With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.
To a solution of 5-bromobenzofuran (250 mg, 1.27 mmol, 1.0 equiv.) and 2-methylpiperazine (508.4 mg, 5.08 mmol, 4.0 equiv.) in toluene (7 mL) was added PdCl2[P(o-Tol)3]2 (30 mg, 0.04 mmol, 0.04 equiv.) followed by sodium tert-butoxide (183 mg, 1.91 mmol, 1.5 equiv.). The resulting mixture was heated to 100 C. with stirring under nitrogen. After stirred at same temperature for 16 hours, the reaction mixture was cooled to room temperature and then diluted with ethyl acetate (100 mL). The resulting solution was washed with water, brine and then dried over Na2SO4. After removal of solvent, the crude product was purified by chromatography to give 132 mg (48% yield) of 1-Benzofuran-5-yl-3-methyl-piperazine. 1H NMR (400 MHz, CDCl3), delta (ppm): 7.56 (d, 1H), 7.39(d, 1H), 7.10 (d, 1H), 7.00 (dd, 1H), 6.69 (m, 1H), 3.44 (d, 2H), 306 (m, 3H), 2.72 (dt, 1H), 2.38 (d, 1H), 1.14 (d, 3H).
As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.
Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
Piperazine – Wikipedia
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