Category: piperazines

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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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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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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Piperazines – an overview | ScienceDirect Topics

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.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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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.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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122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: General procedure for the synthesis of 15b-15u. To a solution ofcompound 13a (0.41 g, 1.06 mmol) in 2-butanol (5 mL), 1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-amine (0.196 g, 1.27 mmol)and trifluoroacetic acid (94 mL) were added in a sealed tube. Thereactionwas heated at 95 C for 18 h. The reaction mixturewas thenallowed to cool to room temperature. The mixture was transferredto a round-bottom flask and then the solvent was removed underreduced pressure. The residue was dissolved in DCM (2.0 mL) andTFA (2.0 mL), and the resulting mixture was stirred for 5 h at roomtemperature. The solvent was removed under reduced pressure,and the residue was neutralized with saturated NaHCO3 aqueoussolution. The water layer was extracted with DCM. The organiclayer was combined and washed with brine, dried over Na2SO4,filtered, concentrated, and purified by silica gel chromatography toafford 15a as a yellow solid (0.264 g, 65% for two steps)., 122833-04-9

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Yu, Lei; Huang, Minhao; Xu, Tianfeng; Tong, Linjiang; Yan, Xiao-e; Zhang, Zhang; Xu, Yong; Yun, Caihong; Xie, Hua; Ding, Ke; Lu, Xiaoyun; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 1107 – 1117;,
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674792-05-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.674792-05-3,(S)-1-Boc-2-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

1-Propanephosphonic acid cyclic anhydride (1.752mmol, 1.043ml_, 1115mg) was added to a solution of (S)-tert-butyl 2-isopropylpiperazine-1-carboxylate (0.876mmol, 200mg), 4-amino-3-fluorobenzoic acid (0.876mmol, 136mg) and triethylamine (1.752mmol, 0.244 mL, 177mg) in dichloromethane and stirred at room temperature for 2 hours. After this time, ethyl acetate (10OmL) was then added to the reaction. The organic mixture was washed with saturated sodium hydrogen carbonate, water, dried over sodium sulphate and concentrated under vacuum. The residue was then dissolved in dichloromethane (5ml_) and trifluoroacetic acid (17.52mmol, 1997mg) added. The resultant solution was allowed to stand at room temperature overnight. The reaction was concentrated under vacuum and purified by strong cation exchange chromatography to give the title compound (200mg) as a clear oil. MS (ESI) m/z 266.3 [M+H]+

As the paragraph descriping shows that 674792-05-3 is playing an increasingly important role.

Reference£º
Patent; N.V. ORGANON; WO2009/24550; (2009); 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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

100g of concentrated hydrochloric acid (12mol / L) 250ml round bottom flask was placed in an ice bath, was slowly added 40g of anhydrous piperazine, the addition, the ice bath was removed, the reaction overnight at room temperature, filtered off with suction, the filter cake was placed It was dried in an oven, the resulting white solid, a piperazine dihydrochloride. o-fluorobenzoic acid was weighed 7g (0.05mol) dissolved in 20ml of dry tetrahydrofuran, was slowly added CDI 8.9g (0.055mol), after 4h the reaction was reacted at room temperature 4 h. Then a constant pressure dropping funnel was added dropwise a solution of piperazine dihydrochloride hydrochloride 20g (0.125mol), anhydrous piperazine 10g (0.125mol), 60ml of 14g of sodium chloride at room temperature after 5 hours the reaction solution is suction filtered, the filtrate was evaporated to dryness to remove THF, extracted with ethyl acetate again 10ml, NaOH saturated solution was adjusted to pH 10, and extracted 3 times with ethyl acetate and the combined organic phases, the organic phase was dried over anhydrous sodium sulfate overnight, filtration, rotary evaporation of ethyl acetate, the resulting white crystals which was 1- (2-fluorophenyl formyl) piperazine The crude product 4.7g, 45% yield.

142-64-3, As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference£º
Patent; XI’AN JIAOTONG UNIVERSITY; ZHANG, JIE; ZHANG, TAO; DONG, JINYUN; PAN, XIAOYAN; HE, LANGCHONG; LU, WEN; WANG, SICEN; SHI, YALING; (19 pag.)CN104262263; (2017); B;,
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Piperazines – an overview | ScienceDirect Topics