Month: September 2021

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of ferf-butyldimethylsilyl chloride (1.53 g, 10.17 mmol) in DCM (10 ml) was added dropwise to (S)-4-N-Boc-2-hydroxymethyl-piperazine (2 g, 9.25 mmol) and triethylamine (2.58 ml, 18.49 mmol) in DCM (50 ml) at 20C over a period of 5 minutes under air. The resulting solution was stirred at 20C for 16 hours then evaporated to dryness. The residue was purified by flash silica chromatography, elution gradient 0 to 5% EtOH in EtOAc. Pure fractions were evaporated to dryness to afford ferf-butyl (S)-3-(((ferf-butyldimethylsilyl)oxy)methyl)piperazine-l-carboxylate (2.84 g, 93%) as a colourless oil. 1H NMR (500 MHz, CDCI3) 0.00 (s, 6H), 0.84 (s, 9H), 1.40 (s, 9H), 2.48 (s, 1H), 2.6 – 2.87 (m, 3H), 2.92 (d, 1H), 3.41 (dd, 1H), 3.52 (s, 1H), 3.85 (s, 2H)., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (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.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

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

To a solution of piperazine-2-carboxylic acid dihydrochloride (25.0 g, 123 mmol), dioxane (180 ml) and 5N aqueous sodium hydroxide solution (90 ml) was added dropwise di-tert-butyl dicarbonate (62.7 g, 288 mmol) under ice-cooling. The mixture was stirred at room temperature for 4 hr, and the solvent was evaporated under reduced pressure. The residue was washed with ether, and acidified to pH=2-3 with concentrated hydrochloric acid under ice-cooling, and the mixture was extracted with ethyl acetate. The extract was dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure to give the object product (31.5 g, 77.6%) as a solid. 1H-NMR (CDCl3) delta; 1.44 (18H, s), 2.87 (1H, br s), 3.08-3.23 (2H, m), 3.76-4.10 (2H, m), 4.51-4.75 (2H, m), 5.07 (1H, br s).

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Matsumoto, Takahiro; Kamo, Izumi; Nomura, Izumi; US2009/318412; (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.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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.393781-70-9,(R)-1-Boc-2-Ethylpiperazine,as a common compound, the synthetic route is as follows.,393781-70-9

The original compound 82a is4-chloro-N- (1-methyl-1H-pyrazol-4-yl) pyrimidin-2-amine (627 mg, 3.00 mmol)And N, N-dimethylformamide (20 mL)Into a single-mouth bottle,Then compound 90b is(R) -2-Ethylpiperazine-1-carboxylic acid tert-butyl ester(632mg, 3.0mmol)And cesium carbonate (1.95g, 6.0mmol)Into a single-mouth bottle,The reaction was carried out at 90 C for 16 hours.Add the reaction solution after washingEthyl acetate extraction (100mL * 3),Combined organic phases,After washing with water and saturated saline,Dry and concentrated,Purification by column (ethyl acetate / methanol = 20/1) gave compound 90c as a pale yellow solid, namely(R) -2-ethyl-4- (2-((1-methyl-1H-pyrazol-4-yl) amino) pyrimidine-4-yl) piperazine-1-carboxylic acid tert-butyl ester(740 mg, 55% yield).

The synthetic route of 393781-70-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Jiaxing Tekeluo Biological Technology Co., Ltd.; Xing Li; Li Guanqun; Wang Xiaolei; Cai Yuting; Jiang Xiang; Pan Xiang; Zhu Wenhao; Wang Yang; Wang Zengquan; (51 pag.)CN110862376; (2020); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, EXAMPLE 3 4-((4-methyl-1-piperazinyl)methyl)aniline (I-c) Crude I-a (8.5g, 36.2mmol), FeO(OH)/C, 2.0 g as catalyst and 95% ethanol (100 ml) were added into a 500 mL single neck flask, which was refluxed. Into the reaction system were added slowly and dropwise a mixture of 25 mL hydrazine hydrate and 20 mL 95% ethanol. The depletion of the starting materials was confirmed by TLC (methanol: chloroform = 1:15). Suction filtration was performed while the reaction mixture was hot. The filter cake was washed with hot ethanol twice (30 ml *2). After removal of the solvent under reduced pressure, white solid was obtained, which was dried under vacuum to give 6.7 g (I-c); Yield: 90.3%. The product was used for subsequent reaction without further purification. 1H-NMR[300MHz, DMSO-d6]: delta2.1 (3H, s, -CH3), 2.3-2.5 (8H, m, -CH2-*4), 3.5 (2H, s, -CH2-), 4.0(2H, s, -NH2), 7.5 (2H, d, J = 8.7 Hz, ArH), 8.1 (2H, d, J = 8.7 Hz, ArH).

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference：
Patent; China Pharmaceutical University; LU, Tao; WANG, Yue; CHEN, Yadong; LU, Yi; WANG, Zhanwei; JIN, Qiaomei; YANG, Taotao; LIN, Guowu; GUO, Qinglong; ZHAO, Li; EP2955185; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,129799-15-1

Potassium carbonate (1 .2 g, 8.7 mmol) was added to a solution of 3-(2-bromo-thiazol-4-yl)-5-(2,6-difluoro-phenyl)-4,5-dihydro-isoxazole (1.25 g, 3.6 mmol) and 1-N-Boc-2-piperazinecarboxylic acid methyl ester (1 .1 g, 4.4 mmol) in 15 ml of acetonitrile. The reaction mixture was stirred for 150 h at 90 00 and subsequently cooled and filtered. The solid potassium salt was washed with ethyl acetate and the filtrate as well as the washing layers were combined and evaporated. The remainder was purified by column chromatography onsilica gel (cyclohexane I ethyl acetate 4: 1) to obtain 4-{4-[5-(2,6-difluoro-phenyl)-4,5- di hydro-isoxazol-3-yl]-th iazol-2-yl}-piperazine-1 ,2-d icarboxylic acid 1 -tert-butyl ester 2-methyl ester as a light yellow foam. M.p. 68 – 72 00 1H-NMR (400 MHz, 0D013): oe = 1.42 – 1.53 (m, 9H), 3.09 (dd, 1 H), 3.33 (dt, 2H), 3.52 (dd, 1 H), 3.69 (t, 1 H), 3.74 (s, 3H), 3.91- 4.08 (m,2H), 4.42 (dd, 1H), 4.70 -4.93 (m, 1H), 6.02 (t, 1H), 6.89 (t, 2H), 7.00 (s, 1H), 7.24- 7.31 (m, 1H). MS: mlz = 509 (M+1).

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference：
Patent; SYNGENTA PARTICIPATIONS AG; LAMBERTH, Clemens; SULZER-MOSSE, Sarah; CEDERBAUM, Fredrik; UMARYE, Jayant; SONAWANE, Ravindra; WO2013/127784; (2013); 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.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

112257-12-2, tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Commercially available imidazole (0.33 g, 4.9 mmol) was dissolved in 2 mL of freshly distilled DMF, under N2, and cooled to 0 C. Sodium hydride (0.14 g, 5.9 mmol) was added to the reaction and stirred for 30 min before a dropwise addition of tert-butyl 4-(2-bromoacetyl)piperazine-1-carboxylate (1.50 g, 4.9 mmol) dissolved in 2 mL of DMF. The mixture was slowly warmed to room temperature and stirred overnight. Addition of 10 mL of water caused a white precipitate to form. The solid was filtered and dried under reduced pressure overnight to afford tert-butyl 4-(2-(1H-imidazol-1-yl)acetyl)piperazine-1-carboxylate 8a (0.97 g,3.3 mmol, 67%); mp: 147-149 C. 1H NMR (400 MHz, CDCl3) delta 7.53(s, 1H), 7.11 (s, 1H), 6.96 (s,1H), 4.80 (s, 2H), 3.62 (bs, 2H), 3.48 (bs,6H), 1.47 (s, 9H); 13C NMR (100 MHz, CDCl3) delta 165.0, 154.5, 138.1, 129.7, 120.2, 80.8, 48.2, 45.1, 43.5, 42.2, 28.5; HRMS (ESI TOF): [M+H]+Calc’d for C14H23N4O3 m/z 295.1770. Found, m/z 295.1751.

112257-12-2, As the paragraph descriping shows that 112257-12-2 is playing an increasingly important role.

Reference：
Article; Abuteen, Akram; Zhou, Feifei; Dietz, Christopher; Mohammad, Innus; Smith, Michael B.; Zhu, Quing; Dyes and Pigments; vol. 126; (2016); p. 251 – 260;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics