Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.928025-56-3,(S)-tert-Butyl 3-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,928025-56-3

To a solution of tert-butyl (S)-3-ethylpiperazine-1-carboxylate (150 mg, 0.700 mmol) and 4,4′-(chloromethylene)bis(fluorobenzene) (0.131 mL, 0.700 mmol) in acetonitrile (2 mL) was added DIPEA (0.244 mL, 1.400 mmol). The reaction mixture was heated to 80 C for 2 h. and diluted with water. The mixture was extracted twice with ethyl acetate (20 mL). The organic layer was separated, dried over Na2SO4 and evaporated to dryness. The crude was purified by ISCO (Column: 24 g RediSep silica, Solvent run: 0-50 % EtOAc in petroleum ether). The product was eluted at 30 % EtOAc in petroleum ether to afford tert-butyl (S)-4-(bis(4-fluorophenyl)methyl)-3- ethylpiperazine-1-carboxylate (50 mg, 8.8 % yield); LCMS: m/z = 417.4 (M+H); rt 2.39 min. Method: AQUITY UPLC BEH C18 (3.0 x 50 mm) 1.7 ^m, Mobile phase A:10 mM ammonium acetate:acetonitrile (95:5) Mobile phase B: 10 mM ammonium (1077) acetate:acetonitrile (5:95), Flow: 0.7 mL/min

The synthetic route of 928025-56-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); 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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Step B: 3-(6,8-dimethylimidazo[1,2-a]pyrazin-2-yl)-7-fluoro-2H-chromen-2-one hydrobromide (100 mg, 0.25 mmol) was stirred with (R)-2-methylpiperazine (52 mg, 0.52 mmol) in DMSO (0.5 mL) with K2CO3 (0.14 g, 1.0 mmol) at 120¡ã C. for 2 h. The mixture was cooled to room temperature and diluted with water to produce a precipitate. The solid was collected by vacuum filtration and purified by silica gel chromatography (10percent MeOH in CH2Cl2) to give the title compound (64 mg, 64percent) as a yellow solid. MS m/z 390.2 [M+H]+; 1H NMR (500 MHz, CDCl3): delta 8.74 (1H, s), 8.45 (1H, s), 7.77 (1H, s), 7.51 (1H, d, J=8.8 Hz), 6.88 (1H, dd, J=8.8 Hz, 2.5 Hz), 6.77 (1H, d, J=2.5 Hz), 3.77-3.67 (2H, m), 3.21-3.14 (2H, m), 3.06-2.92 (3H, m), 2.91 (3H, s), 2.64-2.56 (1H, m), 2.48 (3H, s), 1.20 (3H, d, J=6.3 Hz)., 75336-86-6

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PTC Therapeutics, Inc.; F. Hoffmann-La Roche AG; Woll, Matthew G.; Chen, Guangming; Choi, Soongyu; Dakka, Amal; Huang, Song; Karp, Gary Mitchell; Lee, Chang-Sun; Li, Chunshi; Narasimhan, Jana; Naryshkin, Nikolai; Paushkin, Sergey; Qi, Hongyan; Turpoff, Anthony A.; Weetall, Marla L.; Welch, Ellen; Yang, Tianle; Zhang, Nanjing; Zhang, Xiaoyan; Zhao, Xin; Pinard, Emmanuel; Ratni, Hasane; (317 pag.)US9617268; (2017); B2;,
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.112984-60-8,6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1 ,3]-thiazeto-[3,2-a]- quinoline-3-carboxylic acid of formula IV (100 gms, 0.286 moles) in 4.0 It of acetonitrile, DIPEA (70 ml , 0.402 moles)) was added at room temperature, stirred for 10 minutes. The reaction mass was cooled to 10-15C and a solution of 4-(bromomethyl)-5-methyl- 1 ,3-dioxol-2-one (formula V) in 500 ml of acetonitrile was slowly added at 10-15C over a period of 1 hour. The contents were stirred at 25-30C for 20 hour, filtered over hyflo, and the bed washed with 200 ml of acetonitrile. The solvent was distilled off completely under vacuum below 50C. Acetonitrile (100 ml) was added at 50C and the contents were stirred for 30-60 minutes. The reaction mass was slowly chilled to 0-5C and the precipitated solid was filtered, washed with acetonitrile (25 ml) and dried to yield 65 gms of prulifloxacin.

112984-60-8, The synthetic route of 112984-60-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CIPLA LIMITED; PATHI, Srinivas Laxminarayan; RAO, Dharmaraj Ramachandra; KANKAN, Rajendra; CHINIMILLI, Venugopalarao; CURTIS, Philip Anthony; WO2012/1357; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2-((1 H-pyrrolo[2,3 -b]pyridin-5 -yl)oxy)-4-(4-((4?-chloro-S,S- dimethyl-3 ,4,5 ,6-tetrahydro- [1,1 ?-biphenyl] -2-yl)methyl)piperazin-1 -yl)benzoic acid (1-1 b) (0.010 g, 0.02 mmol), (S)-2-(morpholinomethyl)-7-nitroindoline-5 -sulfonamide (1-la) (6.7 mg, 0.02 mmol), EDCT (0.011 g, 0.06 mmol), Et3N (6.0 mg, 0.06 mmol) and DMAP (8.0 mg, 0.06 mmol) in DCM (4 mL) was stirred at 30C for 20 h. The mixture was extracted by DCM (25 mL), washed with brine (15 mL), dried with Na2SO4 and concentrated. The residue was purified by preparative TLC eluting with DCM / MeOH (15:1) to give the title compound (S)-2-((1H-pyrrolo[2,3 -b]pyridin-5 -yl)oxy)-4-(4-((4?-chloro-5,5-dimethyl-3 ,4,5,6-tetrahydro-[1 , 1?-biphenyl] -2-yl)methyl)piperazin- 1 -yl)-N-((2-(morpholinomethyl)-7-nitroindolin-5 -yl)sulfonyl)b enzamide (1-1). MS-ESI (m/z): 895 [M+ 1]., 1235865-77-6

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SHANGHAI FOCHON PHARMACEUTICAL CO., LTD.; FOCHON PHARMACEUTICALS, LTD.; LIU, Hongbin; RONG, Yue; ZHANG, Huajie; CHEN, Zhifang; TAN, Rui; HE, Chengxi; LI, Zhifu; ZHOU, Zuwen; TAN, Haohan; RAN, Kai; WANG, Xianlong; ZOU, Zongyao; JIANG, Lihua; LIU, Yanxin; ZHAO, Xingdong; WANG, Weibo; (173 pag.)WO2018/192462; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55112-42-0, 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55112-42-0, EXAMPLE 107: 4-(4-(l,3-BenzothiazoI-6-ylamino)-7fl-pyrrolo[2,3-rf|-pyrimidin-6-yl)methylpiperazinyI-3,6-dihydropyridine-l(2fl)-yI)-carboxamide.; [342] To a suspension of benzothiazol-6-yl-[6-(l ,2,3,6-tetrahydropyridin-4-yl)-7^-pyrrolo[2,3-J]pyrimidin-4-yl]-amine tris-hydrochloride (200mg, 0.44mmol) in NJJ-dimethylformamide (6mL) was added AfAf-diisopropylethylamine (O.SmL, 3mmol). Thereaction mixture was stirred at 0C for 5min prior to the addition of 4-methylpiperazine-l-carbonyl chloride hydrochloride (87mg, 0.44mmol). The resulting mixture was stirred at 0Cfor Ih, diluted with water (50mL), and the resulting precipitate was collected by filtration,washed with EtOAc (5mL), and dried in vacua to give the title compound. LC-MS (ES,Pos.): 474 [MH+], and ‘H NMR (DMSO-d6, 400 MHz): 5 = 1.99 (s, 3H), 2.24 (m, 4H), 2.50(m, 2H), 3.18 (m, 4H), 3.41 (m, 2H), 3.93 (m, 2H), 6.41 (s, IH), 6.82 (s, IH), 7.87 (d, J= 8.8Hz, IH), 8.04 (d, J= 8.8 Hz, IH), 8.34 (s, IH), 8.91 (s, IH), 9.23 (s, IH), 9.59 (s, IH), 11.99(s, IH).

The synthetic route of 55112-42-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; OSI PHARMACEUTICALS, INC.; WO2006/17443; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

655225-01-7, tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

655225-01-7, A mixture of 4-bromo-6-hydroxypyrazolo[l,5-a]pyridine-3-carbonitrile (Intermediate PI, 200 mg, 0.840 mmol) in DMA (4.20 mL) was treated sequentially with K2CCb(s) (348 mg, 12.1 mmol) and tert-butyl 4-(2-bromoethyl)piperazine-l -carboxylate (493 mg, 1.68 mmol), then stirred for 3 h at 60 ¡ãC. After cooling to ambient temperature, the mixture was diluted with brine. The resulting suspension was filtered, and the solids were rinsed with water (5x). The solids the were collected, dissolved in DCM and concentrated in vacuo to cleanly afford the title compound (239 mg, 63percent yield). MS (apci) m/z = 452.0 (M+H).

655225-01-7 tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate 15946441, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ANDREWS, Steven W.; ARONOW, Sean; BLAKE, James F.; BRANDHUBER, Barbara J.; COLLIER, James; COOK, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; MCFADDIN, Elizabeth A.; MCKENNEY, Megan L.; MCNULTY, Oren T.; METCALF, Andrew T.; MORENO, David A.; RAMANN, Ginelle A.; TANG, Tony P.; REN, Li; WALLS, Shane M.; (946 pag.)WO2018/71454; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: Cool in ice a solution of the product of Preparation 13, Step 3 (1.50 g, 5.1 mmol) in THF (40 ml). Add DIPEA (1.08 ml, 6.2 mmol), then 2-chloroethyl chloroformate (0.76 g, 5.3 mmol). Stir 3 h and partition with ether and satd. NaHCO3. Dry (MgSO4) and concentrate to obtain the carbamate as a brown solid, 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Schering Corporation; US2004/220194; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,630125-91-6

To a solution of 2-chloro-4 6-dimethylpyrimidin-5-amine (50 mg 0.317 mmol) in THF (10 mL) was added triphosgene (33.0 mg 0.111 mmol) . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo to give 2-chloro-5-isocyanato-4 6-dimethylpyrimidine (50 mg 0.257 mmol 81yield) . To a solution of 4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) aniline (94 mg 0.327 mmol) and Et3N (0.114 mL 0.817 mmol) in THF (10 mL) was added a solution of 2-chloro-5-isocyanato-4 6-dimethylpyrimidine (50 mg 0.272 mmol) in THF (10 mL) . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo. The residue was dissolved in DCM (60 mL) and washed with H2O (20 mL) and brine (20 mL) . The organic layer was dried over Na2SO4 filtered and concentrated. The residue was purified by preparative HPLC (DCM/MeOH 10/1) to yield a white solid of 1- (2-chloro-4 6-dimethylpyrimidin-5-yl) -3- (4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) phenyl) urea (80 mg 0.167 mmol 61.2yield) 1HNMR(400 MHz CD3OD) delta 7.88 (s 1H) 7.39 (d J 8.0 Hz 1H) 6.99 (d J 2.8 Hz 1H) 3.75 (s 2H) 3.04 (m 8H) 2.49 (m 8H) 1.37 (m 3H) ES-LCMS m/z 471.0 (M+H)

630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R & D COMPANY LIMITED; CHEUNG, Mui; DEMARTINO, Michael P.; EIDAM, Hilary Schenck; GUAN, Huiping Amy; QIN, Donghui; WU, Chengde; GONG, Zhen; YANG, Haiying; YU, Haiyu; ZHANG, Zhiliu; (391 pag.)WO2016/37578; (2016); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

A solution of di-tert-butyldicarbonate (63 g, 290 mmol) in MeOH (100 mL) was added portionwise to a solution of piperazine-2-carboxyilic acid dihydrochloride (25.0 g, 123 mmol) and triethylamine (48 mL, 340 mmol) in MeOH (150 mL) over 30 minutes. Upon complete addition, the reaction mixture was heated to 50 0C for 2 h. Upon cooling to rt, the reaction mixture was concentrated under reduced pressure. The material was dissolved in water (300 mL) and the solution was brought to pH 2 with 1 M aqueous HCl. This was extracted with EtOAc (4 x 200 mL), and the combined extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure until -100 mL EtOAc remained. The solution was diluted with hexanes (150 mL) and cooled to 0 0C. The resulting solid was collected by filtration, washed with hexanes (2 x) and air- dried. This gave 38.9 g (96%) of the title compound as a white solid. Analytical data: 1H NMR (400 MHz, DMSO-J6) delta 13.02-12.80 (br, IH), 4.50-4.24 (m, 2H)5 3.94-3.72 (br, IH), 3.66 (d, J= 12.8 Hz, IH), 3.22-2.92 (m, 2H), 2.90-2.68 (brs IH), 1.42-1.34, (m, 18H)., 3022-15-9

3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); A2;,
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

After dissolving 1-(6-chloropyrimidin-4-yl)-N-(2, 6-dichloro-3,5-dimethoxyphenyl)- 1 H-benz[d]imidazol-2- amine (20 mg, 0.044 mmol) and 4-(4-ethylpiperazin-1-yl) aniline (13.6 mg, 0.066 mmol) in a mixture of 1,4-dioxane(0.1 mE) and dimethyl sulfoxide (0.1 mE) and cooling to 0 C., trifluoroacetic acid (10.2 pL, 0.133 mmol) was slowly added dropwise. Then, after heating to 120 C., the reaction mixture was stirred for 20 hours. Afier the reaction was terminated, the reaction mixture was cooled to room temperature. Afier extracting several times using ethyl acetate, the obtained organic layer was washed with water and a saturated sodium chloride solution, dried using sodium sulfate and then concentrated. The obtained residue was purified by colunm chromatography (dichloromethane/methanol, 20:1) to obtain a target compound (16 mg, 59% yield) as a yellow solid. ?H NMR (400 MHz, CDC13) oe 9.91 (brs, 1H), 8.62 (s, 1H), 7.49 (d, J=7.6 Hz, 1H), 7.28 H (m, 2H), 7.15 (t, J=7.6 Hz, 2H), 7.02 (t, J=8.0 Hz, 1H), 7.00 (d, J=8.8 Hz, 2H), 6.51 (s, 1H), 3.93 (s, 6H), 3.26 (t, J=4.6 Hz, 4H), 2.64 (t, J=4.4 Hz, 4H), 2.36 (q, J=7.2 Hz, 2H), 1.15 (t, J=7.2 Hz, 3H). ?3C NMR (400 MHz, CDC13) oe 163.49, 158.07, 156.36, 154.72, 150.63, 149.39, 142.67,135.44,131.39,129.12,124.81,123.28,120.86,117.78, 116.76, 112.85,110.17,95.25,92.88,56.47,52.64,52.30,49.03, 11.85. MSmIz: 620 [M+1].

115619-01-7, 115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY; SIM, Tae Bo; YOON, Ho Jong; YOON, Ji Hye; HUR, Woo Young; ROH, Eun Joo; KWAK, Yeon Ui; (19 pag.)US2016/145240; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics