Month: June 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

13889-98-0, Example 83 1-acetyl-4-{[2-(5-{1-[4-(methylsulfonyl)phenyl]-2-(tetrahydro-2H-pyran-4-yl)ethyl}-1H-pyrrol-2-yl)pyridin-4-yl]methyl}piperazine To a solution of 2-(5-{1-[4-(methylsulfonyl)phenyl]-2-(tetrahydro-2H-pyran-4-yl)ethyl}-1H-pyrrol-2-yl)pyridine-4-carbaldehyde (170 mg) in 1,2-dichloroethane (5 mL) was added 1-acetylpiperazine (115 mg), and the mixture was stirred at room temperature for 30 min. To the reaction mixture was added sodium triacetoxyborohydride (250 mg), and the mixture was stirred overnight at room temperature. The reaction mixture was diluted with ethyl acetate, washed with saturated aqueous sodium hydrogen carbonate and saturated brine, dried (MgSO4) and concentrated. The residue was subjected to basic silica gel column chromatography, and the title compound (180 mg, yield 85%) was obtained as a pale-yellow amorphous solid from a fraction eluted with ethyl acetate-methanol (19:1, volume ratio). MS:551(MH+). 1H NMR (300 MHz, CDCl3) delta1.29 – 1.50 (3 H, m), 1.54 – 1.60 (1 H, m), 1.82 – 1.97 (1 H, m), 2.08 (3 H, s), 2.36 – 2.50 (4 H, m), 3.04 (3 H, s), 3.20 – 3.37 (2 H, m), 3.40 – 3.53 (4 H, m), 3.58 – 3.69 (2 H, m), 3.86 – 3.99 (2 H, m), 4.14 – 4.22 (1 H, m), 6.15 (1 H, t, J=3.0 Hz), 6.59 – 6.72 (1 H, m), 6.93 – 7.06 (1 H, m), 7.36 – 7.53 (3 H, m), 7.87 (2 H, d, J=8.3 Hz), 8.32 (1 H, d, J=4.5 Hz), 9.28 (1 H, brs).

The synthetic route of 13889-98-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Takeda Pharmaceutical Company Limited; EP2149550; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Manufacturing example 10: 1-(4-benzoylpiperazine-1-yl)propan-2-one [Show Image] 0.10 g (0.53 mmol) 1-benzoylpiperazine and potassium carbonate 0.22 g (1.58 mmol, 3.0 eq.) were added to 5 ml acetonitrile and 0.05 g (0. 53 mmol, 1.0 eq.) chloroacetone were added dropwise slowly at room temperature. After mixing for one hour, 5 ml purified water were added, and the reaction mixture was extracted with 10 ml ethylacetate three times. After collecting organic layer, drying with anhydrous magnesium sulfate, and concentrating with decompression, residues obtained were purified with silicagel chromatography (mobile phase: dichloromethane/methnol=10:1) and 0.11 g (83%) target compound as yellow syrup were yielded. 1H NMR(400MHz,CDCl3) 2.18(3H,s), 2.41-2.69(4H,m), 3.27(2H,s), 3.42-3.54(2H,m), 3.81-3.93(2H,m), 7.40-7.46(5H,m)

13754-38-6, 13754-38-6 1-Benzoylpiperazine 762654, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Yang Ji Chemical Co., Ltd.; EP2452939; (2012); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred mixture of 4-chloro-5-[3-(chloromethyl)-1-[[2-(difluoromethyl)phenyl]methyl]- 1H,4H,5H,6H,7H-pyrazolo[4,3-c]pyridin-5-yl]-2-(oxan-2-yl)-2,3-dihydropyridazin-3-one (150 mg, 0.286 mmol, 1 equiv.) and 4-methylpiperazin-2-one (97.95 mg, 0.858 mmol, 3.00 equiv.) in ACN (10 mL) were added KI (47.48 mg, 0.286 mmol, 1.00 equiv.) and t-BuONa (41.24 mg, 0.429 mmol, 1.50 equiv.) in portions at rt under nitrogen atmosphere. The final reaction mixture was irradiated with microwave radiation for 2 h at 100 degrees C. The reaction was monitored by LCMS. The mixture was allowed to cool down to rt. The resulting mixture was concentrated under reduced pressure. The resulting mixture was extracted with EtOAc (3 x 100 mL). The combined organic layers were washed with brine (2 x 50 mL), dried over anhydrous Na2SO4. After filtration, the filtrate was concentrated under reduced pressure. This resulted in 4-chloro-5- (1-[[2-(difluoromethyl)phenyl]methyl]-3-[(4-methyl-2-oxopiperazin-1-yl)methyl]- 1H,4H,5H,6H,7H-pyrazolo[4,3-c]pyridin-5-yl)-2-(oxan-2-yl)-2,3-dihydropyridazin-3-one (110 mg, 63.87%) as a yellow oil. The resulting mixture was used in the next step directly without further purification.

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GOLDFINCH BIO, INC.; YU, Maolin; DANIELS, Matthew, H.; HARMANGE, Jean-christophe, P.; TIBBITTS, Thomas, T.; LEDEBOER, Mark, W.; WALSH, Liron; MUNDEL, Peter, H.; MALOJCIC, Goran; (860 pag.)WO2019/55966; (2019); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of Benzoylpiperazine XXX To a stirred solution of 2-methylpiperazine (10.0 g, 0.1 mol) in dry CH2Cl2 (500 ml) under argon was added a solution of 1.0 M Me2AlCl or Et2AlCl in hexanes (100 ml, 0.1 mmol) and methyl benzoate (12.4 ml, 0.1 mmol) at room temperature. The reaction mixture was then stirred for 2 days before 2N NaOH (200 ml) was added. Aqueous layer was extracted with EtOAc (3*100 ml). The combined organic layer was dried over MgSO4 and concentration of solution provided 20.0 g of crude product (98%), with was pure enough for the further reactions., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference：
Patent; Bristol-Myers Squibb Company; US6469006; (2002); B1;,
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

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 1-Z-piperazine (8.5 g, 38.5 mmol) in dry THF (100 mL), 1,1-thiocarbonyldimidazole (12.37 g, 69.4 mmol) was added and the mixture was stirred at 60 °C for 5 h. It was concentrated under vacuum and NH3 in EtOH (2 N, 300 mL) was added at 0°C. The resulting mixture was stirred at 55°C for 8 h in an autoclave. It was diluted with water (100 mL) and extracted with DCM (2 x 100 mL). The DCM layer was washed with water (100 mL), dried over in anhydrous Na2SO4 and concentrated. The resulting crude product was purified by flash chromatography to afford the title product. Yield: 87percent (7 g, white solid). 1H NMR (400 MHz, DMSO-d6): delta 7.51 (s, 2H), 7.38-7.31 (m, 5H), 5.1 (s, 2H), 3.78 (m, 4H), 3.43-3.33 (m, 4H). LCMS: (Method A) 280.2 (M+H), Rt. 2.33 min, 95.4percent (Max).

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh, S.; GIRI, Awadut Gajendra; (247 pag.)WO2017/144639; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(5-Chloro-1-methyl-1H-pyrrolo[2,3-c]pyridin-2-yl)(2,6-difluoro-3,5-dimethoxyphenyl)methanol (1000 mg, 2.8 mmol), 4-(4-ethylpiperazin-1-yl)phenylamine (900 mg, 3.6 mmol), Pd2 (dba) 3 (540 mg,0.6 mmol), XantpHos (700 mg, 1.2 mmol), Cs2CO3 (2.0 g, 6 mmol) and toluene (15 ml) were mixed and stirred overnight under 110 C, Ar. The reaction solution was directly dried by column chromatography (dichloromethane:methanol = 97:3) to give compound (2,6-difluoro-3,5-dimethoxyphenyl) (5-((4-(4-) Ethyl piperazin-1-yl)phenyl)amino)-1-methyl-1H-pyrrolo[2,3-c]Pyridin-2-yl)methanone 1.1 g, yield 75%.

115619-01-7, As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

Reference：
Patent; Shanghai Xin Qibo Biological Technology Co., Ltd.; Wang Zhaoyin; Ma Jianbin; (39 pag.)CN110092798; (2019); A;,
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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

A solution of tert-butyl-3 -(2-bromophenyl)propyl (methoxymethyl)carbamate (250 mg, 0.70 mmol), ()-2-methylpiperazine (140 mg, 1.40 mmol), Pd2(dba)3 (64 mg, 0.07 mmol), BINAP (87 mg, 0.14 mmol), t-BuONa (202 mg, 2.10 mmol) in PhMe (10 mL) was stirred at 80C for 16 h under N2 atmosphere, then concentrated, and purified by chromatography (silica, PE/EtOAc = 10/1 to 5/1) to afford (S)-tert-butyl-methoxymethyl(3 -(2-(3 -methylpiperazin- 1- yl)phenyl)propyl)carbamate (150 mg, 0.40 mmol, 57%) as a yellow oil. ESI-MS (EI, m/z): 378.0 [M+H]., 74879-18-8

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (565 pag.)WO2018/89433; (2018); 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.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

4-fluoro-3-nitrobenzenesulfonamide (235 mg, 1.06 mmol, 1.00 eq) and2 – ((1H-pyrrolo [2,3-b] pyridin-5-yl) oxy) -4- (4 – ((4′-chloro-5,5-dimethyl- , 6-tetrahydro- [1,1′-biphenyl] -2-yl) methyl) piperazin-1-yl) benzoic acid(600 mg, 1.06 mmol, 1.0 eq) (see Example 1, Step 14) was added to 6 mL of phosphorus oxychloride and reacted at 85 C for 5 h. The reaction solution was poured into 20 mL of ice water and extracted with EA (10 mL x 3). The organic phase was separated, dried over anhydrous sodium sulfate, dried over the column, PE / EA (v / v) = 2/1 and DCM / EtOH (v / v) = 10/1 as an eluent to give 830 mg of a white solid product in 100% yield.

1235865-77-6, As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference：
Patent; Sunshine Lake Pharma Co.,Ltd.; Kou, Yuhui; Hu, Bolin; Jiang, Haigang; Ye, Jiuyong; Liu, Zhiqiang; Xie, Hongming; Zhang, Yingjun; (42 pag.)CN106565706; (2017); A;,
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.350684-49-0,tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

[0408] A mixture of intermediate 33 (0.12 g, 0.33 mmol), 4-(4-amino-benzoyl)- pirhoerazine-1-carboxylic acid tot-butyl ester (0.12 g, 0.45 mmol), Pd2(dba)3 (0.030 g, 0.037 mmol), Xantphos (0.038 g, 0.075 mmol) and cesium carbonate (0.33 g, 1.1 mmol) were suspended in dioxane (6 mL), sealed in a microwave reaction tube and irradiated with microwaves at 160 0C for 15 min. The reaction was decanted and the organic phase concentrated in vacuo. The residue was purified by silica gel chromatography (25%-100% EtOAc in Hexanes). Product was then treated with 20 mL of 20% TFA solution in DCM. Solvents then removed by rotary evaporation. Resulting material purified by HPLC to afford the title compound as a white solid (0.045 g, 26%).[0409] 1H NMR (500 MHz, DMSOd6): delta 1.11 (s, 9H)5 2.14 (s, 3H), 2.82 (br s, 4H), 3.48 (br s, 4H), 7.24 (d, J= 9.0 Hz, 2H), 7.51-7.53 (m, 2H), 7.55 (s, IH), 7.71 (d, J= 9.0 Hz, 2H)5 7.94 (S5 IH)5 8.06-8.08 (m, 2H), 8.65 (br s, IH), 9.25 (s, IH). MS (ES+): m/z 524 (M+H)+.

350684-49-0, The synthetic route of 350684-49-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TARGEGEN, INC.; WO2007/53452; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics