Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

A solution of methyl (Z)-3-(chloro(4-ethylphenyl)methylene)-2-oxoindoline-5-carboxylate (100 mg, 0.29 mmol), N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (88 mg, 0.34 mmol) and TEA (0.08 mL, 0.59 mmol) in EtOH (1.0 mL) was stirred under refluxed for overnight. The reaction solvent was evaporated under reduced pressure, and the residue was purified by column chromatography with dichloromethane/ethanol (50/1, v/v) to obtain the final compound 95 as a yellow solid (166 mg, quant. yield): 1H NMR (500 MHz, DMSO-d6) _ 11.95 (s, 1H), 11.13 (s, 1H), 7.58 (dd, J = 8.2, 1.7 Hz, 1H), 7.42 – 7.38 (m, 5H), 7.13 (d, J = 8.2 Hz, 2H), 6.93 (d, J = 8.2 Hz, 1H), 6.89 (d, J = 8.2 Hz, 2H), 6.51 (s, 1H), 3.62 (s, 3H), 3.05 (bs, 2H), 2.72 (q, J = 7.6 Hz, 2H), 2.68 (bs, 2H), 2.18 (bs, 2H), 2.10 (s, 3H), 1.27 (t, J = 7.6 Hz, 3H); 13C NMR (125 MHz, DMSO-d6) _ 170.4, 168.6, 166.4, 157.3, 146.4, 140.4, 139.8, 137.5, 129.5, 128.9, 128.5, 127.7, 125.6, 124.0, 123.6, 121.3, 119.5, 108.9, 97.5, 59.2, 54.6, 52.4, 51.5, 45.8, 36.7, 28.3, 15.8; HRMS (ESI-TOF) m/z calcd for C31H32N6O6 [M + H+] 567.2846 found 568.2941., 262368-30-9

262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; DALBY, Kevin N.; EDUPUGANTI, Ramakrishna; TALIAFERRO, Juliana; LEE, Juhyeon; (0 pag.)WO2018/160967; (2018); 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

General procedure: Substituted amine (1.2 equiv) was added to a mixture of 4-fluoronitrobenzene (1 equiv) and K2CO3 (2.0 equiv) in DMF (7mL/g). The reaction mixture was stirred at 40C and followed by TLC. After completion of the reaction, the mixture was poured into stirring ice-water. The resulting precipitate was filtered and dried to obtain compounds 11 as a yellow solid.

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

Reference£º
Article; Hou, Yunlei; Zhu, Liangyu; Li, Zhiwei; Shen, Qi; Xu, Qiaoling; Li, Wei; Liu, Yajing; Gong, Ping; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 690 – 709;,
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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: Compound 6 (1mmol) was dissolved in freshly distilled dichloromethane (5mL) under nitrogen atmosphere. Then HOBt (1.1mmol), EDC,HCl (1.1mmol) were added to it. The reaction mixture was stirred for 5min, secondary amine 7a-l (1.2mmol) was added in a slow stream and followed by the addition of triethylamine (2mmol) and the reaction mixture was stirred for 24hat room temperature. The progress of the reaction was monitored by TLC. After completion of the reaction, water (10mL) was added to the reaction mixture and extracted with dichloromethane. Organic layer was collected and dried over anhydrous Na2SO4. After filtration, the solvent was removed under reduced pressure and the crude product was purified by silica gel chromatography using an eluent of 50% ethyl acetate in hexane., 30459-17-7

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

Reference£º
Article; Banu, Saleha; Bollu, Rajitha; Bantu, Rajashaker; Nagarapu, Lingaiah; Polepalli, Sowjanya; Jain, Nishant; Vangala, Radhika; Manga, Vijjulatha; European Journal of Medicinal Chemistry; vol. 125; (2017); p. 400 – 410;,
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

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (0.6g, 1.28mmol), 1-Boc-3- methyl piperazine (376mg,1.54mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide salts Salt (368mg, 1.92mmol) and N- hydroxy-7-aza-benzotriazole (435mg, 3.20mmol) was dissolved in dichloromethane (20mL) The conditions at 0 C tothis solution was added dropwise N, N- diisopropylethylamine (0.89mL, 5.12mmol), stirred at rt for 6h,Saturated chlorinated Sodium solution (15mL ¡Á 3) washing the organic phase dried over Na 2 SO 4 anhydrous,solvent was removed concentrate was subjected to column chromatography (eluent: Petroleumether / EtOAc (v/ v) = 4/1), to give 714mg white solid, yield: 80%.

129799-08-2, 129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference£º
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

1072027-36-1, 4-(4-Boc-1-piperazinyl)-5-bromo-7H-pyrrolo[2,3-d]pyrimidine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

INTERMEDIATE: (S)-tert-butyl-4-(5-(3-fluoropyrrolidin-l-yl)-7H-pyrrolor2,3- dlpyrimidin-4-yl) piperazine- 1 -carboxylate.Chemical Formula C19H27FN6O2 Exact Mass 390 22 1H-NMR (DMSO-d6/300 MHz): 11.44 (s, IH), 7.97 (d, J= 1.9 Hz, IH), 5.60 (d, J= 69 Hz, IH), 5.32 (s, IH), 3.66 (m, 4H), 3.36 (m, 10H), 1.38 (s, 9H). MS (ES+, m/z): 391.2 (M++., 100.0).

1072027-36-1, 1072027-36-1 4-(4-Boc-1-piperazinyl)-5-bromo-7H-pyrrolo[2,3-d]pyrimidine 58497312, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SUPERGEN, INC.; WO2008/128072; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1-CYCLOPROPYL-6, 7-difluoro-1, 4-DIHYDRO-8-METHOXY-4-OXO-3- quinoline carboxylic acid (100G), 2-methylpiperazine (67.8gs) and anhydrous DMSO (300 ml) were stirred for 40-45 hrs at 60-65C. The reaction mass was then diluted with 1500 ml isopropyl alcohol. It was then stirred for 30 min at 25-30C followed by cooling at 5 to 10 C along with stirring for 2 hours. The product was obtained by filtration, which was washed with 3 x 50 ml isopropyl alcohol followed by drying at 50 to 55C for 4 hours to provide 71 g Gatifloxacin (Yield 55. 9%) Example 2: Step A: A mixture of L-CYCLOPROPYL-6, 7-difluoro-1, 4-dihydro-8-methoxy-4-oxo-3- quinoline carboxylic acid (120Kg) 2-methylpiperazine (40.8 Kg), and anhydrous DMSO (361 lit) was heated to 60-65C temperature and stirred for 2 hrs. A second lot of 2-methylpiperazine (10.2 Kg) was added, and stirred for next 1 hr, at 60-65C. followed by the addition of a third lot of 2-methylpiperazine (10.2Kg). The mixture was stirred for next 2 hrs at 60-65C. A fourth lot of 2-methylpiperazine (20.4Kg) was added to the mixture and the stirring was continued for the next 24 hrs maintaining the temperature at 60-65C followed by cooling to 25-35C. This reaction mass was added in 1802-1 isopropyl alcohol. Reaction mass was then stirred for 30 min at 25- 30C followed by cooling at 5 to 10 C along with stirring for 2 hours. Product so obtained was centrifuged, washed with 3 x 60-1 isopropyl alcohol. The wet cake of PRODUCT WAS MIXED WITH 241-LIT METHANOL AND STIRRED FOR 1 HR. , AGAIN THE PRODUCT WAS centrifuged followed by washing with 59 lit of methanol. The wet Gatifloxacin was dried at 60 to 65C for 6 hrs to yield 81. 92 Kg dry Gatifloxacin (Yield= 53.7%) HPLC Purity = 99.74% M/C=3. 42%, 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CADILA HEALTHCARE LIMITED; WO2004/101527; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,934-98-5

