Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.,4318-42-7

A mixture of 2-(morpholine-4-carbonyl)-1-(2,2,2-trifluoro-ethyl)-1H-indole-5-carboxylic acid (100 mg, 0.28 mmol) and 1,1′-carbonyl-diimidazole (59 mg, 0.37 mmol) in tetrahydrofuran was stirred at room temperature overnight. 1-Isopropylpiperazine (72 mg, 0.56 mmol) was then added and the mixture was stirred for an additional 40 min. The volatiles were removed in vacuo and the residue was purified by flash chromatography on silica gel with dichloromethane:methanol:ammonia (95:5:0.25 v/v) as eluant, to give 90 mg (68percent) of the desired compound as an off-white solid.MS (TIC): 467.5 (M+H+)

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
Patent; Nettekoven, Matthias; Plancher, Jean-Marc; Richter, Hans; Roche, Olivier; Taylor, Sven; US2007/244125; (2007); 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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, Example 169 Amethyl 3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)benzoate; To a solution of 3-(methoxycarbonyl)benzoic acid (0.9 g, 5 mmol) in dichloromethane (20 mL), 1-hydroxybenzotriazole (0.75 g, 5.5 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (1.06 g, 5.5 mmol) and triethyl amine (2 mL) were added. The mixture was stirred at room temperature for 30 min, and then cyclopropyl(piperazin-1-yl)methanone (1.0 g, 5 mmol) was added and the mixture was stirred at room temperature for 16 h. The resulting mixture was added water (50 mL) and extracted with dichloromethane (100 mL×3), the organic phase was washed with sodium bicarbonate, brine and concentrated. The crude product was purified by column chromatography (silica gel, petroleum ether/ethyl acetate 20:1 to 2:1), 0.95 g of methyl 3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)benzoate as an oil was obtained, Yield 60%. 1H-NMR (400 MHz, CDCl3) 0.80-0.82 (m, 2H), 1.00-1.04 (m, 2H), 1.24-1.27 (m, 1H), 3.25-3.78 (m, 8H), 3.94 (s, 3H), 7.52-7.55 (t, J=7.6 Hz, 1H), 7.63-7.65 (d, J=7.6 Hz, 1H), 8.09-8.14 (m, 2H); LC-MS (ESI) m/z: 317(M+1)+.

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LEAD THERAPEUTICS, INC.; US2009/197863; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5317-33-9, 3-(4-Methylpiperazin-1-yl)propan-1-ol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5317-33-9, Step b:4.775 g (30 mmol) of 3-(4-methylpiperazin-1-yl)propan-1-ol are dissolved in 20 ml of dioxane, 20 ml of 4 N HCl in dioxane are added, and the mixture is evaporated to dryness. This residue is triturated in MTBE, filtered off with suction and dried. This solid (6.7 g) is suspended in 50 ml of acetonitrile, and 6 g (30 mmol) of trichloromethy choroformate, dissolved in 10 ml of acetonitrile, are added at 0. The mixture is stirred at room temperature for a further 48 h. The reaction mixture is filtered off with suction, washed with acetonitrile and dried, giving a white solid, m.p. 248-250 (decomposition).

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG; US2011/269756; (2011); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

4-Bromobenzonitrile 52a (1.00 mmol) was placed in a reaction tube. Toluene (10 mL), Cs2CO3 (2.50 mmol), Pd2dba3 (0.03 mmol), Xphos (0.12 mmol) and piperazine (2.50 mmol) were added. The tube was sealed and the suspension was warmed to 110 C and stirred for 12 h. After this time, water was added and the mixture was extracted with EtOAc, washed with brine, dried over Na2SO4 and concentrated. The residue waxs purified by flash chromatography (hexanes/EtOAc 3:1). White solid. M.p. 186-188 C. Yield: 78%. 1H-NMR (delta, ppm): 7.44 (d, 2H, J=8.8 Hz), 6.82 (d, 2H, J=8.8 Hz), 3.31-3.29 (m, 4h), 2,53-2,51 (m, 4H), 2.31 (s, 3H).13C-NMR (delta, ppm): 153.31, 133.40, 120.04, 114.16, 100.02, 54.54, 46.99, 46.03. HRMS (ESI) [M + H]+ calculated for C12H15N3: 201.1266, found: 201.1293.

109-01-3, As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference：
Article; La Pietra, Valeria; Sartini, Stefania; Botta, Lorenzo; Antonelli, Alessandro; Ferrari, Silvia Martina; Fallahi, Poupak; Moriconi, Alessio; Coviello, Vito; Quattrini, Luca; Ke, Yi-Yu; Hsing-Pang, Hsieh; Da Settimo, Federico; Novellino, Ettore; La Motta, Concettina; Marinelli, Luciana; European Journal of Medicinal Chemistry; vol. 150; (2018); p. 491 – 505;,
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

Step 1: 2-(4-Cyclopentyl-piperazin-1-yl)-pyrimidin-4-ylamine (Intermediate 1) A mixture of 0.5 g (3.86 mmol) 2-chloro-4-pyrimidinylamine (commercially available) and 1-cyclopentyl-piperazine (commercially available) in 1 mL DMF was heated to 70 C. for 16 h. The residue after filtration washed with diethyl ether and dried to yield 0.49 g (51%) of the title compound (intermediate 1) as white solid. MS (m/e): 284.3 (MH+)., 21043-40-3

The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Nettekoven, Matthias Heinrich; Roche, Olivier; US2007/281921; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2,5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Triethylamine (3.83 mL) and di-tert-butoxydicarbonate (6.32 mL) were added to a mixed solution of piperazin-2-one (2.5 g) in tetrahydrofuran (50 mL) and methanol (50 mL) at room temperature, and the resultant mixture was stirred for 4 hours. The reaction solvent was evaporated under reduced pressure, water and ethyl acetate were added to the residue thus obtained, and the mixture was partitioned. The organic layer was washed with water and saturated saline in this order, and then the washing water layer was combined for further extraction with ethyl acetate. The organic layers were combined and dried over anhydrous magnesium sulfate. After separation by filtration, a residue obtained by evaporating the solvent under reduced pressure was solidified using ethyl acetate-hexane, thus to obtain 3-oxopiperazine-1-carboxylic acid tert-butyl ester (3.6 g, 72%). 1H-NMR(400MHz, CDCl3)delta: 1.48(9H, s), 3.37-3.40(2H, m), 3.62-3.65(2H, m), 4.01(2H, s), 6.32(1H, br s).1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester To a mixed solution of piperazin-2-one (5.07 g) in tetrahydrofuran (50 mL) and methanol (50 mL), triethylamine (7.76 mL) and di-tert-butyl dicarbonate ester (12.17 g) were added at room temperature, and the resultant mixture was stirred for 4 hours. The solvent of the reaction solution was evaporated under reduced pressure, diethyl ether was added to a residue thus obtained, and the precipitated solid was filtered, to obtain 3-oxopiperazine-1-carboxylic acid tert-butyl ester (9.36 g, 92%). 1H-NMR(400MHz, DMSO-d6)delta: 1.40(9H, s), 3.15(2H, br), 3.45(2H, br), 3.81(2H, br), 8.03(1H, br). ESI-MSm/z: 201(M+H)+.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, Preparation of l-methyl-4- f2-(4-{4- beta-ftrifluoromethyl) fl,2,41 triazolo f4,3- blpyridazin-6-vHpiperazin-l-yl}phenoxy)ethyllpiperazin-2-one2-(4- {4-[3-(Trifluoromethyl)[ 1 ,2,4]triazolo[4,3-b]pyridazin-6-yl]piperazin- 1 – yl}phenoxy)ethyl methanesulfonate (300 mg, 0.62 mmol), 1 -methylpiperazin-2-one (339 mg, 0.93 mmol), DIPEA (0.644 mL, 3.70 mmol) and sodium iodide (9.24 mg, 0.06 mmol) were suspended in DMA (3 mL) and sealed into a microwave tube. The reaction was heated to 1500C for 1 hour in the microwave reactor and cooled to room temperature. The reaction mixture was absorbed on to silica, evaporated and purified by flash silica chromatography, elution gradient 0 to 5percent MeOH in DCM. Pure fractions were evaporated to dryness to afford a gum, which was further purified by ion exchange chromatography using an SCX column, eluting from the column with 2M ammonia/MeOH. Further purification by flash silica chromatography, elution gradient 0 to 5percent MeOH in DCM gave 1 -methyl-4-[2-(4- {4-[3-(trifluoromethyl)[l ,2,4]triazolo[4,3-b]pyridazin-6-yl]piperazin- 1 – yl}phenoxy)ethyl]piperazin-2-one (44.0 mg, 14.14percent) as a solid.IH NMR (399.9 MHz, CDC13) delta 2.78 (4H, m), 2.89 (3H, s), 3.15 (4H, m), 3.22 (2H, s), 3.28 (2H, t), 3.71 (4H, m), 4.01 (2H, t), 6.80 (2H, d), 6.86 (2H, d), 7.05 (IH, d), 7.89 (IH, d); m/z = 505 [M+H]+.

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert, Hugh; RABOW, Alfred, Arthur; WO2010/131022; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 250 mL round bottom flask equipped with a stir bar was charged with Example 1U (1.96 g) and anhydrous dichloromethane (160 mL) at room temperature under nitrogen. The mixture was cooled to 0° C. in an ice bath, and 2-(4-methylpiperazin-1-yl)ethanamine (0.395 mL) was added via a syringe. The mixture was stirred for 25 minutes at 0° C., and sodium triacetoxyborohydride (156 mg) was added as a solid. The reaction mixture was stirred for 15 minutes at 0° C., and powdered activated 3 angstrom molecular sieves were added (1.96 g). The reaction mixture was stirred 2 hours at 0° C., and was allowed to stir and warm slowly to room temperature overnight. LC/MS indicated one major peak with a mass that corresponded to desired product. The reaction mixture was quenched with dichloromethane and water. The layers were separated, and aqueous layer was extracted with dichloromethane and 10percent methanol/dichloromethane. The aqueous layer was neutralized with saturated aqueous NaHCO3 mixture, and was extracted one more time with 10percent methanol/dichloromethane. The combined extracts were washed with saturated aqueous NaHCO3 and brine, dried with Na2SO4, filtered, and concentrated. The residue was dissolved in dichloromethane and was purified on a Grace Reveleris X2 MPLC using a Teledyne Isco RediSep? Rf gold 750 g silica gel column eluting with a gradient of 0-20percent of methanol/dichloromethane over 40 minutes. The mixed fractions were purified on a Grace Reveleris X2 MPLC using a Teledyne Isco RediSep? Rf gold 330 g silica gel column eluting with a ramp of 0-15percent of methanol/dichloromethane over 40 minutes to collect additional title compound. The material from both columns was combined to provide the title compound. 1H NMR (501 MHz, dimethyl sulfoxide-d6) delta ppm 8.61 (m, 2H), 7.47 (m, 2H), 7.39 (d, 1H), 7.17 (m, 7H), 7.04 (td, 1H), 6.96 (dd, 1H), 6.67 (d, 1H), 6.51 (d, 1H), 5.84 (dd, 1H), 5.06 (m, 2H), 4.07 (ddq, 2H), 3.90 (d, 1H), 3.75 (s, 3H), 3.68 (dd, 2H), 3.50 (d, 1H), 3.17 (m, 1H), 3.08 (m, 1H), 2.90 (m, 2H), 2.65-2.20 (m, 10H), 2.14 (s, 3H), 1.67 (s, 3H), 1.09 (t, 3H). MS (ESI) m/z 928.4 (M+H)+., 934-98-5

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
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;,
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.2762-32-5,Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

2-Piperazinecarboxylic acid and 2-chloro-1, 3-pyrimidine were stirred with triethylamine and MeOH. After stirring overnight at reflux, the mixture was filtered and concentrated in vacuo to give the desired compound which was used directly in Step B (MH+ = 209).

2762-32-5, As the paragraph descriping shows that 2762-32-5 is playing an increasingly important role.

Reference：
Patent; SCHERING CORPORATION; PHARMACOPEIA DRUG DISCOVERY, INC.; WO2005/68460; (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.25057-77-6,1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

A solution of 7-fluoro-1H-quinazoline-2,4-dione (4.1 g, 23 mmol), dimethylpiperazine (6.2 mL, 46 mmol), and tripropylamine (8.7 mL, 46 mmol) in dioxane (55 mL), was cooled to 0 C. and treated with phosphorous oxychloride (6.4 mL, 68 mmol). The reaction mixture was heated to 100 C. for 1 h, cooled to ambient temperature and stirred an additional 16 h. Chloroform (about 200 mL) was added and the mixture was slowly poured over ice. After neutralizing to pH>10 with 25% NaOH (about 30 mL), the organic layer was separated. The aqueous layer was extracted again with chloroform, and the combined organic extracts were dried over sodium sulfate, filtered and concentrated. Silica gel chromatography (10% ethyl acetate in hexanes) afforded 3.7 g (58%) of the desired product as a light brown solid., 25057-77-6

As the paragraph descriping shows that 25057-77-6 is playing an increasingly important role.

Reference：
Patent; Caprathe, Bradley William; Glase, Shelly Ann; Konstantinou, Zissis; Schelkun, Robert Michael; Sheehan, Susan M.; Thomas, Anthony Jerome; Yuen, Po-Wai; US2005/96327; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics