Heterocyclic Building Blocks-piperazine

78551-60-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To EtMgBr (344 mL) in THF cooled to -78C was added Ti(O1Pr)4 (39 g, 137.93 mmol), followed by commercially available 4-benzyl-3-oxo-piperazine-l-carboxylic acid tert- butyl ester (40 g, 137.93 mmol) and the resultant reaction mixture was heated to reflux for 1 h. After cooling the reaction mixture to 5C, another portion of EtMgBr (344 ml) and Ti(O1Pr)4 (39 g, 137.93 mmol) was added. The mixture was stirred for 16 h at RT. The reaction mixture was quenched with NH4CI solution and stirred for 15 min and filtered through a celite bed and washed with EtOAc. The aqueous layer was again extracted with EtOAc (3 x). The combined EtOAc layers were washed with water and dried over Na2SO4 and concentrated under reduced pressure. Purification by column chromatography to afforded the title compound as a solid (24 g, 58%). 1H NMR (300 MHz, DMSO) delta = 7.20 (m, 5H), 3.80 (s, 2H), 3.40 (m, 2H), 3.22 (m, 2H), 2.63 (m, 2H), 1.38 (s, 9H), 0.58 (br, 4H)

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LEO PHARMA A/S; NIELSEN, Simon Feldbaek; GREVE, Daniel, Rodriguez; RYTTERSGAARD, Carsten; GRUE-S?RENSEN, Gunnar; OTTOSEN, Erik, Rytter; POULSEN, Tina, Dahlerup; SCHOU, S¡ãren, Christian; MURRAY, Anthony; WO2011/3418; (2011); A1;,
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5271-27-2, 1-Methyl-3-phenylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5271-27-2, General procedure: 4.2 General procedures: C. Reflux. Carried out under an inert atmosphere in the normal way.

5271-27-2 1-Methyl-3-phenylpiperazine 2760009, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Dubois, Nathalie; Glynn, Daniel; McInally, Thomas; Rhodes, Barrie; Woodward, Simon; Irvine, Derek J.; Dodds, Chris; Tetrahedron; vol. 69; 46; (2013); p. 9890 – 9897;,
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70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add 8.5 g (36.2 mmol) of crude I-a to a 500 mL one-necked flask. 2.0 g of FeO(OH)/C catalyst and 100 mL of 95% ethanol, Heating back, Slowly add a mixture of 25 mL of hydrazine hydrate and 20 mL of 95% ethanol. The disappearance of the starting material by TLC (methanol: chloroform = 1:15). Hot and suction filtration, The filter cake was washed twice with hot ethanol (30 mL x 2). The solvent was evaporated under reduced pressure to give a white solid. It was dried under vacuum to give (I-b) 6.7 g, yield: 90.3%. The product was directly fed to the next reaction without further purification., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; China Pharmaceutical University; Wang Yue; Lu Shuai; Zhi Yanle; Yao Chao; Lu Tao; Li Baoquan; Chen Puzhou; Bao Jiyin; (26 pag.)CN109970717; (2019); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.930782-89-1,(R)-4-Benzyl 1-tert-butyl 2-(hydroxymethyl)piperazine-1,4-dicarboxylate,as a common compound, the synthetic route is as follows.

930782-89-1, Compound 28 (4.74 g, 13.53 mmol) was dissolved in anhydrous DCM (45 mL) and triethylamine (7.54 mL, 54.11 mmol) added and the mixture was cooled to 0 C. A solution of pyridine sulfur trioxide (6.46 g, 40.58 mmol) in DMSO (45 mL) was added at 0 C and stirred for 1 hour. The reaction was quenched with a saturated NaHCCb solution and diluted with ether. The aqueous phase was extracted with ether (3x). Combined organic layers were extracted with sodium phosphate dibasic (Na2HP04), 1M HC1 and brine; dried over anhydrous Na2S04, filtered and evaporated. The crude product was used for the next step without purification.

930782-89-1 (R)-4-Benzyl 1-tert-butyl 2-(hydroxymethyl)piperazine-1,4-dicarboxylate 16124590, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; ALTAS TAHIROVIC, Yesim; WILSON, Lawrence; PELLY, Stephen Christopher; (102 pag.)WO2019/183133; (2019); A1;,
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20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 6(4-Cvclopropyl-piperazin-1 -yl)-(4-morpholin-4-ylmethyl-phenyl)- methanone bis-hvdrochloride saltStep A: PreparationA 100-L glass-lined reactor was charged with toluene (45.00 kg) and stirred at ~20-25C. To the stirring toluene was added 4-(4- morpholinylmethyl)benzoic acid hydrochloride (6.50 kg, 93.5%, 24.04 mol), 1- hydroxybenzothazole monohydrate (2.32 kg, 15.13 mol), 1 – cyclopropylpiperazine (3.50 kg, 27.07 mol) and acetonitrile (9.00 kg). The resulting off-white slurry was stirred under N2 at ~20-25C for 40 minutes. N- (3-Dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (3.50 kg, 27.07 mol) was added, followed by an acetonitrile (1 .20 kg) rinse. After the addition, the reaction mixture was stirred at ~20-25C overnight. Water (32.50 kg) and aqueous saturated sodium carbonate (19.50 L) were then added to the stirring suspension. The suspension was stirred for an additional 30 minutes. The resulting biphasic solution was allowed to settle. The aqueous phase was discarded and the organic phase was washed with a 50% brine solution [water (19.50 L) / brine (19.50 L)]. To the stirred organic phase was then added anhydrous sodium sulfate (2.86 kg) and the resulting mixture was stirred at ~20-25C for 1.5 hours. The solid sodium sulfate was filtered off and the filter cake was washed with acetonitrile (15.30 kg). The filtrate was transferred to a clean 100-L glass-lined reactor and stirred at ~20-25C. Water (0.47 kg) and 5/6N HCI in 2-propanol were added to precipitate the title compound as the corresponding bis-hydrochloride salt as a solid. The solid was filtered, washed with acetonitrile (10.2 kg) and dried (60 Torr, ~40-45C) to a constant weight to yield the title compound as a white solid.Step B: PurificationIn a 50-L glass reactor, the white solid prepared as in Step A above (15.0 kg, 37.28 mol) was dissolved in 1 :1 (v/v) mixture of ethanol :water (15.0 L: 15.0 L) at ~20-25C. The resulting mixture was stirred for 45 minutes and polish filtered (to remove any foreign particles) into a clean 100-L glass-lined reactor. The filtrate was transferred to a clean reaction vessel. Upon stirring, (polish filtered) ethanol (75.0 L) was added and the title compound precipitated as a bis-HCLmono-hydrate salt. The resultant white slurry was stirred at -20- 25C overnight. The solid was filtered, washed with ethanol (7.5 L) and dried at ~20-25C under vacuum to yield the title compound as a monohydrate bis- hydrochloride salt as a white solid.Karl Fisher analysis showed 3.4-3.6% water present. Chromatographic Purity (%w/w) showed 96.6%, 20327-23-5

As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/76685; (2008); A2;,
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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.

8-tert-butyl-6-(4-fluorophenyl)imidazo[l,2-b]pyridazine-2-carboxylic acid (5g, 16 mmol), DMF (l20mL), HATU (7.3g, 19.2 mmol), tert-butyl 3, 3 -dimethylpiperazine-l -carboxylate (4.lg, 1.92 mmol) and DIPEA (lOmL, 57.4 mmol) afforded tert-butyl 4-(8-(tert-butyl)-6- (4-fluorophenyl)imidazo [l,2-b]pyridazine-2-carbonyl)-3 ,3 -dimethylpiperazine- 1 – carboxylate that was dissolved in 4N HC1 solution in l,4-dioxane (60 mL) affording 4-(8- (tert-butyl)-6-(4-fluorophenyl)imidazo[l,2-b]pyridazine-2-carbonyl)-3,3- dimethylpiperazine hydrochloride (6.5g, 97%) as a solid. 1H NMR (401 MHz, DMSO) d 9.71 (bs, 2H), 8.57 (s, 1H), 8.17 – 8.10 (m, 2H), 7.50 (s, 1H), 7.44 – 7.36 (m, 2H), 4.16 – 4.08 (m, 2H), 3.35 – 3.27 (m, 2H), 3.23 – 3.14 (m, 2H), 1.61 (s, 6H), 1.59 (s, 9H)., 259808-67-8

As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; AURELIO, Luigi; BUNNETT, Nigel; FLYNN, Bernard Luke; GIANG, Le; (125 pag.)WO2019/124567; (2019); A1;,
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120737-78-2, 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 : To a lOOmL three-necked flask was added 20mL toluene and compound 13a (3g, 0.014mol, l .Oeq), compound 13b (4.3g, 0.022mol, 1.5eq) and t-BuONa (2.064g, 0.022mol, 1.5eq). The reaction was heated to 80oC with nitrogen. Then BINAP (0.3g, 0.42mmol, 0.03eq) and Pd2(dba)3.CHCl3 (0.15g, 0.14mmol, O.OOleq) was added to the stirred mixture . The reaction was heated to reflux for 18h. The solution was cooled, concentrated and extracted with 30 EA from lOmL water. The organic layer was washed with brine , dried , concentrated in vacuum and purified by column chromatography on silica gel eluted with PE: EA= 10: 1 to afford the compound 13c (4g, HPLC: 98%) as a white solid. Yield: 86%.

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LIANG, Congxin; (62 pag.)WO2018/5713; (2018); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.692058-21-2,1-Boc-4-(2,2,2-trifluoroethyl)piperazine,as a common compound, the synthetic route is as follows.

Hydrogen chloride gas was bubbled through a solution of tert-butyl 4- (2, 2, 2-TRIFLUOROETHYLPIPERAZINE-1-CARBOXYLATE (8 g) in ethyl acetate (50 ml) during 1.5 hours. A precipitate formed as carbon dioxide gas was evolved. The precipitate was collected by filtration, washed with ethyl acetate and dried under vacuum. There was thus obtained 1- (2, 2, 2-trifluoroethyl) piperazine hydrochloride (7 g); NMR Spectrum : (DMSOd6 and CF3CO2D) 2.85 (m, 4H), 3.1 (m, 4H), 3.35 (q, 2H), 692058-21-2

692058-21-2 1-Boc-4-(2,2,2-trifluoroethyl)piperazine 16748694, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/41829; (2004); A1;,
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118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a well-stirred solution of intermediate 5a (2.0 g,5.29 mmol) in ethanol (10 mL) was added 1-amino-4-methylpiperazine 9a (0.61 g, 5.29 mmol) and a drop of acetic acid,and the mixturewas stirred at 78 C for 2 h. The mixturewas cooledto room temperature and the resulting solid was collected byfiltration and purified by column chromatography to give the targetcompounds 6a-1 as a yellow solid in 75% yield. M.p: 228-230 C;

118753-66-5, As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

Reference£º
Article; Wu, Yachuang; Ding, Xiudong; Yang, Yifeng; Li, Yingxiu; Qi, Yinliang; Hu, Feng; Qin, Mingze; Liu, Yajing; Sun, Lu; Zhao, Yanfang; European Journal of Medicinal Chemistry; vol. 185; (2020);,
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30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of Intermediate?B? (150 mg, 0.41 mmol) in CH2CI2 (5 mL) was added Et3N (126 mg, 1.25 mmol), in portions, followed by the addition of l-[4-(trifluoro- methyl)phenyl]piperazine (96 mg, 0.42 mmol), in portions. The resulting solution was stirred for 16 h at rt, then quenched by the addition of 20 mL H2O and extracted with 2×20 mL of EtOAc. The combined organic layers were concentrated under vacuum to afford 180 mg (90%) of the title compound as an off-white solid. LC-MS: (ES, m/z) 480, 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CENTAURUS THERAPEUTICS; ROMERO, Donna, L.; BLITZER, Jeremy; (242 pag.)WO2019/140188; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics