m, 4H), 2.31 (s, 3H).13C-NMR (delta, ppm): 153.31, 133.40, 120.04, 114.16, 100.02, 54.54, 46.99, 46.03. HRMS (ESI) [M + H]+ calculated for C12H15N3: 201.1266, found: 201.1293.

109-01-3, As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference:
Article; La Pietra, Valeria; Sartini, Stefania; Botta, Lorenzo; Antonelli, Alessandro; Ferrari, Silvia Martina; Fallahi, Poupak; Moriconi, Alessio; Coviello, Vito; Quattrini, Luca; Ke, Yi-Yu; Hsing-Pang, Hsieh; Da Settimo, Federico; Novellino, Ettore; La Motta, Concettina; Marinelli, Luciana; European Journal of Medicinal Chemistry; vol. 150; (2018); p. 491 – 505;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics