Month: June 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

General procedure: General procedure for the synthesis of 15b-15u. To a solution ofcompound 13a (0.41 g, 1.06 mmol) in 2-butanol (5 mL), 1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-amine (0.196 g, 1.27 mmol)and trifluoroacetic acid (94 mL) were added in a sealed tube. Thereactionwas heated at 95 C for 18 h. The reaction mixturewas thenallowed to cool to room temperature. The mixture was transferredto a round-bottom flask and then the solvent was removed underreduced pressure. The residue was dissolved in DCM (2.0 mL) andTFA (2.0 mL), and the resulting mixture was stirred for 5 h at roomtemperature. The solvent was removed under reduced pressure,and the residue was neutralized with saturated NaHCO3 aqueoussolution. The water layer was extracted with DCM. The organiclayer was combined and washed with brine, dried over Na2SO4,filtered, concentrated, and purified by silica gel chromatography toafford 15a as a yellow solid (0.264 g, 65% for two steps).

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Article; Yu, Lei; Huang, Minhao; Xu, Tianfeng; Tong, Linjiang; Yan, Xiao-e; Zhang, Zhang; Xu, Yong; Yun, Caihong; Xie, Hua; Ding, Ke; Lu, Xiaoyun; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 1107 – 1117;,
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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Method 27 (3R, 5S)-3,5-Dimethyl-1-(4-nitrophenyl)piperazine; 1-Fluoro-4-nitrobenzene (lOg, 70. 87mmol) and (2R, 6S)-2, 6-dimethylpiperazine (17g, 148. 83mmol) were heated in acetonitrile (25ml) at 70°C for 2h. The solution was concentrated in vacuo, then the residue was partitioned between DCM and water + sat. sodium hydrogen carbonate. The organic extract was washed with water (4 times), brine, dried and concentrated to give the title compound as a yellow solid which was dried in vac oven overnight at 50°C (16.13g, 97percent). NMR (400MHz) 1.04 (d, 6H), 2.39 (m, 2H), 2.77 (m, 2H), 3.89 (dd, 2H), 7.02 (d, 2H), 8.03 (d, 2H); m/z 236.

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/75461; (2005); 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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, To a solution of 1-boc piperazine (5.0 g, 26.88 mmol) in dry THF (50 mL), 1,1-thiocarbonylimidazole (5.48 g, 29.56 mmol) was added at room temperature and stirred for 2 h. The reaction mixture was heated at 50C for 1 h. It was cooled down to 0 C and methanolic ammonia solution (50 mL, 7 N) was added. The mixture was stirred at 60C for 20 h. It was then diluted with water and extracted with EtOAc. The organic layer was dried over anhydrous Na2SO4 and concentrated under vacuum. The crude product was purified by flash chromatography to give the title compound. Yield: 92% (4.0 g, white solid). 1H NMR (400 MHz, DMSO-d6): delta 9.2 (m, 2H), 3.16-3.14 (m, 2H), 2.49-2.48 (m, 6H), 1.30 (s, 9H). LCMS: (Method A) 246.2 (M+H), Rt. 2.93 min, 95.3% (Max).

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (2016); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.,3022-15-9

Step A. To a solution of piperazine-2-carboxylic acid dihydrochloride (10 g, 49 mmol) in 40 ml water was added an aqueous solution of sodium hydroxide (39 ml, 2.5 M). A solution of copper (II) sulfate pentahydrate (6.5 g, 26 mmol) in 80 ml water was added, and the deep blue solution was cooled to 5 C. Sodium bicarbonate (5 g, 59 mmol) was added in one portion, followed by the dropwise addition of benzylchloroformate (7.7 ml, 54 mmol) in 40 ml dioxane over 10 minutes. Sodium bicarbonate was added as needed to maintain a basic solution. The reaction was allowed to warm to rt and was stirred for 16 h. The precipitate was filtered and dried to afford 4-carbobenzyloxypiperazine-2-carboxylic acid, copper chelate used directly in the next step.

As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference：
Patent; Robichaud, Albert; Mitchell, Ian S.; Lee, Taekyu; Chen, Wenting; US2002/177596; (2002); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

197638-83-8, 1-Boc-4-(4-Formylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 19 terf-Butyl 4-(4-(6-bromo-7-(4-(4-chlorobenzyl)piperazin-1-yl)-3H-imidazo[4,5- b]pyridin-2-yl)benzyl)piperazine-1-carboxylate To a mixture of 5-bromo-4-[4-(4-chloro-benzyl)-piperazin-1-yl]-3-nitro-pyridin-2- ylamine (0.043 g, 0.10 mmol) and EtOH (6.0 mL) was added tert-butyl 4-(4- formylbenzyl)piperazine-1-carboxylate (0.040 g, 0.13 mmol) followed by a freshly prepared aqueous solution of Na2S2theta4 (1 M; 0.40 mL, 0.40 mmol). The reaction mixture was stirred at 80 0C for 24 h, then allowed to cool to room temperature and concentrated in vacuo. The residue was absorbed on silica gel, the free-running powder was placed on a 10 g isolute silica column, and elution with a gradient of methanol (0 to 7%) in ethyl acetate / dichloromethane (v:v; 1 :1 ) afforded the title compound as a pale yellow solid (0.036 g, 53%). 1H-NMR (500 MHz, DMSO-d6) 1.39 (s, 9H, OC(CH3)3), 2.33 (br t, J = 4.7 Hz, 4H), 2.61 (br s, 4H), 3.33 (br s, 4H), 3.67 (br s, 4H) (4 x piperazine N(CH2)2), 3.56 (s, 2H) and 3.57 (s, 2H) (NCH2-C6H4CI and C6H4CH2, 7.41 (m, 4 H, C6H4CI), 7.47 (d, J = 7.6 Hz, 2H) and 8.14 (d, J = 7.6 Hz, 2H) (3,5-C6H4 and 2,6-C6H4), 8.23 (s, 1 H, imidazo[4,5-197638-83-8, As the paragraph descriping shows that 197638-83-8 is playing an increasingly important role.

Reference：
Patent; CHROMA THERAPEUTICS LTD.; WO2009/1021; (2008); 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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step A. 4-{2-Fluoro-4-[(R-tetrahvdro-furan-3-carbonyl)-amino1-phenyl)- piperazine-1-carboxylic acid tert-butyl ester. A mixture of 4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (0.7 g, 2.4 mmol), (R)-tetrahydro-furan-3-carboxylic acid (0.33 g, 2.9 mmol) and HATU (1.1 g, 2.9 mmol) was dissolved into DMF (15.0 ml.) and stirred for 1 h at room temperature. The resulting mixture was diluted with ethyl acetate (200 mL) and washed with 1 N NaOH (30 mL) and then with water (2x 200 mL), dried (Na2SO4), filtered and concentrated to dryness to yield a residue. Chromatography of the residue (SiO2, 0-5 % acetone/DCM) yielded the title compound. MS (ESI) mass calculated for C20H28FN3O4, 393.46, m/z measured, 394.6 [M+H]+1H NMR (CDCI3): 7.50-7.40 (m, 2H), 7.1 1-7.06 (m, 1 H), 6.86 (t, J = 9.0, 1 H), 4.09-3.98 (m, 2H), 3.97-3.90 (m, 1 H), 3.88-3.80 (m, 1 H), 3.62-3.54 (m, 4H), 3.08-2.92 (m, 5H), 2.30-2.20 (m, 2H), 1.48 (s, 9H).

154590-35-9, As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of (R)-2-methylpiperazine (7 g, 70 mmol, Aldrich) in DCM (200 mL) and DIEA (6.7 mL, 38.5 mmol, Aldrich) was added benzyl chloroformate (5 mL, 35 mmol, Aldrich) dropwise at 0 C. The mixture was then warmed up to RT and was stirred for 16 h. The solvents were removed and the residue was purified on silica gel using ISCO Combiflash system with DCM/2M methanolic ammonia gradient to give the title compound as light yellow oil. MS (ESI, positive ion) m/z: 235 (M+1)., 75336-86-6

75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Gore, Vijay Keshav; Ma, Vu Van; Norman, Mark H.; Ognyanov, Vassil I.; Xi, Ning; US2006/84640; (2006); 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.923565-99-5,(R)-1-Cbz-2-methylpiperazine,as a common compound, the synthetic route is as follows.,923565-99-5

To a room temperature solution of (iotaR)-benzyl 2-methylpiperazine-l-carboxylate (1.7 g, 7.2 mmol, 1.0 equiv) and and 3-amino-2-fluorobenzaldehyde (1.0 g, 7.2 mmol, 1.0 equiv) in THF (10 mL) was added NaHB(OAc)3 (3.84 g, 18.1 mmol, 2.5 equiv) as a solid in one portion. After stirring at room temperature for 1.5 h, the reaction was complete, as determined by LCMS. The remaining reducing reagent was quenched by the careful addition of aq. satd. NaHCtheta3, and the mixture was diluted with EtOAc. The layers were separated and the organic layer was washed with aq. satd. NaHCtheta3 and brine, dried over sodium sulfate and concentrated in vacuo to provide (/?)-benzyl 4-(3-amino-2-fluorobenzyl)-2-methylpiperazine- 1-carboxylate (2.8 g, >100% mass recovery). The material was used without further purification. LCMS m/z (APCI) = 358.5 (M+H).

