Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of (2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid 1 (0.17 g, 0.615 mmol) in dry DCM (10 mL) were added te/f-butyl 4-aminopiperazine-1-carboxylate 205 (0.19 g, 0.923 mmol), 1-hydroxybenzotriazole (0.125 g, 0.923 mmol), 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (0.177 g, 0.923 mmol) and 4- dimethylaminopyridine (0.113 g, 0.923 mmol) at room temperature. The reaction mixture was stirred at room temperature overnight, and then concentrated under vacuum. The residue was purified by column chromatography to give terf-butyl 4-({[(2S,5R)-6-(benzyloxy)-7-oxo- 1 ,6-diazabicyclo[3.2.1]oct-2-yl]carbonyl}amino)piperazine-1-carboxylate 206 (0.25 g, 88%) as a clear thick oil. 1H NMR (400 MHz, CDCl3): delta 1.46 (9H, s), 1.62 (1 H, m), 1.95 (2H, m), 2.38 (1 H, m), 2.70 (1 H, d, J = 12.0Hz), 2.76 (4H, m), 2.99(1H, d, J = 12.0 Hz), 3.30 (1 H, m), 3.57 (4H, m), 3.89 (1 H, d, J = 8.0 Hz), 4.90 (1H, d, J = 11.6 Hz), 5.04 (1 H, d, J = 12.0 Hz), 7.21 (5H, m), 8.90 (1 H, br s)., 118753-66-5

118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NAEJA PHARMACEUTICAL INC.; MAITI, Samarendra N.; NGUYEN, Dai; KHAN, Jehangir; LING, Rong; WO2014/91268; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

350684-49-0, tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of tert-butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate (2d, 1.7 g, 5.7 mmol, 1 equiv.), 3,5-dibromo-1-methylpyrazin-2(1H)-one (2e, 1.8 g, 6.8 mmol, 1.2 equiv.)and N,N-diisopropylethylamine (1.48 mL, 8.5 mmol, 1.5 equiv.) in N,N-dimethylacetamide (5 mL) was stirred in a sealed vial at 105 C for 30 h. The reaction was cooled to room temperature and EtOAc (20 mL) was then added. The solid precipitate was filtered and dried on high vacuum overnight to provide tert-butyl 4-(4-((6-bromo-4-methyl-3-oxo-3 ,4- dihydropyrazin-2-yl)amino)benzoyl)piperazine- 1 -carboxylate 2f. The product was carriedonto the next step without further purification., 350684-49-0

350684-49-0 tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate 2763355, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; DOBROVOLSKY, Dennis; HUANG, Hai-Tsang; (152 pag.)WO2018/98275; (2018); 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.1284243-44-2,tert-Butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To the solution of tert-butyl 4-(4-fluorophenyl)-3-oxopiperazine- 1-carboxylate (2g, 6.80 mmol) in dichloromethane (5 ml) was added slowly hydrogenchloride in1,4-dioxane (16.99 ml, 68.0 mmol) at 0°C and reaction was stirred for 3 h at 25°C. After completion of the reaction, the solvent was evaporated under reduced pressure to obtained salt was triturated with diethyl ether (2 x 10 ml) decanted it and dried to give 1-(4-fluorophenyl)piperazin-2-one hydrochloride (1.2 g, 5.20mmol, 77 percent)?H NMR (400 MHz, DMSO-d6) 6 9.90 (bs, 1H, D20 exchangeable), 7.38-7.34 (m, 4H), 3.85-3.72 (m, 4H), 3. 55-3.50 (m, 2H).MS: m/z 195 (M+1).

1284243-44-2, 1284243-44-2 tert-Butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate 67085032, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; LUPIN LIMITED; JANA, Gourhari; KURHADE, Sanjay, Pralhad; JAGDALE, Arun, Rangnath; KUKREJA, Gagan; SINHA, Neelima; PALLE, Venkata, P.; KAMBOJ, Rajender, Kumar; WO2014/9872; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N-acetyl-N-(2-(trifluoromethyl)phenyl)acetamide (13.28 g, 52.54 mmol) was added to 2R,6S-2,6-dimethylpiperazine (5 g, 43.79 mmol) in EtOH (75 mL) and the mixture was stirred at ambient temperature for 24 hours. This was then evaporated to dryness, redissolved in DCM (25 mL) and washed with 2M aqueous HC1 (25 mL). The aqueous solution was then basified to pH 14 with concentrated aqueous NaOH and extracted with DCM (2 x 25 mL). The combined organics were evaporated to dryness to give a yellow liquid. This was purified by flash silica chromatography, elution gradient 0 to 10 percent 7M NH3/MeOH in DCM. Pure fractions were evaporated to dryness to afford 1-((3S,5R)-3,5-dimethylpiperazin-1-yl)ethanone (4.00 g, 66.7 percent) as a pale tan oil. 1H NMR (400 MHz, DMSO, 100 °C) 0.98 (6H, d), 1.78 (1H, br s), 1.96 (3H, s), 2.26 (2H, br s), 2.58 – 2.68 (2H, m), 3.94 (2H, br s).

21655-48-1, As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert Hugh; RABOW, Alfred Arthur; WARING, Michael James; MCCABE, James Francis; GLOSSOP, Steven Christopher; MAHMOOD, Arshed; COTTER, Zoe Ann; (88 pag.)WO2016/16618; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-34-8, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At room temperature, 3.5 g (10 mmol) of intermediate Ib was dissolved in 35 mL of 90% EtOH and heated to 70 C. 0.44 g (1.5 mmol) of FeCl · 6H2O and 0.038 g (3 mmol) of activated charcoal were added and stirred for 10 min. A solution of 6.73 g (100 mmol) of 80% hydrazine hydrate was added dropwise and heated to 90 C for 2 h. Reaction is completed, the hot filter, the solvent evaporated to dry the crude product, and then add 50mL of crude water, the platform stirring 0.5h, filter, filter cake with a small amount of water rinse, dry pale yellow solid 2.5g, yield 78.6 %, 154590-34-8

The synthetic route of 154590-34-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shenyang Red Flag Pharmaceutical Co., Ltd.; Li Juan; Yang Bo; Li Xingyuan; Zhang Tiejie; Sun Jukui; (19 pag.)CN107033095; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The 10 mmol of acid (6-8, 11a,b or 14) was dissolved in anhydrous acetonitryle (25 ml). The solution was cooled to -5 C, and triethylamine (1.4 ml, 10 mmol), and then HBTU (3.79 g, 10 mmol) or HATU (3.8 g, 10 mmol), were added. The mixture was stirred for 1 h at -5 C and then 10 mmol of amine 5 was added. The reaction mixture was allowed to stand overnight at room temperature. The residual amount of the activated ether (Bt- or At-ether of starting acid) was destroyed by addition of few drops of N,N-dimethylpropane-1,3-diamine, and the solvent was evaporated in vacuo to dryness. The residue was dissolved in 100 ml of chloroform. The solution was washed with water (40 mL), aqueous solution of 1 M HCl (40 ml) and 5% aqueous solution of NaHCO3 (40 ml). The organic layer was dried over Na2SO4, filtered off, and the solvent was evaporated in vacuo to dryness. The resulting residue was triturated with warm hexane (20 ml), and the precipitate was collected by filtration and dried., 162046-66-4