General procedure: To the suspension of sodium hydride (60percent, 0.23 g, 5.66 mmol) in dried dimethyl formamide (15 mL) was added 6-bromo (or 7-bromo)-[1,2,4]triazolo[1,5-a]pyridin-2-amine (0.60 g, 2.82 mmol),stirred for 10 min at room temperature, added N,N’-carbonyldimidazole(CDI, 1.37 g, 8.46 mmol), stirred at 60 ¡ãC until the starting material consumed, then added amine (9.87 mmol) and stirred at 60 ¡ãC for 6 h. The volatile was removed under reduced pressure to give a white pale yellow residue. Water (30 mL) was added tothe residue. The mixture was stirred. The precipitate was collected by filtration, dried to afford the expected product as a white solid. 5.1.1.7 1-(6-Bromo-[1,2,4]triazolo[1,5-a]pyridin-2-yl)-3-(2-(4-methylpiperazin-1-yl)ethyl)urea (2g) White solid; yield: 81.0percent; mp: 182-184 ¡ãC; 1H NMR (CDCl3): delta 9.60 (s, 1H, NH), 8.80 (s, 1H, Ar-H), 8.46 (s, 1H, NH), 7.63 (m, 2H, Ar-H), 2.60 (m, 10H, CH2 * 5), 2.36 (s, 3H, CH3). MS m/z (ESI): 382.1 [M+H]+.

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference£º
Article; Wang, Xiao-Meng; Mao, Shuai; Cao, Lei; Xie, Xiao-Xiao; Xin, Min-Hang; Lian, Jia-Fang; Cao, Yong-Xiao; Zhang, San-Qi; Bioorganic and Medicinal Chemistry; vol. 23; 17; (2015); p. 5662 – 5671;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

To a 10 ml RBF containing a magnetic stir bar was added 2-(4- Methylpiperazine-l-yl)ethanamine (143 mg, 1 mmol) in DCM (1 ml). Let stir under argon at room temperature. 1 , 1′-Carbonyldiimidazole (207 mg, 0.5 mmol) was added to the above solution using a spatula. Started forming a white precipitate. TLC on Sipsi2 in 100percent MeOH against the imidazolde indicated a very polar product.Let the solution stir overnight under argon. TLC indicated the completion of the reaction. Extracted the mixture into 25 ml EtOAc. Washed with 2×20 ml of distilled water and 20 ml brine. Combined the desired fractions and dried over anhydrous MgSOphi Filtered and concentrated in vacuo. Dissolved in the minimumamount of EtOAc and reprecipitated from hexanes. Filtered the product as a colorless solid and dried under vacuum to obtain a 69percent yield.eta and 13C NMR in CDCl3 with 2 drops of MeOD. Sample was designated NTF-2006-1-006A1FfNMR (300 MHz, CDCl3) 0.78 (t, J= 7.5 Hz, 3H), 1.08 (m, J= 7.5 Hz, 2H),1.38 (m, J= 7.5 Hz,4H), 1.47 (br s, 4H), 2.27 (s, 3H), 2.47 (br t,4H),2.54 (br t, 4H), 2.60 (t, J=6 Hz, 3H), 3.08 (m, J= 9.0 Hz, 2H), 3.52 (m, J= 5.7 Hz, 2H), 6.89 (d, J= 9.0 Hz, 2H), 7.07 (t, J= 6.9 Hz, IH), 7.28 (t, J= 8.4 Hz, 2H), 7.45 ( br d,J=1.8 Hz, IH), 7.55 (br d, IH) EPO 13C NMR (75 MHz, CDCl3) 14.00, 20,16, 31.32, 36.84, 43.26, 43.36, 46.23,53.07, 55.21, 56.99, 112.96, 115.64, 124.05, 130.44, 132.81, 136.18, 142.79, 142.84, 156.20FABMS 490 (M+H)+ ;HRMS calcd for 024H36N5O4S+ 489.2410 ; found 490.2510

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; FLYNN, Gary, A.; YOOL, Andrea, J.; MIGLIATI, Elton, Rodrigues; RITTER, Leslie, S.; WO2008/52190; (2008); 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.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

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£º
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Step 1: CbzCl (17 g, 0.1 mol) was added into a solution of compound 219-1 (30 g, 0.3 mol) and DIPEA (40 g, 0.3 mol) in DCM (200 mL) at 0C, then the mixture was stirred at room temperature for 3h and the solvent was removed, the crude product was purified by column chromatography to deliver compound 2 (11 g, yield 47%) as yellow oil. MS ESI calcd for C13H18N2O2 [M+H]+ 235, found 235., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD; WU, Hao; LIN, Jun; LI, Yunhui; WEI, Changqing; CHEN, Shuhui; LONG, Chaofeng; CHEN, Xiaoxin; LIU, Zhuowei; CHEN, Lijuan; (212 pag.)EP3124482; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics