Category: piperazines

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
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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;,
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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
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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;,
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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
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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;,
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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.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

A mixture of 4-((4-ethylpiperazin- 1 -yl)methyl)-3-(trifluoromethyl)aniline (Intermediate Cl)(500 g, 1.74 mmol) and methyl 3-hydroxybenzoate (Intermediate B2) (317 mg, 1.91 mmol)in anhydrous THF (5.0 mL) was cooled to -20 C and added potassium tert-butoxide (1M, 10 mL, 10.44 mmol). The mixture was stirred at RT for 3 h. The reaction mixture was cooled to-20 C and quenched with saturated sodium bicarbonate solution. The aqueous mixture was extracted twice with ethyl acetate and the combined organic layers were washed with waterfollowed by brine. The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated to yield 220 mg of the desired product. ?H NMR (400 MHz, DMSO-d6) oe 0.98 (t, J = 6.8 Hz, 3H), 2.31-2.50 (m, 8H), 2.51 (br s, 2H), 3.56 (s, 2H), 6.98-7.01 (br d, 1H), 7.3 1-7.35 (m, 2H), 7.39 (d, J = 6.4 Hz, 1H), 7.69 (d, J = 8.8 Hz, 1H), 8.03 (d, J = 8.4 Hz, 1H), 8.21 (s, 1H), 9.79 (s, 1H), 10.42 (s, 1H); ESI-MS (m/z) 408 (M+H).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); A1;,
Piperazine – Wikipedia
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694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

After taking the two 50mL round bottom flask was added sequentially aniline compound 5 (1.10mmol), NaNO2 (2.21mmol), ultrapure water (20 mL), the system was cooled to 0 deg.] C, was slowly added dropwise HCl (3.30mmol) in 5mL aqueous solution The After the addition, maintain the temperature of the reaction system continue to react 1.5h. It was then slowly added dropwise an aqueous solution of NaN3 (1.32mmol). After the addition was complete, maintainingThe reaction temperature of the reaction system, 3h, TLC monitored the reaction. After completion of the reaction, a saturated NaHCO3 solution was added 20mL, extracted with ethyl acetate 30mL ¡Á 2, combined organic phases were dried over anhydrous Na2SO4, and concentrated to give azide 6 directly administered next.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Tianjin International Bio-pharmaceutical Joint Institute; Rao Zihe; Bai Cuigai; Yang Cheng; Chen Yue; Li Huiying; Wang Lei; Gao Yuan; Yang Juan; Sun Tao; Zhong Chuanke; (26 pag.)CN106749278; (2017); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step B: tert-butyl(9aS)-3-hydroxy-3-( 1 -oxo-3.4-dihydro- 1H-isochromen-6- yl)hexahydropyrazino [2,1-c] [1,41 oxazine-8( 1H)-carboxylate: 6- (Bromoacetyl)-3 ,4-dihydro- 1H- isochromen-1-one (-.1.54 g, -.5.72 mmol, presence of cx-chloroketone was noted, -.10%) and commercially available (S)-4-N-BOC-2-hydroxymethylpiperazine (1.24 g, 5.72 mmol) were added to a round bottom flask and diluted with THF (50 mL). Diisopropylethylamine (1.30 mL,7.44 mmol) was then introduced and the mixture left stirring for 14 h at RT during which time a considerable amount of solid had formed. The reaction mixture was diluted with EtOAc, then washed with saturated NH4C1aq followed by H20. Both aqueous layers were sequentially back extracted once with another portion of EtOAc, the organics were then combined, dried with MgSO4, filtered, and concentrated in vacuo. The recovered crude product was subjected topurification by flash chromatography (Biotage, 50% EtOAc/Hex) to afford the title compound

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics