New learning discoveries about 1-(2,4-Difluorophenyl)piperazine

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

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, General procedure: To a solution of 4 (100 mg, 0.23 mmol) in acetonitrile (CH3CN, 10 mL) was added the corresponding arylpiperazine or phenylpiperidine (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 (1/5, v/v) as eluent to afford the corresponding products, and all compounds were recrystallized from trichloromethane and n-hexane.

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

Reference:
Article; Chen, Hong; Liang, Xue; Xu, Fang; Xu, Bingbing; He, Xuelan; Huang, Biyun; Yuan, Mu; Molecules; vol. 19; 8; (2014); p. 12048 – 12064;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 115761-79-0

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

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

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) -2-phenylpropanoic acid (50 mg, 0.13 mmol) , 1- (2, 4-difluorophenyl) piperazine (25 mg, 0.13 mmol) , HATU (59 mg, 0.16 mmol) and DIEA (33 mg, 0.26 mmol) in DMF (5 mL) was stirred at rt for 2 hrs. The solution was added with water (10 mL) , extracted with ethyl acetate (10 mL) and washed with brine (10 mL) . The organic layer was dried, concentrated and purified by column chromatography (PE: EA = 2: 1) and preparative TLC (DCM: MeOH = 20: 1) to get the desired product (20 mg, 28%) .1H NMR (400 MHz, DMSO-d6) delta 8.31 (s, 1H) , 8.08 (br. s, 2H) , 7.95 (d, J = 4.0Hz, 1H) , 7.30-7.11 (m, 7H) , 6.92-6.86 (m, 2H) , 6.74 (d, J = 4.0Hz, 1H) , 3.71 (br. s, 2H) , 3.45-3.40 (m, 2H) , 3.16-2.90 (m, 4H) , 2.35 (s, 3H) ppm. MS: M/e 570 (M+1)+

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

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

Downstream synthetic route of 1-(2,4-Difluorophenyl)piperazine

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

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

To 48 (26 mg, 0.1 mmol) in DMF (1 mL) was added 2,4- difluorophenylpiperazine (20 mg, 0.1 mmol). The reaction mixture was stirred for 1.5 hours. To the crude mixture was added 2-thiopheneethylamine (14 pL, 0.12 mmol), DIEA (38 pL, 0.22 mmol) and HATU (42 mg, 0.11 mmol). The reaction was stirred overnight at room temperature. The reaction mixture was poured into water and extracted with EtOAc. The combined organic layers were washed with 0.1 N NaOH, 0.1 N HCI, and brine; dried over sodium sulfate and concentrated in vacuo to yield 49 as an oil (49 mg, 94%). HPLC- MS tR = 2.10 min (UV254 nm); mass calculated for formula C24H27F2N3O6S 523.2, observed LCMS m/z 524.4 (M+H) ; purity > 95% (ELSD).

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

Reference£º
Patent; SCHERING CORPORATION; WO2005/121130; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 115761-79-0

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

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

Take 50mL one-mouthed flask, were successively added 2-(1-methylcyclopropyl)methoxy-5-(methylsulfonyl)benzoic acid (50mg, 0.19mmol), 1-(2,4-difluorophen-1-yl)piperazine (36mg, 0.18mmol), HATU (108mg, 0.29mmol), TEA (0.10mL, 0.66mmol), DMF (10mL), the reaction at room temperature overnight, saturated sodium chloride (20 mL), and extracted with ethyl acetate (20mL * 3), the organic phase with anhydrous sodium sulfate, and concentrated to dryness to give a crude product, after reverse phase preparative chromatography crude was pure 35mg, yield: 42%., 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; Shanghai Hansoh BioMedical Co., Ltd.; Jiangsu Stockhausen Pharmaceutical Group Co., Ltd.; Liao, Jianchun; Yu, Hongping; Xu, Yaochang; Chen, Jianghua; Zhang, Shaobao; Xiu, Wenhua; Liu, Zhaomin; (48 pag.)CN105712952; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-(2,4-Difluorophenyl)piperazine

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

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

General procedure: The substituted piperazine (0.01 mol) was added to a magnetically stirred solution of compound 3 and anhydrous K2CO3 in dry DMF (25 mL). The reaction mixture was heated at 80C for 6-8 h and the reaction was monitored by TLC. The resulting solid was filtered off at room temperature and subjected to anion exchange to convert into its chloride form. The crude product was chromatographed on an Al2O3 column, eluted with CHCl3/CH3OH (9:1, v/v) to give the proposed compound., 115761-79-0

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

Reference£º
Article; Mistry, Bhupendra; Keum, Young-Soo; Kim, Doo Hwan; Journal of Chemical Research; vol. 39; 8; (2015); p. 470 – 474;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 1-(2,4-Difluorophenyl)piperazine

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

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.

