Category: 115761-79-0

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 24 2-(4-Methylpiperazin-1-yl)ethyl 4-(2,4-difluorophenyl)piperazine-1-carboxylate trihydrochloride 2-(4-Methylpiperazin-1-yl)ethyl 4-nitrophenyl carbonate (Intermediate 4; 680 mg, 2.2 mmol) was dissolved in DMF (20.mL). DIPEA (0.76 mL, 4.4 mmol) and 4-(2,4-difluorophenyl)piperazine (508 mg, 2.2 mmol) were added and the reaction mixture was stirred at room temperature for 24 hours, and the reaction mixture was then concentrated in vacuo. The residue was purified by normal phase column chromatography (eluding with DCM, followed by a 200:8:1 mixture of DCM:EtOH:NH3) followed by reverse phase column chromatography (gradient eluding with MeOH in water, with 1% formic acid in each solvent, 0-100%). The residue was dissolved in DCM (10 mL) and 2M HCl in Et2O (3 mL) was added. The reaction mixture was then concentrated in vacuo to give the title compound 2-(4-methylpiperazin-1-yl)ethyl 4-(2,4-difluorophenyl)piperazine-1-carboxylate trihydrochloride (630 mg, 65%) as a white solid. Analytical HPLC: purity 100% (System A, RT=4.02 min); Analytical LCMS: purity 100% (System A, RT=5.76 min), ES+: 369.5 [MH]+; HRMS calcd for C18H26F2N4O2: 368.2024, found 368.2038.

115761-79-0, The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Biovitrum AB; US2009/281087; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

A mixture of 2- (5-amino-2- (furan-2-yl) -7H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yl) -4-methylpentanoic acid (35.5 0.1 mmol) , 1- (2, 4-difluorophenyl) piperazine (19.8 mg, 0.1 mmol) , HATU (46 mg, 0.12 mmol) and DIPEA (25.8 mg, 0.2 mmol) in DMF (3 mL) was stirred overnight. The reaction mixture was poured into H2O (15 mL) and extracted with EtOAc (20 mL x 3) . The combined organic layers were washed with brine, dried over Na2SO4, concentrated and purified by column chromatography (petroleum ether/EtOAc = 10: 1 3: 1) to give the target compound (40 mg, 74.6%) .1H NMR (400 MHz, DMSO-d6) delta 8.21 (s, 1H) , 8.15 (s, 2H) , 7.95 (m, 1H) , 7.23 (d, J = 3.2 Hz, 1H) , 7.21 -7.12 (m, 1H) , 7.02 -6.91 (m, 2H) , 6.74 (m, 1H) , 5.64 (dd, J = 9.6, 4.4 Hz, 1H) , 3.74 (m, 1H) , 3.62 (m, 2H) , 3.49 (m, 1H) , 2.94 (m, 2H) , 2.75 (m, 1H) , 2.39 (m, 1H) , 2.31 -2.19 (m, 1H) , 1.91 -1.80 (m, 1H) , 1.27 (mz, 1H) , 0.95 (d, J = 6.4Hz, 3H) , 0.83 (d, J = 6.4Hz, 3H) ppm. MS: M/e 536 (M+1)+.

115761-79-0, As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference：
Patent; BEIGENE, LTD.; ZHANG, Guoliang; SUN, Hanzi; ZHOU, Changyou; (253 pag.)WO2020/20097; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,115761-79-0

To a solution of l-(2,4-difluorophenyl)piperazine [C.A.S. 115761-79-0] (0.088 g, 0.446 mmol) in DCE (2.14 ml) stirred at r.t. was added D88 (0.1 g, 0.371 mmol) and the resulting mixture was stirred at r.t. overnight. Then, acetic acid (0.037 ml) was added and stirred at r.t. for 4 h more. Then, sodium triacetoxy-borohydride (0.87 g, 0.409 mmol) was added and stirred at r.t. overnight. The reaction mixture was neutralized with Na2CO3 (aqueous sat. solution) and extracted with DCM. The organic layer was dried (Na2SO4) and concentrated in vacuo. The crude product thus obtained was purified by column chromatography (silica gel; DCM/EtOAc from 100/0 to 50/50 as eluent). The desired fractions were collected and concentrated in vacuo. The residue obtained was triturated with DIPE to yield final compound E224 (0.107 g, 64%).

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC; ADDEX PHARMA S.A.; CID-NUNEZ, Jose, Maria; OEHLRlCH, Daniel; TRABANCO-SUAREZ, Andres, Avelino; TRESADERN, Gary, John; VEGA RAMIRO, Juan, Antonio; MACDONALD, Gregor, James; WO2010/130424; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,115761-79-0

To a solution of l-(2,4-difluorophenyl)piperazine [C.A.S. 115761-79-0] (0.088 g, 0.446 mmol) in DCE (2.14 ml) stirred at r.t. was added D88 (0.1 g, 0.371 mmol) and the resulting mixture was stirred at r.t. overnight. Then, acetic acid (0.037 ml) was added and stirred at r.t. for 4 h more. Then, sodium triacetoxy-borohydride (0.87 g, 0.409 mmol) was added and stirred at r.t. overnight. The reaction mixture was neutralized with Na2CO3 (aqueous sat. solution) and extracted with DCM. The organic layer was dried (Na2SO4) and concentrated in vacuo. The crude product thus obtained was purified by column chromatography (silica gel; DCM/EtOAc from 100/0 to 50/50 as eluent). The desired fractions were collected and concentrated in vacuo. The residue obtained was triturated with DIPE to yield final compound E224 (0.107 g, 64%).

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC; ADDEX PHARMA S.A.; CID-NUNEZ, Jose, Maria; OEHLRlCH, Daniel; TRABANCO-SUAREZ, Andres, Avelino; TRESADERN, Gary, John; VEGA RAMIRO, Juan, Antonio; MACDONALD, Gregor, James; WO2010/130424; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

General procedure: To a stirred solution of compound 5a-b (2 mmol) in dry DCM (10 mL) was added K2CO3 (1.1 equiv, 2.2 mmol, 304 mg). The mixture was cooled with a bath of ice/water, and then the appropriate N-substituted piperazine (2 equiv, 4 mmol), dissolved in DCM (2 mL), was added slowly over 30 min. The mixture was then stirred at room temperature for two hours, diluted with DCM (10 mL), washed with water (10 mL) and then with brine (10 mL). The organic layer was dried (Na2SO4), filtered and concentrated in vacuo to give a brown residue that was purified by column chromatography to furnish the derivatives 6a-aq.

115761-79-0, As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference：
Article; Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Maria Dora; Cara, Carlota Lopez; Cruz-Lopez, Olga; Salvador, Maria Kimatrai; Preti, Delia; Tabrizi, Mojgan Aghazadeh; Shryock, John C.; Moorman, Allan R.; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Bioorganic and Medicinal Chemistry; vol. 20; 2; (2012); p. 996 – 1007;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

General procedure: To a solution of 4 (100 mg, 0.23 mmol) in acetonitrile (CH3CN, 10 mL) was added the corresponding arylpiperazines (1.2 equiv) and potassium carbonate (6.0 equiv). The reaction mixture was stirred at reflux for 16 h. After cooling to ambient temperature, the reaction mixture was filtered through a Buchner funnel. After filtration the filtrate was concentrated in vacuo and the residue was purified by silica gel column chromatography using ethyl acetate/petroleum ether (1:4, v/v) as eluent to afford the corresponding products, and all compounds were recrystallized from trichloromethane and n-hexane., 115761-79-0

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Xu, Fang; Chen, Hong; Xu, Jingyi; Liang, Xue; He, Xuelan; Shao, Binhao; Sun, Xianqiang; Li, Bing; Deng, Xiaoliang; Yuan, Mu; Bioorganic and Medicinal Chemistry; vol. 23; 24; (2015); p. 7735 – 7742;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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, 5-CHLORO-2-FURAN-2-YL- [1, 2,4] triazolo [1, 5-a] pyrimidin-7-ylamine (1 g ; see Example L (b) above) was suspended in 22 mL OF DMSO along with 1.5 eq OF CSF ANZ 5 eq of aminoacetaldyde dimethyl acetal. The reaction mixture was stirred at 100 C for 10 hours. It was then cooled to room temperature and diluted with EtOAc and washed with H2O and brine, dried with NA2S04 and concentrated to afford N5-(2, 2- dimethoxy-ethyl)-2-furan-2-yl-[1, 2,4] triazolo [1, 5-a] pyrimidine-5,7-diamine. This dimethyl acetal intermediate (50 mg) was then unmasked to the corresponding aldehyde by suspending in a solution of 2 mL OF CH2CL2 and 0.2 mL of 2: 1 solution O : TFA/H20. The resulting reaction mixture was stirred at room temperature for 4 hours It was then neutralized with 0.3 mL OF ET3N. 1- (2, 4-Difluoro-phenyl) -piperazine (1.5 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) 7.72 (d, J = 1.0 Hz, 1 H), 7.35 (br s, 2 H), 7.29 (d, J = 3.6 Hz, 1 H), 6. 7-7.4 (M, 3 H), 6.75 (dd, J = 3.6 Hz, 1.0 Hz, 1 H), 5.7 (S, 1H), 3.1 (BR S, 2 H), 2. 2- 3.6 (M, 12 H). MS : m/z: 441 [M + H]+.

As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference：
Patent; BIOGEN IDEC MA INC.; WO2004/92171; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 3; Example 3A; 1 -f 2.4-difIuorophenyl)-4-(2-naphthv1sulfonyl)rhoiperazine; Step 3A; To a stirred solution of naphthalene-2-sulfonyl chloride (350 mg, 1.54 mmol) and l-(2,4-difluororhohenyl)piperazine (305.0 mg, 1.54 mmol) in anhydrous dichloromethane (5 mL) was added diisopropylethylamine (0.670 mL, 3.85 mmol). The mixture was stirred for 30 minutes. Reaction was complete as determined by TLC. The reaction mixture was purified via flash column chromatography to afford l-(2,4-difluorophenyl)-4-(2-naphthylsulfonyl)piperazine in 55% yield (327 mg) as white solid.IH NMR (400 MHz, DMSO-D6) delta ppm 3.00 – 3.07 (m, 4 H) 3.07 – 3.15 (m, 4 H) 6.94 – 7.02 (m, 1 H) 7.03 – 7.12 (m, 1 H) 7.12 – 7.21 (m, 1 H) 7.67 – 7.84 (m, 3 H) 8.11 (d, J=8.08 Hz, 1 H) 8.21 (d, J=8.59 Hz, 1 H) 8.25 (d, J=8.08 Hz, 1 H) 8.49 (d, J=I.77 Hz, 1 H). HRMS: calcd for C20H18F2N2O2S + H+, 389.11298; found (ESI-FTMS, [M+H]l+), 389.113. HPLC Method 1: room temperature, 6.658 min, 96.32%, HPLC Method 2: room temperature, 7.312 min, 99.29%., 115761-79-0

As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference：
Patent; WYETH; WO2007/92435; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

General procedure: A mixture of 1-substituted piperazines (1.5mmol), carbon disulfide (0.45mL, 7.5mmol) and finely powered anhydrous potassium phosphate (0.32g, 1.5mmol) in DMF (7.5mL) was stirred at room temperature for 30min. 6-(Bromomethyl)-2,4-diaminoquinazoline (7) (0.38g, 1.5mmol) was added to the solution, and stirring was continued at room temperature for 4h. After poured into water (100mL), the resulting precipitate was collected by filtration, which was purified by column chromatography (CC) on silica gel or recrystallization from appropriate solvent to give compounds 8a-u., 115761-79-0

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Cao, Sheng-Li; Han, Ying; Yuan, Chong-Zhen; Wang, Yao; Xiahou, Zhi-Kai; Liao, Ji; Gao, Rui-Ting; Mao, Bei-Bei; Zhao, Bao-Li; Li, Zhong-Feng; Xu, Xingzhi; European Journal of Medicinal Chemistry; vol. 64; (2013); p. 401 – 409;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

To a solution of the product from the previous step (150 mg, 0.41 mmol) in CH2CI2 (5 mL) was added in portions Et3N (126 mg, 1.25 mmol), followed by the addition in portions of l-(2,4-difluorophenyl)piperazine (82 mg, 0.41 mmol, 1.00 equiv). The resulting solution was stirred for 16 h at rt, then quenched by the addition of 15 mL H20 and extracted with 2×30 mL of EtOAc. The combined organic layers were concentrated under vacuum to afford 170 mg (92%) of the title compound as an off-white solid. LC-MS: (ES, m/z) 448

115761-79-0, 115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; CENTAURUS THERAPEUTICS; ROMERO, Donna, L.; BLITZER, Jeremy; (242 pag.)WO2019/140188; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics