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.
115761-79-0, Example 8 N7- {2-[4-(2,4-Difluoro-phenyl)-piperazin-1-yl]-ethyl}-2-furan-2-yl- [1, 2, 4] triazolo [1, 5-C] PYRIMIDINE-5, 7-DIAMINE 7-CHLORO-2-FURAN-2-YL- [1, 2, 4] TRIAZOLO [1, 5-c] PYRIMIDIN-5-YLAMINE (1 g; see Example 1 (b) above) was suspended in 20 mL OF DMSO along with 1.5 eq of CsF and 5 eq of aminoacetaldyde dimethyl acetal. The reaction mixture was stirred at 110 oC for 18 hours. It was then cooled to room temperature and diluted with EtOAc and washed with H20 and brine, dried with NA2S04 and concentrated to afford N7-(2, 2- dimethoxy-ethyl)-2-furan-2-yl- [1, 2,4] triazolo [1, 5-c] pyrimidine-5, 7-diamine. This dimethyl acetal intermediate (40 mg, 0.13 mmol) was then unmasked to the corresponding aldehyde by suspending in a solution of 2 mL OF CH2C12 and 0.2 mL of 2: 1 solution OF TFA/H20. The resulting reaction mixture was stirred at room temperature for 4 hours. It was then neutralized with 0.25 mL of ET3N. 1- (2, 4- Difluoro-phenyl) -piperazine (40 mg, 1.5 eq; see Example 6 (a) above) 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 the title compound. 1H NMR (DMSO-d6) 8 7.60 (d, J = 1. 0 Hz, 1 H), 7.28 (br s, 2 H), 7.22 (d, J = 3.6 Hz, 1 H), 6.8-7. 3 (m, 3 H), 6.68 (dd, J = 3.6 Hz, 1.0 Hz, 1 H), 6.5 (s, 1H), 3.1 (br s, 2 H), 2.2-3. 6 (m, 12 H). MS: m/z: 441 [M + NU.
As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.
Reference£º
Patent; BIOGEN IDEC MA INC.; WO2004/92172; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics