Category: piperazines

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 (synthesized according to Example 5, Step 1, 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

As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference£º
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (2016); A1;,
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169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,169447-70-5

To a solution of iodobenzene (2.08 g, 10.19 mmol) in toluene (60 mL) at rt was added (S)-tert-butyl-2-methylpiperazine-l-carboxylate (1.7 g, 8.49 mmol), Pd2(dba)3 (778 mg, 0.85 mmol) , t-BuONa (2.44 g, 25.46 mmol), XantPhos (982 mg, 1.70 mmol) under nitrogen. The reaction mixture was stirred at 100 C for 16 h, then cooled to rt and diluted with EtOAc (60 mL x 3). The combined organic layers were washed with brine, dried over Na2S04, filtered, concentrated, and purified by chromatography (silica, EtOAc/PE = 1/10) to afford (S)-tert-butyl- 2-methyl-4-phenylpiperazine-l-carboxylate (1.8 g , 6.5 mmol, 64%) as an oil. ESI-MS (EI+, m/z): 277.2 [M+H]+.

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (184 pag.)WO2018/89493; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

[0707] To a mixture of 1-[4-(trifluoromethyl)phenyl]piperazine (600 mg, 2.61 mmol) and triethylamine (660 mg, 6.52 mmol) in dichloromethane (20 ml) was added 2-chloroacetyl chloride (380 mg, 3.36 mmol) dropwise at 0 C. The resulting solution was stirred for 1 hour at room temperature. The reaction mixture was then quenched by water (80 ml) and extracted with dichloromethane (3¡Á30 ml). The organic layers were combined, dried over anhydrous magnesium sulfate, and concentrated under vacuum. The residue was purified by silica gel column chromatography using 1%-10% ethyl acetate in petroleum ether to afford 2-chloro-1-[4-[4-(trifluoromethyl)phenyl]piperazin-1-yl]ethan-1-one as a white solid (479 mg, 60%). (ES, m/z): [M+H]+ 307.1; 1H NMR (300 MHz, CDCl3): delta 7.52 (d, J=8.4 Hz, 2H), 6.97 (d, J=8.7 Hz, 2H), 4.12 (s, 1H), 3.81 (t, J=5.1 Hz, 2H), 3.72 (t, J=5.1 Hz, 2H), 3.36 (t, J=5.1 Hz, 2H), 3.30 (t, J=5.1 Hz, 2H).

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Merial Limited; Meng, Charles Q.; Long, Alan; Huber, Scot; Gurrala, Srinivas Reddy; Wilkinson, Douglas Edward; Pacofsky, Gregory; US2014/142114; (2014); A1;,
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5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5747-48-8, EXAMPLE 3:PREPARATION OF 1 1 -[4-(2-(2-HYDROXYETHOXY)-ETHYL)- I-PIPERAZINYL] DIBENZO[b,f][l,4]THIAZEPINETo a mixture of 1000 ml of organic layer (obtained from example 2), 100 grams of sodium carbonate (0.944 mol) and 6.25 grams of sodium iodide (0.042 mol), 37.5 ml of chloroethoxyethanol (0.36 mol) and 187.5 ml of N-Methyl pyrrolidone (NMP; 1.95 mol) are added and the reaction mixture is stirred at 1 10-120 degree C for about 8 hours. 1000 ml of water is added to the reaction mass and stirred for 15 min. The organic layer is separated and washed with water (2x1000ml). Organic layer is dried using Dean stark by azeotropic distillation. This organic layer on distillation under reduced pressure yields the title compound (quetiapine free base) as a viscous oil. Yield : 135g (80 % ); Purity (HPLC area%) : 98.5 %.

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; SANDOZ AG; WO2007/20011; (2007); A1;,
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20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 41D (2R)-ethyl 2-((5-((1S)-3-chloro-4-formyl-2-methylphenyl)-6-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-yl)oxy)-3-(5-(((2-(4-cyclopropylpiperazin-1-yl)ethyl)amino)methyl)-2-((2-(2-methoxyphenyl)pyrimidin-4-yl)methoxy)phenyl)propanoate To a mixture of Example 41C (53 mg) in dichloromethane (2 mL) was added 1-cyclopropylpiperazine (24 mg). The mixture was stirred for 20 minutes at room temperature before the addition of sodium triacetoxyborohydride (33 mg). The mixture was stirred at room temperature for 40 minutes. The reaction mixture was diluted with ethyl acetate (200 mL), washed with water and brine, and dried over sodium sulfate. Filtration and evaporation of the solvent provided the title compound, which was used in the next reaction without further purification. MS (ESI) m/z 1027.4 (M+H)+.

20327-23-5, 20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AbbVie Inc.; AbbVie Deutschland GmbH & Co. KG; Brady, Patrick B.; Braje, Wilfried; Dai, Yujia; Doherty, George A.; Gong, Jane; Jantos, Katja; Ji, Cheng; Judd, Andrew S.; Kunzer, Aaron R.; Lai, Chunqiu; Mastracchio, Anthony; Risi, Roberto M.; Song, Xiaohong; Souers, Andrew J.; Sullivan, Gerard M.; Tao, Zhi-Fu; Teske, Jesse A.; Wang, Xilu; Wendt, Michael D.; Yu, Yiyun; Zhu, Guidong; Penning, Thomas D.; (218 pag.)US2019/55264; (2019); A1;,
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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;,
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639068-43-2, tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of 5-(((3-chloro-5-(trifluoromethyl)benzyl)oxy)carbonyl)-4,5,6,7- tetrahydropyrazolo[l,5-a]pyrazine-2-carboxylic acid (140 mg, 0.35 mmol), tert-butyl 3,5- dimethylpiperazine-l-carboxylate (97 mg, 0.45 mmol) and HATU (198 mg, 0.52 mmol) in DMF (3 mL) was added DIPEA (90 mg, 0.69 mmol). The mixture was stirred at rt for 2 h and then concentrated. The residue was purified by column chromatography on silica gel (petroleum ether/EtOAc = 1:2) to give the Boc-protected intermediate as yellow oil (120 mg, 57percent yield). ESI-MS (M+H)+: 600.2., 639068-43-2

The synthetic route of 639068-43-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOGEN IDEC MA INC.; PENG, Hairuo; XIN, Zhili; ZHANG, Lei; SUN, Lihong; KUMARAVEL, Gnanasambandam; TAVERAS, Art; WO2014/152725; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: 1) (Cyanomethylene)tributylphosphorane (262 muL, 1.00 mmol) was added to a solution of (tetrahydrofuran-3-yl)methanol (51 mg, 0.50 mmol) and 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (97 mg, 0.5 mmol) in degassed 1,4-dioxane (2 mL) sealed in a microwave tube at rt under nitrogen. The solution was heated to 150¡ãC for 30 min in the microwave reactor and cooled to rt. 2) 1-Bromo-4-methoxybenzene (94 mg, 0.50 mmol), potassium carbonate (207 mg, 1.50 mmol) and [1,1?-Bis(diphenylphosphino)ferrocene]dichloropalladium(II) complex with CH2Cl2 (40.8 mg, 0.05 mmol) were added to the solution. The tube was sealed, evacuated and backfilled with nitrogen. Degassed water (1 mL) was added under nitrogen. The resulting mixture was stirred at 120¡ãC for 20 min. The reaction mixture was diluted with EtOAc (25 mL) and water (15 mL), the layers were separated, and the aqueous layer was extracted with EtOAc (15 mL). The combined organic layers were washed with saturated brine (15 mL). The organic layer was dried with MgSO4, filtered and evaporated to afford the crude product. The crude product was purified by preparative HPLC (Waters XSelect CSH C18 ODB column, 5mu silica, 30mm diameter, 100mm length), using decreasingly polar mixtures of water (containing 1percent by volume NH3OH (28-30percent in H2O)) and MeCN as eluents to afford 4-(4-methoxyphenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-pyrazole (89mg, 69percent) as a beige solid., 5464-12-0

Big data shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Article; Mosallanejad, Arash; Lorthioir, Olivier; Tetrahedron Letters; vol. 59; 18; (2018); p. 1708 – 1710;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.171504-98-6,Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate,as a common compound, the synthetic route is as follows.

(B) 1,4-Di-(N-tert-Butoxycarbonyl)-2-Piperazinecarboxylic Acid A solution of 1 N sodium hydroxide (1.2 mL) was added to a solution methyl 1,4-di-(N-tert-butoxycarbonyl)-2-piperazinecarboxylate (A, 290 mg) in methanol (10 mL). The mixture was stirred at room temperature for 12 hr and evaporated in vacuo. The residue was diluted with water and washed with ether. The aqueous layer was acidified with 10% citric acid and extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous sodium sulfate, and evaporated in vacuo to give the title compound (230 mg) as a colorless foam: 1H NMR (400 MHz, CDCl3) delta 1.44 (s,18H) and 4.56-4.75 (m, 1H)., 171504-98-6

The synthetic route of 171504-98-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Microcide Pharmaceuticals, Inc.; US6399629; (2002); B1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl 14-((6-(tert-butylsulfonyl)-4-((4,5-dimethyl-lH-pyrazol-3- yl)amino)quinazolin-7-yl)oxy)-3,6,9,12-tetraoxatetradecan-l-oate (200 mg, 0.300 mmol) in DCM (2 mL) was added hydrochloric acid (2.253 mL, 9.01 mmol) 4M in dioxane and the reaction was stirred at 20 C under an atmosphere of nitrogen for one hour. The volatiles were removed under vacuum, and to the resulting residue was added DCM (2 mL) and DMF (200ul), DIPEA (0.210 mL, 1.202 mmol), tert-butyl 2-methylpiperazine-l-carboxylate (0.085 mL, 0.360 mmol) and l-ethyl-3-(3- dimethylaminopropyl)carbodiimide (69.1 mg, 0.360 mmol). The reaction was stirred at room temperature under an atmosphere of nitrogen for 3 days. The reaction was diluted in 50 mL EtOAc, washed with 50 mL saturated sodium bicarbonate solution, 50 mL water, 50 mL 2 M HCI and 50 mL brine. The aqueous layer was neutralised with saturated sodium bicarbonate solution, and washed with 3 x 100 mL EtOAc. The organic layer was passed through a Biotage phase separator and concentrated under vacuum to afford the title compound (75 mg, 0.095 mmol, 32 % yield). LCMS RT= 0.83 min, ES+ve 792. (2R,5S)-Tert-butyl 5-((4-(14-((6-(tert-butylsulfonyl)-4-((3,4-dimethyl-lH-pyrazol-5- yl)amino)quinazolin-7-yl)oxy)-3,6,9,12-tetraoxatetradecan-l-oyl)-2-methylpiperazin-l-yl)methyl)- 4-(2-(6-(4-fluorobenzyl)-3,3-dimethyl-2,3-dihydro-lH-pyrrolo[3,2-b]pyridin-l-yl)-2-oxoethyl)-2- m thylpiperazine-l-carboxylate, 120737-78-2

As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CASILLAS, Linda N.; HARLING, John David; MIAH, Afjal Hussain; SMITH, Ian Edward David; RACKHAM, Mark David; (204 pag.)WO2017/182418; (2017); A1;,
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Piperazines – an overview | ScienceDirect Topics