Heterocyclic Building Blocks-piperazine

509073-62-5, tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of compound 8 (6.0 g, 20 mmol) in H2O (8 mL) andEtOH (24 mL) was added Fe (4.5 g, 80 mmol) and NH4Cl (1.5 g,28 mmol). The mixture was heated under reflux for 2 h. The solidwas filtered off and the liquid was concentrated under vacuum toafford the crude product. The crude product was purified by columnchromatography to provide compound 9 as yellow solid (5.7 g,yield: 93%). Mp: 155-156 C. 1H NMR (400 MHz, CDCl3) delta 7.25 (d,J = 8.4 Hz, 2H), 6.65 (d, J = 8.4 Hz, 2H), 3.94 (s, 2H), 3.59 (s, 4H), 3.44(s, 4H), 1.47 (s, 9H). 13C NMR (100 MHz, CDCl3) delta171.02, 154.54,148.36, 129.26, 124.44, 114.10, 80.15, 44.01, 43.30, 28.29.

509073-62-5, 509073-62-5 tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate 2764459, apiperazines compound, is more and more widely used in various fields.

Reference：
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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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.,115619-01-7

EXAMPLE IB5-bromo-N2-[4-(4-ethylpiperazin-l-yl)phenyl]-N4-[2-(trifluoromethyl)-lH-benzimidazol-5-yl]pyrimidine-2,4-diamineA scintillation vial was charged with EXAMPLE IA (98 mg, 0.25 mmol), 4- (4- ethylpiperazin-l-yl)aniline (66.7 mg, 0.325 mmol), n-butanol (4 ml) and 4 N hydrogen chloride in dioxane (62.5 muL, 0.250 mmol). The mixture was stirred at 80 0C overnight. The reaction mixture was cooled and quenched with water (10 mL), adjusted to pH -135089667 1 with slow addition of cone. aq. NaOH. The mixture was extracted with ethyl acetate and the extract was concentrated. The crude product was purified with HPLC on a Cl 8 reverse-phase column using a gradient of water and acetonitrile with 0.1% TFA as a buffer. The title compound was obtained as the TFA salt as an off-white solid (100 mg, 51%). MS: (ESI(+)) m/e 561.2, 563.2 (M+H)+; 1H NMR (500 MHz, DMSO-d6) delta ppm 9.53 (bs, IH), 9.39 (s, 1 H), 8.99 (s, IH), 8.22 (s, IH), 7.94 (s, IH), 7.73 (d, IH), 7.57 (d, IH), 7.43 (d, 2H), 6.76 (d, 2H), 6.51 (s, IH), 3.66-3.53 (m, 4H), 3.21-3.09 (m, 4H), 2.87 (U H), 1.26 (q, 3H).

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

Reference：
Patent; ABBOTT LABORATORIES; WANG, Gary, T.; MANTEI, Robert, A.; ERICKSON, Scott, A.; FIDANZE, Steve, D.; SHEPPARD, George, S.; WANG, Jieyi; BELL, Randy, L.; WO2010/138578; (2010); A1;,
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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

In 25 ml water compound is added in the bottle (J) 100 mg, EDCI67mg, dichloromethane 10 ml, reaction solution stirring 30 minutes, the compound is added (K) (in accordance with WO2012058392 method preparation) 55 mg, finally adding catalytic DMAP, reaction solution adding stirring reaction sleepovers, to splines end of the detection reaction TLC solvent, ABT-199 HPLC purified to get the pure product 98 mg, yield 65%., 1235865-77-6

As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference：
Patent; Nanjing Acesys Pharmatech Co., Ltd; GE, MIN; XU, YUNLEI; (8 pag.)CN104370905; (2016); B;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78818-15-2, [0713] To the solution of XXIV-1 (20 g, 85.5 mmol) in DMF (100 mL) was added NaH (60%, 4.1 g, 103 mmol) in portions. The mixture was stirred at rt for 30 mm. Then XXIV-2 (14.3 g, 85.5 mmol) was added. The reaction was stuffed at rt overnight. The reaction was quenched with ice- water carefully, and then extracted with EtOAc (100 mLx2). The combined organic layer was washed with brine, dried over anhydrous Na2SO4 and concentrated. The residue was used for next step directly (40 g, 140% crude yield).

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; INTERMUNE, INC.; RAMPHAL, Johnnie, Y.; BUCKMAN, Brad, Owen; EMAYAN, Kumaraswamy; NICHOLAS, John, Beamond; SEIWERT, Scott, D.; WO2015/153683; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Compound P42: 5-(Morpholin-4-yl)-2-nitroaniline To the flask 2-amino-3-nitro-6-chloropyridine (1.50 g, 8.47 mmol), potassium carbonate (1.30 g, 9.32 mmol) and morpholine (10.5 ml, 119 mmol) were added. The reaction was carried out under argon flow at 130°C overnight. The progress of the reaction was monitored by TLC (system: heptane/ethyl acetate, 1 /1 ). The mixture was cooled to room temperature and poured into the ice-water. A precipitated yellow solid was filtered and dried. 1.789 g of the title product were obtained (yield 94.2percent). Compound P58: 2-Nitro-3-[4-(propan-2-yl)piperazin-1 -yl]aniline; The compound was obtained by the method analogous to that described for Compound P42. Starting from 3-chloro-2-nitroaniline (0.459 g, 2.61 mmol), potassium carbonate (0.368 g, 2.66 mmol) and 1 -isopropylpiperazine (1.00 g, 0.741 mmol), 0.602 g of the title product in the form of a red solid were obtained (yield 91.9percent). MS-ESI: (m/z) calculated for Ci3H2iN402 [M + H]+: 265.16, found 265.1 1H NMR (500 MHz, DMSO-d6) delta 7.10 (dd, J = 8.1 Hz, 1 H), 6.52 (dd, J = 8.3, 1.0 Hz, 1 H), 6.35 (dd, J = 8.0, 1.0 Hz, 1 H), 5.83 (s, 2H), 2.85 (dd, J = 17.4, 12.8 Hz, 4H), 2.68 – 2.60 (m, 1 H), 2.47 (dd, 4H), 0.97 (d, J = 6.5 Hz, 6H).

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; CELON PHARMA S.A.; ZDZALIK, Daria; LIPNER, Joanna; WIECZOREK, Maciej; DZWONEK, Karolina; YAMANI, Abdellah; DUBIEL, Krzysztof; LAMPARSKA-PRZYBYSZ, Monika; GRYGIELEWICZ, Paulina; STANCZAK, Aleksandra; WO2014/141015; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, Example No. 134Preparation of (4-methylpiperazin-l-yl) (4- ( (5- (thiophen-2-yl) – IH-pyrazolo [4 , 3 -d] pyrimidin-7-yl) amino) phenyl) methanone7-chloro-2- (4-methoxybenzyl) -5- (thiophen-2-yl) -2H- pyrazolo [4 , 3 -d] yrimidine (0.16 mmol) and (4 -aminophenyl) (4- methylpiperazin-l-yl) methanone (0.3 mmol 2 eq. , ) were suspended in MeOH (dry, 3mL) in a microwave vial (2-5mL) , HCl in dioxane (4M, 3 drops) was added. The reaction mixture was irradiated in a microwave reactor for 5 min at 140C. The reaction mixture was evaporated and used without further purification. The residue was dissolved in TFA (3mL) . The reaction mixture was irradiated in a microwave reactor for 5 min at 140C. The reaction mixture was concentrated and purified by semi -preparative HPLC-MS and freeze dried from water/t-BuOH 4/1. exact mass: 419.1830 g/molHPLC-MS: analytical method Crt: 1.97 min – found mass: 420 (m/z+H)

55121-99-8 (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone 231408, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORIGENIS GMBH; ALMSTETTER, Michael; THORMANN, Michael; TREML, Andreas; TRAUBE, Nadine; WO2012/143144; (2012); A1;,
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5521-39-1, 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5521-39-1

EXAMPLE 39 6-Methoxy-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid {4-[4-(2hydroxy-ethyl)-piperazin-1-yl]-phenyl}-amide. This compound was prepared from 6-methoxy-8-(4-Methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid hydrochloride (Reference Example 2) and 2-[4-(4-amino-phenyl)-piperazin-1-yl]-ethanol (Reference Example 19) as prepared in Example 12, yielding a yellow solid. (80mg=60%). mp=211.5-212.2 (dec.), MS-base peak at m/z=492 by positive ion and m/z=490 by negative ion CI

5521-39-1 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol 767100, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Pierson, Edward; Sohn, Daniel; Haeberlein, Markus; Davenport, Timothy; Chapdelaine, Marc; Horchler, Carey; McCauley, John P.; US2003/13708; (2003); A1;,
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5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5464-12-0, 10.373 g 4-bromo-2-chlorophenol (50 mmol), 14.442 g 2-(4-methylpiperazin-l-yl)ethanol (100 mmol) and 26.229 g PPh3 (100 mmol) were dissolved in 250 mL dry toluene under N2 atmosphere, then 23.027 g DTAD (100 mmol) was added. The mixture was stirred at 50 °C until no further conversion was observed. The volatiles were evaporated under reduced pressure and the residue was purified via flash chromatography using EtOAc and MeOH as eluents. MS (M+H): 333.0

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference：
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; BALINT, Balazs; CSEKEI, Marton; SZABO, Zoltan; SZLAVIK, Zoltan; KOTSCHY, Andras; CHANRION, Maia; GENESTE, Olivier; CHEN, I-Jen; DAVIDSON, James Edward Paul; MURRAY, James Brooke; SIPOS, Szabolcs; ONDI, Levente; PROSZENYAK, Agnes; (164 pag.)WO2016/207217; (2016); A1;,
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5625-67-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

1 Syntheis of 4-tert-Butoxycarbonyl-2-oxopiperazine Di-tert-butyl dicarbonate (10.4 g, 47.6 mmol) was added to a stirred solution of 2-oxopiperazine (4.77 g, 47.6 mmol) in ethanol (100 ml) at room temperature. After stirring at room temperature for 1 hour, the reaction mixture was concentrated in vacuo to give 4-tert-butoxycarbonyl-2-oxopiperazine as colorless crystals (8.00 g, 84%), which were collected by filtration and washed with hexane. 1H-NMR (200 MHz, CDCl3) delta: 6.90-6.56 (1H, m), 4.09 (2H, s), 3.64 (2H, t, J=5.2 Hz), 3.44-3.34 (2H, m), 1.48 (9H, s). IR (KBr): 3265, 3195, 2981, 1691, 1666, 1635, 1419, 1398, 1365, 1338, 1243, 1176, 1131, 1002 cm-1.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Takeda Chemical Industries, Ltd.; US6235731; (2001); B1;,
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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 80 : (2,2-Dimethyl-piperazin- 1 -yl)-(6-methoxy-pyridin-2-yl)-methanone trifluoro acetate 80.1 : 4-(6-Methoxy-pyridine-2-carbonyl)-3,3-dimetyl-piperazine-l-carboxylic acid tert- ester A mixture of 410 mg (2.28 mmol) 6-methoxy-2-pyridinecarboxylic acid and 400 (3.02 mmol) l-chloro-N,N,2-trimethylpropenylamine in 10 mL THF was stirred at RT. After 1.5 h, 600 mg (2.66 mmol) 3,3-dimethyl-piperazine-l-carboxylic acid tert-butyl ester and 1.00 mL (5.81 mmol) DIPEA was added and the reaction mixture was stirred at RT for 30 min. The reaction mixture was diluted with saturated NaHCC”3 solution and extracted with EtOAc. The combined organic phases were dried over sodium sulfate, filtered and concentrated in vacuo. The crude material was purified by flash chromatography (PE/EtOAc = 1/1). Yield: 780 mg (84 %) ESI-MS: m/z = 350 (M+H)+ Rt(HPLC) : 1.23 min (method 3), 259808-67-8

The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; WO2013/87805; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics