With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.
The dimethyl acetal intermediate (40 mg, 0.13 mmol) from subpart (a) above was suspended in 2 mL of CH2Cl2 and 0.2 mL of 2: 1 solution of TFA/H2O was added. The resulting reaction mixture was stirred at room temperature for 4 hours. It was then neutralized with 0.25 mL of triethylamine. 1-(2,4-Difluoro-phenyl)-piperazine (40 mg, 1.5 eq. , prepared by reacting piperazine with 1-bromo-2,4-difluorobenzene according to the procedure described in WO 01/92264 A1), was added, followed by 140 mg of Na(OAc)3BH. The resulting reaction mixture was stirred at room temperature for 2 hours. It was then concentrated and then purified by preparative HPLC to afford N5-{2-[4-(2,4-difluoro-phenyl)-piperazin-1-yl]-ethyl}-2-furan-2-yl-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine. 1H NMR (DMSO-d6) delta 7.90 (br s, 2 H), 7.80 (d, J = 1.0 Hz, 1 H), 7.05 (d, J = 3.6 Hz, 1 H), 7.10-7.50 (m, 3 H), 6.68 (dd, J = 3.6 Hz, 1.0 Hz, 1 H) 3.20-2.75 (m, 12 H) ppm. MS: m/z: 442 [M + H] +., 115761-79-0
115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; BIOGEN IDEC MA INC.; WO2004/92170; (2004); A2;,
Piperazine – Wikipedia
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