The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Krysko, Andrei A.; Samoylenko, Georgiy V.; Polishchuk, Pavel G.; Fonari, Marina S.; Kravtsov, Victor Ch.; Andronati, Sergei A.; Kabanova, Tatyana A.; Lipkowski, Janusz; Khristova, Tetiana M.; Kuz’Min, Victor E.; Kabanov, Vladimir M.; Krysko, Olga L.; Varnek, Alexandre A.; Bioorganic and Medicinal Chemistry; vol. 21; 15; (2013); p. 4646 – 4661;,
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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred solution of 135 1-fluoro-4-nitro-benzene (500 mg, 3.54 mmol) and 213 1-cyclopropylpiperazine (536 mg, 4.25 mmol) in 10 mL of 6 ethanol was added 27 DIPEA (913 mg, 7.08 mmol) and stirred at reflux for 12 h. After completion of reaction, solvent was removed under reduced pressure, diluted with water (20 mL) and extracted with CH2Cl2 (20 mL×3). Combined organic layer was washed with brine solution, dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford crude product which was washed with diethyl ether and dried to afford 214 1-cyclopropyl-4-(4-nitrophenyl)piperazine (450 mg). (0348) LCMS: 248 [M+1]+

20327-23-5, As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference：
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

6.01.33.01 2-Methyl-4-pyrimidin-2-yl-piperazine-1-carboxylic acid tert-butyl ester 100 mg 2-chloro-pyrimidine was added to 175 mg 2-Methyl-piperazine-1-carboxylic acid tert-butyl ester and this mixture was stirred for 2 h at 120 C. to give 240 mg of the desired compound. Rt: 1.31 min (method B), (M+H)+: 279 By using the same synthesis strategy as for 2-methyl-4-pyrimidin-2-yl-piperazine-1-carboxylic acid tert-butyl ester the following compound was obtained:, 120737-78-2

The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GRAUERT, Matthias; BISCHOFF, Daniel; DAHMANN, Georg; KUELZER, Raimund; RUDOLF, Klaus; WELLENZOHN, Bernd; US2013/150341; (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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

The 1-(2-hydroxyethyl)-4-methylpiperazine used as a starting material was prepared as follows: A mixture of 2-bromoethanol (2.36 g), N-methylpiperazine (1.26 g), potassium carbonate (5.0 g) and ethanol (150 ml) was stirred and heated to reflux for 18 hours. The mixture was cooled to ambient temperature and filtered. The filtrate was evaporated and the residue was triturated under a mixture of methylene chloride and acetone. The resultant mixture was filtered and the filtrate was evaporated to give the required starting material as an oil (0.87 g); NMR Spectrum: (CDCl3) 2.18 (s, 3H), 2.3-2.7 (br m, 81), 2.56 (t, 2H), 3.61 (t, 2H)., 109-01-3

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

Reference：
Patent; Hennequin, Laurent Francois Andre; Crawley, Graham Charles; McKerrecher, Darren; Ple, Patrick; Poyser, Jeffrey Philip; Lambert, Christine Marie Paul; US2003/225111; (2003); 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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

5317-33-9, A solution of diisopropyl azodicarboxylate (12.1 ml) in methylene chloride (50 ml) was added dropwise during 30 minutes to a stirred mixture of 4-chloro-3-cyano-7-hydroxy- 6-methoxyquinoline (12 g), 1-(3-hydroxypropyl)-4-methylpiperazine (9.7 g), triphenylphosphine (16.1 g) and methylene chloride (200 ml) that had been cooled to [5C.] The resultant mixture was allowed to warm to ambient temperature and was then stirred for 1 hour. Further portions of diisopropyl azodicarboxylate (1. [2 ML)] and triphenylphosphine (1.6 g) were added and the mixture was stirred at ambient temperature for a further 1 hour. The mixture was poured into water and the organic layer was separated, washed with a saturated brine solution, dried over magnesium sulphate and evaporated. The material so obtained was purified by column chromatography on silica using increasingly polar mixtures of methylene chloride and methanol as eluent. There was thus obtained the required starting material as a solid (14.5 g); NMR Spectrum : [(DMSOD6)] [1.] 95 (m, 2H), 2.13 (s, 3H), 2.24-2. 5 [(M, L OH),] 4.0 (s, 3H), 4.25 (t, 2H), 7.43 (s, [1H),] 7.51 (s, [1H),] 8.95 (s, [1H)] ; Mass Spectrum : M+H+ 375 and 377.

As the paragraph descriping shows that 5317-33-9 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/5284; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics