Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

Example 5: . 2-(lH-IndoI-4-yI)-6-(4-inethanesuIfonvI-piperazin-l-vImethvI)-4- morphoIm-4-yI-thienor2,3-d1pyrimidine; 2-Chloro-6-(4-methyl-piperazm-l-ylmethyl)-4-morpholin-4-yl-thieno[2,3- dlpyrimidine ‘ 2-Chloro-4-morpholin-4-yl-thieno[2,3-d]pyrimidine-6-carbaldehyde (400 mg) and 1-methanesulfonyl-piperazine hydrochloride (1.3eq.) were stirred together in dry 1,2-dichloroethane (20 mL). After 4h sodium triacetoxyborohydride (2.3 eq.) was added and the mixture stirred overnight. The mixture was diluted with Na2CO3 solution then extracted with ethyl acetate. Combined extracts were dried (Na2SO4), filtered and concentrated. Trituration gave product (60%)., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PIRAMED LIMITED; WO2007/122410; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

791846-40-7, tert-Butyl 4-(4-bromo-2-cyanophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,791846-40-7

To a solution of 1-16 (2.5 g, 6.83 mmcl) in DMSO (6 mL) were added aqueous 30% H202 (0.15 ml, 8.88 mmcl) and K2003 at 0CC, and the reaction mixture was stirred at room temperature for 16 hours. After completion of the reaction, the reactionmixture was poured into ice cold water (100 ml) and extracted with diethyl ether (100 mL x 3) . The organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude product so obtained was purified by silica gel column chromatography (60-120 mesh) using 30% EtOAc in hexanesas eluent to give the desired product 1-17 (1.3 g, 50%) as a white solid; LOMS: m/z 384.0 [M+1]

As the paragraph descriping shows that 791846-40-7 is playing an increasingly important role.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; KOUL, Summon; KURHADE, Suresh; NAIK, Keshav; SALUNKHE, Videsh; KULKARNI, Rakesh; PARDESHI, Vishwajeet; BHUNIYA, Debnath; KULKARNI, Bheemashankar; MOOKHTIAR, Kasim Abbaas; (274 pag.)WO2017/38909; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6,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.

Solid K2CO3 (10 g, 72.4 mmol, 1.8 eq) is added to a solution of (R)-2-methyl-piperazine (4.00 g, 40 mmol, 1 eq) and 3,6-dichloro-4,5-dimethyl-pyridazine (8 g, 45.2 mml, 1.1 eq) in DMF (50 mL), and the resulting solution is stirred at 60¡ã C. for 48 h. The reaction mixture is concentrated to 1/2 volume under reduced pressure and the minimum water (ca. 15 mL) required to dissolve the solid salts is added, followed by the addition of dichloromethane (100 mL). The organic layer is separated, dried over sodium sulfate and concentrated under reduced pressure, then purified by silica gel column chromatography (2percent-20percent MeOH/CH2Cl2) to yield the desired compound as a white solid (4.7 g, 49percent).1H NMR (400 MHz, CDCl3) delta=3.08-3.21 (m, 2H), 2.73-2.92 (m, 4H,) 2.47 (dd, J=12.4 Hz, 10.2 Hz, 1H), 2.13 (s, 3H), 2.07 (s, 3H), 0.93 (d, J=6.3 Hz, 3H).HR MS (m/z, MH+): meas. 241.1218.

75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Novartis AG; US2010/41663; (2010); 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

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

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

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

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

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.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