Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.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,as a common compound, the synthetic route is as follows.

2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl)methyl)piperazin-1-yl)benzoic acid (100 mg, 0.175 mmol)Ethyl 8-(2-nitro-4-aminosulfonylphenylamino)octanoate 68mg (0.175mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride (EDCI) 167mg (0.875mmol), 4- dimethylaminopyridine 25.6mg (0.21mmol) ,With anhydrous DCM as solvent, at room temperature for 24h. After the reaction was completed, with 1 M hydrochloric acid,Saturated sodium bicarbonate, saturated brine, the aqueous phase was extracted with EA, the organic phase was combined,Concentration gave 160 mg of a solid which was purified by column chromatography with a yield of 85%., 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; Second Military Medical University; Zheng Canhui; Zhu Ju; Zhou Youjun; Wang Zhongqing; Wang Mingping; Yang Chao; Tian Wei; (18 pag.)CN106957315; (2017); A;,
Piperazine – Wikipedia
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70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,70261-82-4

To a solution of 4-(3-(4-cyanophenyl)imidazo[1,2-a]pyridin-6-yl)benzoic acid (70 mg, 0.206 mmol) in DMF (1.0 mL) were added HATU (117 mg, 0.309 mmol), N-methyl morpholine (90 muL, 0.824 mmol) and 4-((4-methylpiperazin-1-yl)methyl)aniline (51 mg, 0.309 mmol). The reaction mixture was stirred at room temperature under inert atmosphere for 18 h, then it was diluted with water (15 mL) and extracted with EtOAc (3*30 mL). The combined organic layer was dried over Na2SO4 and was concentrated under reduced pressure. The residue was purified by preparative HPLC (C18, eluent ACN, water, formic acid 0.1%) to afford 4-(3-(4-cyanophenyl)imidazo[1,2-a]pyridin-6-yl)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)benzamide (40 mg, 37%, AUC HPLC 99%) as a white solid. 1H NMR (400 MHz, CD3OD) delta 8.78 (s, 1H), 8.05 (d, J=8.4 Hz, 2H), 7.96-7.90 (m, 4H), 7.84 (s, 1H), 7.83 (d, 0.1=8.4 Hz, 2H), 7.80-7.76 (m, 2H), 7.68 (d, J=8.8 Hz, 2H), 7.34 (d, J=8.4 Hz, 2H), 3.56 (s, 2H), 2.70-2.40 (m, 8H), 2.36 (s, 3H); 13C NMR (100 MHz, CD3OD): delta 168.12, 147.47, 141.62, 139.17, 135.76, 134.82, 134.74, 134.53, 134.40, 131.08, 129.56, 129.44, 128.49, 128.30, 127.79, 126.61, 122.95, 122.18, 119.51, 118.48, 112.72, 63.14, 55.55, 53.15, 45.65; MS (ESI) m/z 527 [C33H30N6O+H]+.

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Agency for Science, Technology and Research; Nacro, Kassoum; Duraiswamy, Athisayamani Jeyaraj; Rao, Lohitha; US2014/371199; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

A mixture of 1 -bromo-4-iodobenzene (0.87 g, 3.1 mmol), 4-methylpiperazin-2- one (0.30 g, 2.6 mmol), 3P04 (1.1 g, 5.1 mmol), trans-N, N’-dimethylcyclohexane-l ,2-diamine (0.08 mL, 0.51 mmol) and dioxane (5 mL) was purged with argon gas for 10 min. Copper(I) iodide (0.049 g, 0.26 mmol) was added, the vial sealed and heated at 110 C in an oil bath for 22 h. The reaction was then allowed to cool to rt and was diluted with EtOAc and saturatedNaHC03 was added. The resulting mixture was extracted with EtOAc and the combined organic extracts were dried over MgS04 and concentrated to give the crude product. Purification by silica gel chromatography (MeOH/CH2Cl2, 5:95 to 1 :9) gave an inseparable 2: 1 mixture of the desired product and l-(4-bromophenyl)-4-methylpiperazin-2-one (200 mg). NMR (400 MHz, CDCI3) 6 7.66 (d, J = 8.0 Hz, 2H), 7.02 (d, J = 8.0 Hz, 2H), 3.64 (t, J = 5.0 Hz, 2H), 3.22 (s, 2H), 2.73 (t, J = 5.0 Hz, 2H), 2.35 (s, 3H); MS ESI 317.1 [M + H]+, calcd for [C, ,H|3IN20+ H]+ 317.01.

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

Reference£º
Patent; UNIVERSITY HEALTH NETWORK; PAULS, Heinz, W.; LI, Sze-Wan; SAMPSON, Peter Brent; FORREST, Bryan T.; WO2012/48411; (2012); A1;,
Piperazine – Wikipedia
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54699-92-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.

Example 13; General Method For The Preparation Of Active Esters Of N-Substituted Piperazine Acetic Acid From Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

As the paragraph descriping shows that 54699-92-2 is playing an increasingly important role.

Reference£º
Patent; Applera Corporation.; US2005/148773; (2005); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 2: (S)-tert-butyl 2-methyl-4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indol-5-yl)piperazine-1-carboxylate To a solution of 5-bromo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indole (2 g, 6.13 mmol) and (S)-tert-butyl-2-methylpiperazine-1-carboxylate (1.23 g, 6.13 mmol) in toluene (20 mL) was added Pd2(dba)3 (281 mg, 0.31 mmol), BINAP (381 mg, 0.613 mmol), and t-BuONa (1.17 g, 12.26 mmol). The mixture was stirred at 80 C. for 5 hrs under nitrogen. The resulting mixture was concentrated in vacuo and the residue was purified by column chromatography on silica gel to give (S)-tert-butyl-2-methyl-4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indol-5-yl)piperazine-1-carboxylate (645 mg, 1.45 mmol, 16.5%) as a yellow liquid. ESI-MS (EI+, m/z): 446.4 [M+H]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); A1;,
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, As the paragraph descriping shows that 350684-49-0 is playing an increasingly important role.

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;,
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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 A: tert-Butyl (3S)-4- [2- (4-cyano-3-methoxyphenyl)-2-hydroxyethyl1 -3-(hydroxymethyl)piperazine- 1 -carboxylate: A Pyrex vessel was charged with magnetic stirring bar, (0.350 g, 2.00 mmol) of 2-methoxy-4-(oxiran-2-yl) benzonitrile, (0.457 g, 2.20 mmol) oftert-butyl (3S)-3-(hydroxymethyl)piperazine-1-carboxylate, and 6 mL of EtOH. Then it was introduced in the microwave reactor and irradiated at 150 C for 3 hr. Then the mixture was cooled to room temperature and the solvent was evaporated and the resulting residue was purified by column chromatography (silica gel, 1- 20% dichloromethane/MeOH) which afforded the title compound as a mixture of two diastereomers (1:1). LC/MS: (IE, m/z) [(M + 1) – t-Bu] =336.1., 314741-40-7

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

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

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: Preparation of tert-butyl (2S)-4-[[2-fluoro-4-(morpholin-4-yl)phenyl]methyl]-2- methylpiperazine-l-carboxylate [00251] A 100-mL round-bottom flask was charged with 2-fluoro-4-(morpholin-4- yl)benzaldehyde (0.800 g, 3.82 mmol, 1.00 equiv), tert-butyl (2S)-2-methylpiperazine-l- carboxylate (0.840 g, 4.20 mmol, 1.10 equiv), and 1,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.40 g, 1 1.3 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with 0 (10 mL), and extracted with dichloromethane (3 x 10 mL). The organic layers were combined and washed with brine (50 mL), dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was chromatographed on a silica gel column with ethyl acetate/petroleum ether (25/75) to provide 1.40 g (93% yield) of ter/-butyl (2S)-4-[[2-fluoro-4-(morpholin-4-yl)phenyl]methyl]-2-methylpiperazine-l-carboxylate as a white solid. LCMS (ESI, m/z): 394 [M+H]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Cheryl, A.; JONES, Todd, K.; WANG, Dong-Hui; WEBER, Olivia; CRAVATT, Benjamin, F.; NIPHAKIS, Micah, J.; COGNETTA, Armand; CHANG, Jae Won; WO2013/142307; (2013); 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,59878-57-8

General procedure: To a solution of 14 (200 mg, 0.63 mmol) in DMA (60 mL), HOBt(170 mg, 1.26 mmol), EDCI (242 mg, 1.26 mmol), and DIPEA(0.208 mL, 1.26 mmol) and then the corresponding piperazine wereadded, and the mixture was stirred overnight. Water (10 mL) wasadded to the mixture, which was stirred for an additional 1 h. Then,the mixture was extracted with ethyl acetate (50 mL x 3). Thecombined organic layers were washed with brine, dried overanhydrous sodium sulfate and concentrated to give the crudeproduct, which was purified by column chromatography to affordthe corresponding compounds in good yields.

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

Reference£º
Article; Chen, Wenhua; Guo, Ne; Qi, Minghui; Dai, Haiying; Hong, Minghuang; Guan, Longfei; Huan, Xiajuan; Song, Shanshan; He, Jinxue; Wang, Yingqing; Xi, Yong; Yang, Xinying; Shen, Yanyan; Su, Yi; Sun, Yiming; Gao, Yinglei; Chen, Yi; Ding, Jian; Tang, Yun; Ren, Guobin; Miao, Zehong; Li, Jian; European Journal of Medicinal Chemistry; vol. 138; (2017); p. 514 – 531;,
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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, Nitrobenzyl bromide and N- methyl piperazine after the substitutionreaction, and then get by stannous chloride reduction.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Patent; CHINA PHARMACEUTICAL UNIVERSITY; YANG, ZHAO; WANG, ZHIXIANG; FANG, ZHENG; GUO, KAI; WEI, PING; (23 pag.)CN103739550; (2016); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics