Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

Example 1786-(3-fluorophenyl)-N-{(1S,3R)-3-[(4-methyl-3-oxopiperazin-1 -yl)carbonyl] cyclopenty^nicotinamide To a solution of (1 R, 3S)-3-({[6-(3-fluorophenyl)pyridine-3-yl]carbonyl}amino) cyclyopentanecarboxylic acid (Example 1 1 b, 49.3 mg, 0.15 mmol) and triethylamine (68.2 mg, 0.675 mmol) in dimethylformamide (1.3 mL) was added HBTU (65.2 mg, 0.172 mmol) and the solution was stirred at room temperature for 1 hour. 1-Methylpiperazin-2-one (29.4 mg, 0.195 mmol) was added and the solution was stirred at room temperature overnight. The dimethylformamide was removed by evapouration in vacuo and the residue was partitioned between water (7 mL) and ethyl acetate (7 ml_). The organic layer was separated and evaporated to give a red-brown gum which was purified by HPLC Method (B) to give 23.2 mg of the title compound (LCMS Method (A), RT 2.83 min, 100percent area ES m/z [M+] 424.19).

59702-07-7, 59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER LIMITED; WO2009/153720; (2009); A1;,
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196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of tert-butyl 4-carbamothioylpiperazine-1-carboxylate (1.31 g, 5.36 mmol) in isopropanol (15 mL), tert-butyl 3-bromo-2,4-dioxopiperidine-1-carboxylate obtained in the first step (1.3 g, 4.46 mmol) was added at rt. The reaction mixture was stirred overnight at 90 C It was cooled down to rt and evaporated under reduced pressure. Water (10 mL) was added and the desired product was extracted with diethyl ether (2 x 30 mL), dried over Na2SO4 and concentrated, affording the title product. Yield: 74% (1.42 g,yellow solid). LCMS: (Method A) 239.0 (M-Boc+H), Rt. 0.70 min, 48.39% (Max)., 196811-66-2

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; KOEK, Johannes Nicolaas; (64 pag.)WO2017/144635; (2017); A1;,
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5521-38-0, 2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5521-38-0, To a solution of 2-(4-(4-nitrophenyl)piperazin-l-yl)ethanol (3.6 g, 14.3 mmol) in MeOH (40 mL) was added Pd/C (700 mg) and the resulting mixture was stirred at r.t.overnight. The mixture was filtered, and the filtrate was concentrated to afford 2-(4-(4- aminophenyl)piperazin-l-yl)ethanol (2.8 g, 88% yield) as yellow solid.

The synthetic route of 5521-38-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NEUPHARMA, INC.; QIAN, Xiangping; ZHU, Yong-Liang; WO2015/27222; (2015); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, A mixture of 3-bromomethylbenzoic acid (4.30 g, 20 mmol), 1-methylpiperazin-2-one (2.3 g, 20 mmol),38 and powdered potassiumcarbonate (2.76 g, 20 mmol) in ethanol (50 mL) was stirredfor 17 h at room temperature. The solvent was evaporated off underreduced pressure to give a residue which was treated with HCl(10 mL of 2 M) and extracted with EtOAc. The combined extractswere washed with water, dried and the solvent was evaporatedoff under reduced pressure to give 8, which was recrystallised fromEtOAc/hexane to give a cream crystalline solid, mp 161?166 C; 1HNMR (DMSO-d6) d 2.63 (t, J = 5.5 Hz, 2H), 2.80 (s, 3H), 2.96 (s, 2H),3.26 (t, J = 5.5, 2H), 3.61 (s, 2H), 7.46 (d, J = 8.0 Hz, 2H), 7.90 (d,J = 8.0 Hz, 2H), 12.9 (br s, 1H).

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Manley, Paul W.; Blasco, Francesca; Mestan, Ju?rgen; Aichholz, Reiner; Bioorganic and Medicinal Chemistry; vol. 21; 11; (2013); p. 3231 – 3239;,
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3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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 N). A solution of copper (II) sulfate (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 residue used directly in the next step., 3022-15-9

The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Robichaud, Albert; Mitchell, Ian S.; Lee, Taekyu; Chen, Wenting; US2002/177596; (2002); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Step AF.1 : 4-[3-(4-Chloro-5-iodo-pyrrolo[2,3-d]pyrimidin-7-yl)-cyclobutylmethy.]-1-methyl- piperazin-2-oneMethylpiperazin-2-one HCI salt (290 mg, 1.2832 mmol), 3-(4-Chloro-5-iodo-pyrrolo[2,3- d]pyrimidin-7-yl)-cyclobutanecarbaldehyde (Step AF.2, 265 mg, 0.733 mmol), and DIPEA (1.306 mL, 7.33 mmol) were dissolved in 1,2-dichloroethane (32 mL) and stirred at RT for 45 min. After adding NaBH(OAc)3 (409 mg, 1.832 mmol) the reaction mixture was stirred for 35 min at RT. Then, concentrated NaHC03 solution (50 mL) was added and the reaction mixture was extracted with DCM ( 40 mL, 4 x). The combined organic phases were washed with brine (10 mL), dried (Na2S04), and the solvent was evaporated, the resulting residue was purified by means of a Sepacore Control chromatographer (Buchi, Flawil, Switzerland) using RediSept silica gel column (12 g) (30 mL min; DCM: 10 min, DCM -> DCM/MeOH/NH3(99.45:0.5 :05) in 30 min) yielding the title compound as white solid. HPLC (Method B) tRel = 1.724 min. HPLC/MS tR = 0.52 min, M+H = 441.1. 1H NMR (600 MHz, DMSO-d6) delta ppm 8.16 (s, 1H), 7.74 (s, 1H), 6.15 (s/b, 2H), 5.00 (quintet, 1H), 3.26 (t, 2H), 2.95 (s, 2H), 2.78 (s, 3H), 2.65 (t, 2H), 2.56 (t, 2H), 2.50/2.15 (m/m, 2H/2H), 2.29 (m, 1H).

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; IRM LLC, a Delaware Limited Liability Company; CHEN, Bei; FAIRHURST, Robin, Alec; FLOERSHEIMER, Andreas; FURET, Pascal; JIANG, Songchun; LU, Wenshuo; MARSILJE, Thomas, H.; VAUPEL, Andrea; WO2011/64211; (2011); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

694499-26-8, Triphosgene (1.04 g, 3.5 mmol) and ClCH2CH2Cl (20 mL) were added into a 100 mL round-bottomed flask, and stirred at room temperature until triphosgene was completely dissolved and the system appears colorless and transparent. The reaction system was placed in an ice-salt bath and stirred, 3-iodo-4-methyl aniline (1.64 g, 7 mmol) in ClCH2CH2Cl (20 mL) solution was slowly added dropwise, and the system appears yellow milky. After the addition was complete, the mixture was stirred at room temperature for 4 hours. After the reaction was complete by TLC monitoring, Et3N (1.43 g, 14 mmol) was added, and stirred at room temperature for 0.5 hour. 4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylaniline (1.87 g, 7 mmol) was added and stirred at room temperature for 16 hours, and then the starting materials were monitored by TLC and LC-MS until the reaction was complete. The volatiles were removed by distillation under reduced pressure, and the residue was extracted with ethyl acetate (30 ml*3) and H2O (30 mL). The organic phases were combined, dried over anhydrous Na2SO4, concentrated and purified by column chromatography, to give a yellow solid. ESI-MS mz: [M+H]+=533.2.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nanjing Sanhome Pharmaceutical Co., Ltd.; Wang, Yong; Zhao, Liwen; Zhang, Wenping; Chen, Hongyan; Bi, Sheng; Gao, Yiping; Chen, Hongbin; Liu, Yang; Xu, Xin; Zhang, Cang; US2015/152088; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture of (S)-tert-butyl 2-(hydroxymethyl)piperazine-l -carboxylate (602.7 mg, 2.79 mmol) and (S)-2-methoxyoxirane (308.9 mg, 3.4 mmol) in ethanol (10 mL) was heated at 120 C for 30 min using microwave. The mixture was concentrated to dryness. The residue was purified with flash column chromatography on silica gel using 1 -10% methanol in dichloromethane to afford a oil as the product (794.6 mg) in 94% yield. NMR (500 MHz, Chloroform-*/) delta 4.11 (br, 1H), 3.93 – 3.80 (m, 2H), 3.41 (dd, J = 9.7, 3.7 Hz, 1H), 3.36 (s, 3H), 3.33 (dd, J = 9.7, 6.0 Hz, lH), 3.25 (br, 2H), 3.06 (d, J = 1 1.6 Hz, 1H), 2.89 (br, 2H), 2.79 (d, J = 1 1.2 Hz, 1H), 2.47 (dd, J = 12.7, 9.1 Hz, 1H), 2.49 – 2.33 (m, 1 H), 2.30 – 2.21 (m, 2H), 1.43 (s, 9H). MS for C,4H28N205: 305.2 (MH+).

1030377-21-9, As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference£º
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.373608-48-1,tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a 50 mL RBF was added tert-butyl 4-(3-aminopropyl)piperazine-1-carboxylate (1.105 g, 4.54 mmol), DCE (Volume: 10.32 ml), 3-methylpicolinaldehyde (.5 g, 4.13 mmol) and STAB-H (1.575 g, 7.43 mmol). The reaction was stirred overnight then diluted with DCM and quenched with 2M NaOH. The organic layer was dried with Na2SO4, filtered and concentrated to a yellow oil which was purified via silica gel chromatography (DCM 2 minutes, 10% B(80:20:3, DCM:MeOH:NH4OH) 5 minutes and 50% B 9 minutes) to afford tert-butyl 4-(3-(((3-methylpyridin-2-yl)methyl)amino)propyl)piperazine-1-carboxylate (0.88 g, 2.53 mmol, 61 % yield).1H NMR (400 MHz, CDCl3): delta = 8.37 (d, J= 5.0 Hz, 1H), 7.42 (d, J= 7.3 Hz, 1H), 7.07 (dd, J= 7.6, 4.8 Hz, 1H), 3.88 (s, 2H), 3.43 (t, J= 5.2 Hz, 4H), 2.79 (t, J= 6.8 Hz, 2H), 2.45 (t, J= 7.2 Hz, 2H), 2.39 (t, J= 5.2 Hz, 4H), 2.30 (s, 3H), 1.78 (pent, J= 7.0 Hz, 2H), 1.45 (s, 9H);, 373608-48-1

As the paragraph descriping shows that 373608-48-1 is playing an increasingly important role.

Reference£º
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; WILSON, Robert James; NGUYEN, Huy Hoang; KIM, Michelle Bora; WILSON, Lawrence; MILLER, Eric James; TAHIROVIC, Yesim Altas; TRUAX, Valarie; KAISER, Thomas; (311 pag.)WO2018/156595; (2018); A1;,
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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.

Example 1O 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(2R)-1,4-dioxan-2-ylmethyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide EXAMPLE 1N (170 mg), EXAMPLE 1J (340 mg), 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (150 mg), and 4-dimethylaminopyridine (130 mg) were stirred in CH2Cl2 (5 mL) overnight. N1,N1-dimethylethane-1,2-diamine (0.19 mL) was then added and the mixture was stirred for 90 minutes. Dichloromethane (15 mL) was added, and the reaction mixture was washed with 10% acetic acid:0.75% NaCl in water (2*12 mL). The combined aqueous layers were back-extracted with dichloromethane, and the combined organics were washed with brine, and dried over Na2SO4. After filtration and concentration, the crude material was chromatographed on silica gel with 3/7 dichloromethane/ethyl acetate. The material was then chromatographed on silica gel with 1.5-2.5% CH3OH in dichloromethane. The material was triturated with CH3CN to afford the title compound. 1H NMR (400 MHz, dimethylsulfoxide-d6) delta ppm 11.65 (s, 1H), 8.55 (t, 1H), 8.54 (d, 1H), 8.01 (d, 1H), 7.81 (dd, 1H), 7.50 (m, 3H), 7.32 (d, 2H), 7.07 (d, 1H), 7.02 (d, 2H), 6.66 (dd, 1H), 6.37 (m, 1H), 6.18 (d, 1H), 3.77 (m, 3H), 3.63 (m, 2H), 3.47 (m, 2H), 3.31 (m, 2H), 3.06 (br m, 4H), 2.74 (br s, 2H), 2.19 (br m, 4H), 2.13 (br m, 2H), 1.94 (br m, 2H), 1.37 (t, 2H), 0.90 (s, 6H)., 1235865-77-6

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Tao, Zhi-Fu; Wang, Xilu; Wendt, Michael; Souers, Andrew; Judd, Andrew; Kunzer, Aaron; Sullivan, Gerard; US2014/275082; (2014); A1;,
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