EXAMPLE 14 7-(2-(4-(2,4-Difluorophenyl)piperazin-1-yl)propyl)-2-(furan-2-yl)-7H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, Method A To a suspension of NaH (13.0 mg, 60 wt % in mineral oil, 0.3 mmol) in 2.0 mL of anhydrous DMF is added 2,4-difluorophenylpiperazine (63 mg, 0.32 mmol). After stirring the solution at RT for 15 min, a solution of 1-(5-amino-2-(furan-2-yl)-7H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-7-yl)propan-2-yl methanesulfonate (80 mg, 0.21 mmol) in 1.5 mL of anhydrous DMF is added. The reaction is stirred at RT under N2 for 12 h. However, very little of product formation is seen by LC/MS. The reaction is then heated at 100 C. for 12 h to complete the reaction as detected by LC/MS. The crude reaction mixture is purified by chromatography to afford 7-(2-(4-(2,4-difluorophenyl)piperazin-1-yl)propyl)-2-(furan-2-yl)-7H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine: 1H NMR (400 MHz, CD2Cl2) delta 1.05 (d, 3H, J=6.83 Hz), 2.62-272 (m, 2H), 2.83-3.05 (m, 8H), 3.13-3.22 (m, 1H), 4.10 (dd, 1H, J=14.06 Hz and 6.64 Hz), 4.27 (dd, 1H, J=13.96 Hz and 7.52 Hz), 6.61 (dd, 1H, J=3.51 Hz and 1.76 Hz), 6.73 (d, 1H, J=3.51 Hz), 6.76-6.96 (m, 4H), 7.00 (d, 1H, J=3.32 Hz), 7.22 (dd, 1H, J=3.51 Hz and 0.78 Hz), 7.63 (dd, 1H, J=1.76 HZ and 0.78 Hz)., 115761-79-0

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

Reference£º
Patent; Moorman, Allan R.; US2008/242672; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-(2,4-Difluorophenyl)piperazine

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

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

General procedure: Arylpiperazine or phenylpiperidine (1.2 equiv) and potassium carbonate (6.0 equiv) were added to a solution of 4 (100 mg, 0.23 mmol) in acetonitrile (CH3CN, 10 mL). The reaction mixture was heated to 85 C and stirred for 16 h. Afterward the mixture was cooled to room temperature. The reaction mixture was filtered, and the filtrate was concentrated in vacuo. Then the residue was purified by chromatography on silica-gel column (petroleum ether: ethyl acetate = 15:1, v/v) to obtain the corresponding products (5-28), and then to a solution of above corresponding products in ethyl acetate was added dropwise 4 M HCl solution in ethyl acetate (50 mL), keeping stirring for 0.5 h. Then the resulting solid was collected by filtration to give corresponding hydrochloride salts as a white solid., 115761-79-0

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

Reference£º
Article; Chen, Hong; Wang, Cai-Lu; Sun, Tao; Zhou, Zhan; Niu, Jiang-Xiu; Tian, Xiu-Mei; Yuan, Mu; Bioorganic and Medicinal Chemistry Letters; vol. 28; 9; (2018); p. 1534 – 1539;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 115761-79-0

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

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 compounds 21a, b (0.5mmol) in anhydrous DCM (20mL) was added BOP-Cl (0.6mmol), Et3N (1.5mmol) and the amino parts (3, 4, 8a-l, 9a-d, 13a,b, 14a,b, 16a-i, 18, 22a,b and 23) at room temperature. The mixture was stirred overnight at the same temperature, and washed by H3PO4 solution (1%), saturated NaHCO3 solution and brine, dried over anhydrous MgSO4, filtered, and concentrated. The residue was purified by Flash column chromatography (DCM/MeOH, 0-10%) to afford the crude target compounds as yellow solids. The solid was further purified by treating with EtOAc and hexane (11mL, 1: 10) to yield the target compounds (24, 25, 26a-l, 27a-g, 28a,b, 29a,b, 30a-i, 31, 32a,b, 33).

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

Reference£º
Article; Lv, Kai; Li, Linhu; Wang, Bo; Liu, Mingliang; Wang, Bin; Shen, Weiyi; Guo, Huiyuan; Lu, Yu; European Journal of Medicinal Chemistry; vol. 137; (2017); p. 117 – 125;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 115761-79-0

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

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

New learning discoveries about 115761-79-0

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

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.

1.0 g of 1-(2,4-fluorophenyl)-piperazine (Compound A-1c), 15 mL of acetic acid was added to the sealed reactor, followed by the addition of 3 mL of hydrated formaldehyde, 1.0 g of sodium acetate;The reaction mixture was warmed to 60 C and stirred for 18 hours;The residue obtained was purified to give 1-(2,4-fluorophenyl)-4-methylpiperazine (A-c) (0.92 g, yield 86%)., 115761-79-0

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

Reference£º
Patent; Chengdu Ruizhi Chemical Co., Ltd.; Zhou Zhen; Zhu Mingkui; Li Kun; (9 pag.)CN109897014; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics