With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.
General procedure: In a schlenk-type flask, a mixture of Pd2(dba)3 (0.023 g, 0.025mmol) and XantPhos (0.015 g, 0.025 mmol) in dry dioxane wasstirred at room temperature for 5 min. Then, NHR (2 mmol) andCs2CO3 (0.24 g, 0.75 mmol) were added and stirred for another 5min at ambient temperature. Afterwards, E-6 (F-4) (0.5 mmol)was added, and the flask was evacuated and backfilled with nitrogenfor three times. The reaction mixture was stirred at 100 C for9 h and followed by TLC until completion. After cooling, the solventwas removed under reduced pressure. The residue was purified byflash column chromatography with ethyl acetate/petroleum etherto afford compounds E-a?E-k (F-a?F-j). White solid, yield 31percent, mp: 144?146 C; 1H NMR (400 MHz,CDCl3) d: 7.51 (d, J = 1.6 Hz, 4H, PhH), 7.33 (d, J = 16 Hz, 1H, CH),7.20 (s, 2H, PhH), 6.96 (s, 1H, NH), 5.83 (d, J = 16.6 Hz, 1H, CH),5.62 (s, 1H, pyridine-H), 5.35 (s, 1H, pyridine-H), 3.34 (s, 2H,CH2), 2.80 (s, 4H, CH2), 2.68 (s, 2H, CH2), 2.45 (s, 3H, CH3), 2.14(s, 6H, CH3), 1.89 (s, 2H, CH2), 1.25 (s, 2H, CH2); 13C NMR (100MHz, CDCl3) d: 152.7, 149.8, 133.2, 132.3, 128.2, 117.9, 96.0,86.2, 51.7, 44.9, 16.3; ESI?MS: 508.2 [M+H+]. C30H33N7O (507.27)., 934-98-5
The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.
Reference：
Article; Lu, Xueyi; Yang, Jiapei; Kang, Dongwei; Gao, Ping; Daelemans, Dirk; De Clercq, Erik; Pannecouque, Christophe; Zhan, Peng; Liu, Xinyong; Bioorganic and Medicinal Chemistry; vol. 26; 8; (2018); p. 2051 – 2060;,
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