923565-99-5 (R)-1-Cbz-2-methylpiperazine 40424346, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; CYTOKINETICS, INC.; WO2007/70683; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

197638-83-8, 1-Boc-4-(4-Formylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 11 terf-Butyl 4-(4-(6-chloro-7-(4-((6-(trifluoromethyl)pyridin-3-yl)methyl)piperazin-1-yl)- 3H-imidazo[4,5-/3]pyridin-2-yl)phenyl)piperazine-1-carboxylate To a mixture of 5-chloro-3-nitro-4-(4-((6-(trifluoromethyl)pyridin-3- yl)methyl)piperazin-1-yl)pyridin-2-amine (0.100 g, 0.24 mmol, 1 eq), EtOH (4.3 mL) and DMF (0.57 mL), te/t-butyl-4-(4-formylphenyl)tetrahydro-1-(2H)pyrazine carboxylate (0.077 g, 0.26 mmol, 1.1 eq) was added followed by a freshly prepared aqueous solution of Na2S2O4 (1 M; 0.72 mL, 0.72 mmol). The reaction mixture was heated at 85C for 24 h, then allowed to cool to room temperature and diluted with DCM and a few drops of aqueous NH3 until complete dissolution was observed. This solution was deposited on two preparative silica TLC plates and eluted with DCM/MeOH (v/v; 94:6). The title compound was obtained after trituration with diethyl ether as an off-white solid (0.042 g, 27%); 1H-NMR (500Mz, DMSO-c/6): 1.43 (s, 9H, C(CH3J3), 2.60-2.67 (m, 4H, piperazine N(CH2J2), 3.27 (t, 4H, J = 5.2 Hz, piperazine N(CH2)2), 3.45-3.51 (m, 4H, piperazine N(CH2J2), 3.66-3.72 (m, 4H, piperazine N(CH2)2), 3.73 (s, 2H, NCH2), 7.06 (d, J = 9.0 Hz, 2H, ArH, C6H4), 7.90 (dd, 1H, pyridine H), 8.03 (d, J = 9.0 Hz, 2H, ArH1 C6H4), 8.04 (s, 1 H, imidazo[4,5-]pyridine 5- H), 8.06-8.11 (m, 1H, pyridine H ), 8.75-8.78 (m, 1H, pyridine H), 13.19 (br s, 1H, imidazo[4,5-ib]pyridine N-H); LC (Method B) – MS (ESI, m/z) 4.93 min – 657/659 [(M+H)+, Cl isotopic pattern]; ESI-HRMS: Found: 657.2675, calculated for C32H37CIF3N8O2 (M+H)+: 657.2671.

197638-83-8, The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHROMA THERAPEUTICS LTD.; WO2009/1021; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3-4-3 Preparation of 2-[3-fluoro-4-(BOC-piperazino)]phenylamino-6-chloro-3-nitropyridine To 100ml of methanol were added 2.75g (14.2mmol) of 2,6-dichloronitropyridine and 2.38ml (17.0mmol) of triethylamine and 4.2g (14.2mmol) of [3-fluoro-4-(BOC-piperazino)]aniline obtained in Preparation Example 3-4-2 was then added thereto, followed by reaction at room temperature (20 to 30C) for about 24 hours. After the reaction was complete, the reactant was filtered, washed with 20ml of methanol and then dried under vacuum at about 40C to afford 4.47g (yield: 70%) of the desired compound. Mass (M+): 452.0 1H-NMR (DMSO-d6): 1.42(s, 9H), 2.96(t, 4H), 3.48(m, 4H), 7.01(d, 1H), 7.07(t, 1H), 7.34(d, 1H), 7.53(d, 1H), 8.53(d, 1H), 10.08(s, 1H)., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Dong Wha Pharm. Co., Ltd.; EP2394993; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics