Month: September 2021

53788-49-1, tert-Butyl 4-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

53788-49-1, Deprotection: A solution of 1:1 TFA, DCM with 0.5% water was prepared. This solution was added to the material isolated from the reduction, above (10 mL/g starting material). The reaction was stirred for 30 minutes then the solvent was removed with a rotoevaporator. Solvent evaporation was terminated when no more solvent was observed to be collecting on the condenser. TFA was added to the product residue (2 mL/g starting material) to form a free flowing solution. The TFA solution was transferred to a centrifuge tube and diethyl ether was added to precipitate the product salt. The solution was mixed using a vortex. The solution was then centrifuged and the supernatant decanted to collect the precipitate. The filtrate was then washed 1 time with ether by resuspending the product, vortexing, and re-centrifugation. Product was dried under low vacuum to remove residual ether.

The synthetic route of 53788-49-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Applera Corporation.; US2005/148773; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

883554-88-9, 4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

883554-88-9, The compound 4-carbamoyl-piperazine-1-carboxylate (0.16g, 0.7mmol) was dissolved in dichloromethane(2mL) was added HCl The ethyl acetate solution (4M, 2mL), stirred at rt for 30min, the solvent was removed togive 0.16g of white solid: piperazin-1-carboxamide hydrochloride Salt, yield: 100%.

As the paragraph descriping shows that 883554-88-9 is playing an increasingly important role.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

EXAMPLE IX; Synthesis of Piperazine derivatives; Chemical Formula: C16H2iN3Oe Chemical Formula: C12H15N304 Molecular Weight: 130.15 Molecular Weight: 351.35 Molecular Weight: 265.27a: Boc-ON, NaOH, Dioxaneb: 2-flouronitrobenzene, K2C03, DMSOc: SOCI2, methanol, reflux, 2hrsd: Fmoc-NCS, CH2CI2/DMF; 20% piperidine in methanole: appropriate bromoacetophenonef: 1 N NaOH, Dioxane, reflux, 0.5hrs4-(feri-butoxycarbonyl)piperazine-2-carboxylic acid; [191] 4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid : To a solution of 2-piperazine- carboxylic acid dihydrochloride (1.0 g, 4.92 mmol) in 20 mL of water/dioxane 1 : 1, NaOH 6N was added to adjust the pH to 11. A solution of BOC-ON (1.34 g, 5.41 mmol) in dioxane (5 mL) was then added dropwise, while maintaining the pH=l 1 during the addition and the resulting solution was stirred overnight at room temperature. Another 0.134 g of BOC-ON were added and the reaction mixture was stirred for 2h. The solvent was evaporated under reduced pressure and the residue was diluted with diethyl ether/water (60 mL). The phases were separated and the pH of the aqueous layer was adjusted to 7 by slow addition of HC1 IN. Evaporation of water under reduced pressure afforded the title compound as a white solid which was dried in a vacuum oven at 50 C and used without further purification for the next step., 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; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; CHOREV, Michael; AKTAS, Bertal Huseyin; HALPERIN, Jose A.; WAGNER, Gerhard; WO2012/6068; (2012); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution OF RAC-3-METHYL-PIPERAZINE-L-CARBOXYLIC acid tert-butyl ester (350 mg, 1.75 mmol) in dimethylformamide (3 ml) were added 2-Iodo-5-methanesulfonyl-benzoic acid (540 mg, 1.67 mmol), N-ETHYLDIISOPROPYLAMINE (1. 8 ml, 10.5 mmol), and TBTU (630 mg, 1.92 mmol). The reaction mixture was then allowed to stir at room temperature for 16 hours. The reaction mixture was then concentrated in vacuo and the residue was purified by column chromatography (SI02, 20g, Heptane/EtOAc 0-100percent) to give the title compound (400 mg, 45 percent). MS (m/e): 526.2 (M+NH4+).

120737-59-9, As the paragraph descriping shows that 120737-59-9 is playing an increasingly important role.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; WO2005/23260; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 5 (0.10g, 0.48mmol), DIPEA (0.08ml, 0.48mmol) and EtOH (5ml) was mixed with the 85 (0.07g, 0.48mmol) and refluxed for 2.5hrs. The reaction was quenched by saturated NaHCO3 (aq.) and the mixture was extracted by ethyl acetate (30ml x 3). The residue was purified by flash column over silica gel (dichloromethane: methanol = 9: 1, Rf = 0.28) to afford 89 (0.05g, 33.24%) as a pale yellow solid. 1H-NMR (300MHz, CDCl3): delta 1.13 (t, J= 7.2 Hz, 3H), 2.46 (q, J= 7.2 Hz, 2H), 2.62 (t, J= 5.1 Hz, 4H), 2.98 (d, J= 5.1 Hz, 3H), 3.19 (t, J= 5.1 Hz, 4H), 5.17-5.29 (m, 1H), 5.55 (br, 1H), 6.91 (d, J= 8.7 Hz, 2H), 7.37 (d, J= 8.1 Hz, 1H), 7.46 (s, 1H), 8.20 (d, J= 44.7 Hz, 1H)., 115619-01-7

The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAIPEI MEDICAL UNIVERSITY; YEN, Yun; LIOU, Jing-Ping; CHEN, Chun-Han; (70 pag.)WO2017/15400; (2017); 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.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,548762-66-9

Half of the solid from the previous step was treated with N,N-diisopropylethylamine (0.5 mL, 3 mmol), DMSO (0.5 mL, 7 mmol) and (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (273 mg, 1.27 mmol) and the reaction mixture was heated at 120 C. overnight, concentrated by rotary evaporation, dissolved in a small amount of DCM and purified by silica gel chromatography (0-50% ethyl acetate:hexanes) to produce the title intermediate (288 mg, 29% yield) as a yellow solid. (m/z): [M+H]+ calcd for C24H27F4N4O4 591.09; 593.09. found 593.2.

548762-66-9 (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate 11745988, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; LONG, Daniel D.; MCKINNELL, Robert Murray; JIANG, Lan; LOO, Mandy; LEPACK, Kassandra; VAN ORDEN, Lori Jean; OGAWA, Gavin; HUANG, Xiaojun; ZHANG, Weijiang; US2013/115194; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

24860-46-6, 2-(2-Oxopiperazin-1-yl)acetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Palladium (0.161 g, 10% on carbon) was added to a mixture of 2-Oxo-1-piperazineacetic acid (0.497 g, 3.14 mmol) and (2-Oxo-ethyl)-carbamic acid tert-butyl ester (0.503 g, 3.16 mmol) in methanol (6.2 mL) under argon. The flask was evacuated and the reaction placed under a hydrogen atmosphere for 22 h. The reaction was filtered through a Celite -plugged filter frit, washed with methanol and DCM, and concentrated in vacuo to afford crude product which was carried to the next step without purification. ESI-MS m/z 324 (M+Na)+., 24860-46-6

24860-46-6 2-(2-Oxopiperazin-1-yl)acetic acid 23422809, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; VENATORX PHARMACEUTICALS, INC.; BURNS, Christopher, J.; DAIGLE, Denis; LIU, Bin; MCGARRY, Daniel; PEVEAR, Daniel, C.; TROUT, Robert, E. Lee; WO2014/151958; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

68104-63-2, 4-(Piperazin-1-yl)benzonitrile is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

68104-63-2, To a solution of 6.1 mmol 2-iodo-5-methanesulfonyl-benzoic acid in 20 ml dimethyl formamide were added successively 6.75 mmol TBTU, 43 mmol N-ethyldiisopropylamine and 6.75 mmol 4-piperazin-1-yl-benzonitrile (commercially available, e.g. from Fluka). The reaction mixture was stirred at 20 C. for 1.5 h and then concentrated in vacuo. Addition of 200 ml water followed by filtration yielded the crude product which was recrystallized from methanol to afford the title compound as a white solid (yield 87%). MS (m/e): 495.9 (M+H+, 100%).

The synthetic route of 68104-63-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Jolidon, Synese; Narquizian, Robert; Norcross, Roger David; Pinard, Emmanuel; US2006/149062; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of crude ethyl 6-tert-butyl-l0-methoxy-2-oxo-9-[2-[2-[2-(p- tolylsulfonyloxy)ethoxy]ethoxy]ethoxy]-6,7-drhydrobenzo[a]quinolizine-3-carboxylate (0382) (compound 10b, 65.8 mg, 0.1 mmol) , l-tert-butyl 3-methyl piperazine- l,3-dicarboxylate (29 mg, 0.12 mmol), potassium carbonate (28 mg, 0.2 mmol) and sodium iodide (15 mg, 0.1 mmol) in acetonitrile (1 mL) was heated at 90 C for 20 h. After cooling to room temperature, the reaction mixture was partitioned between CH2CI2 and water, and then extracted with CH2CI2 for three times. The combined organic layer was washed with brine, dried and concentrated to give crude O l-tert-butyl 03-methyl 4-[2-[2-[2-[(6-tert-butyl-3-ethoxycarbonyl-l0-methoxy-2-oxo-6,7- dihydrobenzo [a] quino lizin-9-yl)oxy] ethoxy] ethoxy] ethyl]piperazine- 1 ,3 -dicarboxylate (0383) (compound 11a, 85 mg) as a brown oil, which was directly used for next step without further purification. MS obsd. (ESI+) [(M+H)+]: 730.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HAN, Xingchun; JIANG, Min; WANG, Yongguang; YANG, Song; (83 pag.)WO2019/129681; (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.112257-12-2,tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

4-(2-Oxo-2-piperazin-1-ylethyl)morpholine (42-2) Morpholine (0.22 g, 2.59 mmol), 42-1 (0.61 g, 1.99 mmol) and DIEA (0.33 g, 2.59 mmol) were dissolved in DMF (2 mL) and stirred for 18 hours at room temperature. The DMF was then removed under reduced pressure and the residue partitioned between water and methylene chloride. The methylene chloride was drawn off, dried and evaporated to a solid to afford 42-2. This recovered product was treated with neat trifluoroacetic acid and the excess trifluoroacetic acid evaporated off. The resulting residue was partitioned between methylene chloride and aqueous Na2CO3. The free base did not extract from the aqueous so the aqueous was evaporated to dryness, washed the methanol, and the solids filtered off to afford 42-2. 1H-NMR(CD3O): 3.69(t, 4H); 3.59 (t, 2H); 3.54(t, 2H); 3.22(s, 2H); 2.83(t, 2H); 2.77(t, 2H); 2.49(t, 4H).

112257-12-2, 112257-12-2 tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate 15829155, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Bilodeau, Mark T.; Hartman, George D.; Hoffman JR., Jacob M.; Sisko, John T.; Manley, Peter J.; Smith, Anthony M.; Tucker, Thomas J.; Lumma JR., William C.; Rodman, Leonard; US2002/137755; (2002); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics