Heterocyclic Building Blocks-piperazine

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

138775-02-7, (R)-4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

PREPARATIVE EXAMPLE 5; The title compound from Prepartive Example 4 (9.6 gm, 26.3 mmol) was dissolved in absoluteEtOH (100 mL) in a hydrogenation vessel. The vessel was flushed with N2 and 10% Pd/C (3.0g, 50% by weight with water) was added. The mixture was hydrogenated at 55 psi of H2 for 18 hours during which time a precipitate formed. When the reaction was complete (TLC, 30% MeOH/NH3/CH2Cl2), the reaction mixture was filtered through a pad of celite, and the pad washed with EtOH followed by distilled H2O. The filtrate was evaporated to ?1/3 the volume and distilled H2O (200 mL) was added. The resulting solution was extracted with EtOAc (contains pure N,N-Di-Boc-2-carboxy-piperazine which was saved). The water layer was evaporated to dryness with azeotropic removal of residual H2O with methanol (2X) to give pure product (3.98g)., 138775-02-7

The synthetic route of 138775-02-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; EP1140904; (2005); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 5.6 g (35 mmol) 2-chloro-4-nitropyridine, 5.75 g (37 mmol) 1-cyclo- pentyl piperazine and 4,59 g (35 mmol) N,N-diisopropylethylamine in 35 ml DMF and 12 ml water was heated to 95 0C for 3 h . After evaporation to dryness the residue was taken up in 150 ml NaHCO3 aq. and 150 ml ethyl acetate. The aqueous phase was extracted two times with 150 ml ethyl acetate each and the combined organic phases were washed twice with 10O1 ml NaHCO3 aq each and 100 ml NaCl aq. sat. and dried with MgSO4 and evaporated to dryness. The residue was purified with columnchromatography to^yield 2.85 g (29 %) l-cyclopentyl-4~(4-nitro-pyridin-2-yl)- piperazine (m/e): 277.3 (MH+; 100%) and 4.47 g (47 %) l-(2-chloro-pyridin-4-yl)-4- cyclopentyl-piperazine (m/e): 266.3 (MH+; 100%)., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference：
Patent; F.HOFFMANN-LA ROCHE AG; WO2006/63718; (2006); A1;,
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

A mixture of 2,3-dichloropyrazine (2.80 g, 18.8 mmol), racemic 2- methylpiperazine (1.88 g, 18.8 mmol) and K2CO3 (3.90 g, 28.2 mmol) in acetonitrile (25 mL) was heated at 65 C for 15 h with stirring. The reaction mixture was filtered and concentrated. The crude product was purified by flash chromatography on silica gel using CHCl3/MeOH (15: 1) as eluent to give 3.2 g (79%) of the title compound. MS m/z 213 (M+H) +., 109-07-9

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

Reference：
Patent; BIOVITRUM AB; WO2004/9586; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics