Heterocyclic Building Blocks-piperazine

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-ethylpiperazine (3.40g, 29.8mmol), 80 K2CO3 (4.10g, 29.6mmol), and 93 TBAI (0.42g, 1.2mmol) were added to a solution of 82 5-bromo-2-nitropyridine (4.00g, 19.7mmol) in 83 DMSO (40mL). The mixture was heated at 80C for 16h, and the reaction was poured into ice water, and extracted with DCM. The combined organic layers were washed with water, dried over anhydrous Na2SO4, concentrated under a vacuum, and purified by silica gel column chromatography (DCM/MeOH=100:1-10:1) to obtain 94 1-ethyl-4-(6-nitropyridin-3-yl)piperazine (3.59g; yield, 56%) as a yellow solid. Pd/C (0.10g) was added to the 1-ethyl-4-(6-nitropyridin-3-yl)piperazine (0.90g, 3.8mmol) in EA/MeOH (9 mL/9mL) solution. The mixture was degassed by H2, stirred at RT under a H2 atmosphere for 2h, and filtered and concentrated under a vacuum to obtain INT-2 (720.0mg; yield, 92%) as an off-white solid. ESI-MS: m/z 207.2 [M+H]+.

As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference£º
Article; Yin, Lei; Li, Heng; Liu, Wenjian; Yao, Zhenglin; Cheng, Zhenzhen; Zhang, Huabei; Zou, Hui; European Journal of Medicinal Chemistry; vol. 144; (2018); p. 1 – 28;,
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

General procedure: The mixture of compound 10a-10e (3.24 mmol), compound 9(1.04 g, 3.4 mmol), Pd(OAc)2 (0.11 g, 0.5 mmol), Xantphos (0.28 g,0.5 mmol), and K3PO41.38 g, 6.48 mmolin DMF (8 mL) was heated 22 h at 125 C under argon followed by cooling to roomtemperature.The mixture was extracted with dichloromethane(20 mL x 3), the combined organic phase was washed with water(15mL x 2), dried over anhydrous Na2SO4 and concentrated toafford the crude product. The crude product was purified by columnchromatography to obtain compounds 11a-11e.

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

Reference£º
Article; Su, Yue; Li, Ridong; Ning, Xianling; Lin, Zhiqiang; Zhao, Xuyang; Zhou, Juntuo; Liu, Jia; Jin, Yan; Yin, Yuxin; European Journal of Medicinal Chemistry; vol. 177; (2019); p. 32 – 46;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Method B: Oxalyl chloride (2 M in CH2Cl2) was added dropwiseto an ice-cooled solution of 2 in dry CH2Cl2 under an argon atmosphere. After 1 h, the ice-bath was removed and the reaction batch was stirred overnight at ambient temperature in an atmosphere of Ar. Subsequently the solvent was evaporated in vacuo and the crude acyl chloride was dissolved in dry DMF and added dropwise to a stirred suspension of amine and K2CO3 in dry DMF at 0 ¡ãC. The stirring was continued for 1 h and then at ambient temperature overnight. After 20 h the suspension was filtered, the solvent evaporated, the residue taken up in water and extracted with CH2Cl2. The organic layer was washed with 5percent aqueous NaHCO3 and brine.Then it was dried over anhydrous sodium sulfate, filtered and the solvent was evaporated in vacuo yielding the raw quinoline-4-carboxamides 9?11, which were further purified by column chromatography.

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Hochegger, Patrick; Faist, Johanna; Seebacher, Werner; Saf, Robert; Maeser, Pascal; Kaiser, Marcel; Weis, Robert; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2251 – 2259;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 119 Preparation of rac-6-chloro-3-(3-chloro-benzyl)-3-[4-(4-trifluoromethyl-phenyl)-piperazin-yl]-1,3-dihydro-indol-2-one The mixture of rac-3-bromo-6-chloro-3-(3-chloro-benzyl)-1,3-dihydro-indol-2-one (100 mg, 0.270 mmol), 1-(4-trifluoromethyl-phenyl)-piperazine (75 mg, 0.324 mmol) and DIPEA (42 mg, 0.324 mmol) In acetonitrile (3 mL) was stirred at room temperature for overnight. The crude was concentrated and the residue was purified with preparative HPLC to give 76 mg of rac-6-chloro-3-(3-chloro-benzyl)-3-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-1,3-dihydro-indol-2-one as a white solid. MS: 520 (M+H)+. H1-NMR (400 MHz, CDCl3) delta 7.584 (s, 1H), 7.493 (d, 2H), 7.240 (d, 1H), 7.081 (t, 2H), 7.011 (t, 1H), 6.908 (d, 3H), 6.766 (d, 1H), 6.684 (d, 1H), 3.431 (d, 1H), 3.329-3.206 (m, 5H), 2.947 (t, 4H).

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chen, Li; Yang, Song; Zhang, Jing; Zhang, Zhuming; US2008/81810; (2008); 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

To a solution of 4-methyl-2-piperazinone (26.16 mg, 0.23 mmol) in N,N-dimethylformamide (3mL) was added sodium hydride (18.34 mg, 60% purity, 0.46 mmol) at 0 C. The reaction was stirred for 20 minutes at 0 C. 2-[[8-Chloro-6-(chloromethyl)-7-fluoro-3-isoquinolyl]amino]-6-isopropyl-5,8-dihydro-4H-pyrazolo[1,5-d][1,4]diazepin-7-one (50 mg, 0.11 mmol) was added and stirred at 25 C. for 1 hour. The reaction was quenched with water, extracted with ethyl acetate, dried with anhydrous sodium sulfate. After filtration, the filtrate was concentrated under vacuum. The residue was purified by reverse phase chromatography ( acetonitrile 0-40/0.1% sodium bicarbonate in water) to afford 2-[[8-chloro-7-fluoro-6-[(4-methyl-2-oxo-piperazin-1-yl)methyl]-3-isoquinolyl]amino]-6-isopropyl-5,8-dihydro-4H-pyrazolo[1,5-d][1,4]diazepin-7-one (9 mg, 0.018 mmol) as a yellow solid. LCMS (ESI) [M+H]+=514.

As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference£º
Patent; Genentech, Inc.; Chan, Bryan; Drobnick, Joy; Gazzard, Lewis; Heffron, Timothy; Liang, Jun; Malhotra, Sushant; Mendonca, Rohan; Rajapaksa, Naomi; Stivala, Craig; Tellis, John; Wang, Weiru; Wei, BinQing; Zhou, Aihe; Cartwright, Matthew W.; Lainchbury, Michael; Gancia, Emanuela; Seward, Eileen; Madin, Andrew; Favor, David; Fong, Kin Chiu; Hu, Yonghan; Good, Andrew; US2018/282282; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Piperazin-1-yl-ethanol (8.2g, 63.1 mmol) was added to a solution of 4,6-dichloro-2- methylpyrimidine (5.2g, 31.9 mmol) in dichloromethane (80 ml) at rt. The mixture was stirred for two hours and triethylamine (0.9 ml) was added. The mixture was stirred at rt for 20h. The resultant solid was filtered. The cake was washed with dichloromethane (20 ml). The filtrate was concentrated to give an oil. This oil was dried under high vacuum for 20h to give a solid. This solid was stirred with heptane (50 ml) at rt for 5h. Filtration gave 7C (8.13g) as a white solid

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2005/77945; (2005); A2;,
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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

EXAMPLE 4 In a reaction vessel, a mixture of 11-piperazinyldibenzo[b,f][1,4]-thiazepine (10 Kg), 2-(2-chloroethoxy)ethanol (6.3 kg), 5.4 kg triethyl amine and 0.2 kg sodium iodide was heated under mixing to about 85 C. The reaction mixture was maintained at about 80 to 85 C. for about 3 hours. Starting 11-piperazinyldibenzo[b,f][1,4]-thiazepine was about 0.1% by HPLC. Maintained for another 2 hours till 11-piperazinyldibenzo[b,f][1,4]-thiazepine was about less than 0.05% by HPLC analysis. The reaction mass was cooled to about 30 C. and added 40 litres of water and aqueous layer extracted with methylene chloride. The organic layer was washed with water and concentrated under reduced pressure. The oily residue was so obtained suspended in 100 litres of ethanol (commercial) and 3.3 kg fumaric acid was added. The mixture was stirred for about 6 hours and cooled to about 15 C. The precipitated quetiapine hemi-fumarate salt was filtered and dried to give 12 Kg (yield 80% and purity 99.8% by HPLC analysis).

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

Reference£º
Patent; Kumar, Ashok; Singh, Dharmendra; Patil, Swapnali Hemant; Mahale, Ganesh Devidas; Sawant, Uttamrao Arjunrao; Jadhav, Balasaheb Ganpat; Rana, Ragneshkumar; US2007/293471; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (2 R,5R)-5-hydroxymethyl-2-methyl-piperazine- 1 -carboxylic acid tert-butyl ester (3.48 g, 15.1 mmol), benzaldehyde (1.76 g, 16.6 mmol), sodium triacetoxyborohydride (3.84 g, 18.1 mmol) and 1 ,2-dichloroethane (30 mL) was stirred at 20 c for 18 h, then partitionedbetween saturated aqueous NaHCO3 (150 mL) and DCM (3 x 50 mL). Combined organic extracts were dried (Na2SO4) then evaporated in vacuo to give an oil. Chromatography (Si02, 0 – 30% EtOAc in petrol) gave the title compound (4.588 g, 74%) as a colourless solid. MS: [M+H] = 321.

As the paragraph descriping shows that 1403898-64-5 is playing an increasingly important role.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; MILLEMAGGI, Alessia; HOWARD, Steven; SAXTY, Gordon; HEIGHTMAN, Thomas Daniel; WO2014/60768; (2014); 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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Example 19Synthesis of provide 4-(S-C6.7-dimethoxycinnolin-4-yl^pyridin-2-gammalVl methylpiperazin-2-one[00205] In a microwave vial was placed 4-(6-fluoropyridin-3-yl)-6,7- dimethoxycinnoline (0.0652 g, 0.229 mmol) in 2 ml DMSO. 1 -Methylpiperazin-2-one hydrochloride (0.3626 g, 2.29 mmol) and potassium carbonate (0.147 ml, 2.40 mmol) was added and the temperature was brought to 90 0C to stir overnight. The reaction solution was allowed to cool to room temperature. The solution was moved to a separatory funnel and deionized water and ethyl acetate were added. The aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with water, brine, dried with MgSO4, filtered, and concentrated. The crude product was adsorbed onto a plug of silica gel and chromatographed through a Biotage pre-packed silica gel column (25M), eluting with a gradient of 1% to 5% MeOH in CH2Ch, to provide 4-(5-(6,7-dimethoxycinnolin-4-yl)- pyridin-2-yl)-l -methylpiperazin-2-one (0.0413 g).

The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AMGEN INC.; MEMORY PHARMACEUTICALS CORPORTION; WO2007/98169; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 200 mL reaction flask, ethyl 2-(2-(4-fluoro-3-carboxyphenyl)acetyl)benzoate (Formula I, R=Et) (5 g, 15.14 mmol)And acetonitrile (100mL), after the addition is completed, the system is stirred until the system is dissolved.Additional 1-cyclopropyl-formylpiperazine (2.57 g, 16.67 mmol) and EDCI (3.50 g, 18.31 mmol) were added.Subsequently, DIPEA (2.40 g, 18.5 mmol) was added dropwise to the system, and the reaction temperature was controlled to be no higher than 35 C during the dropwise addition.After the addition was completed, the system was kept at 30 ¡À 5 C overnight. After the reaction is completed, the system removes the solvent under high vacuum.Ethyl acetate (150 mL) and H 2O (150 mL) were directly added to the residue, and the mixture was stirred, and the organic phase was separated.The aqueous phase was extracted twice with ethyl acetate (2¡Á100 mL), and the organic phase was combined.The residue was purified by column chromatography (ethyl acetate / n-heptane = 5 / 1-2 / 1) to give a pale yellow solid (formula IV, R = Et) (6.02g, 85.2%).

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

Reference£º
Patent; Jiangsu Jun Ruo Pharmaceutical Co., Ltd.; Haimen Baikang Bio-pharmaceutical Co., Ltd.; Nanjing Jun Ruo Bio-pharmaceutical Institute Co., Ltd.; Wei Wanguo; Xu Zichen; Fang Xianjie; Zhu Xinlei; Liu Rufeng; Yi Mingyue; Zhou Chenglong; Liu Jie; Song Yaojie; (7 pag.)CN110078671; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics