Category: piperazines

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

118753-66-5, Synthesis of Compound 3: Commercially available 1 -t-butyloxycarbonyl-4-amino-piperazine 1 (1 .0 g, 4.97 mmol) and N-acetyl-4-piperidone 2 (0.61 1 ml_, 4.97 mmol) were stirred in 30 mL of dichloromethane at room temperature for 30 minutes. To the solution was added 1 .68 g of solid sodium triacetoxyborohydride (7.95 mmol) in portions, and the suspension was stirred at room temperature over night. Additional sodium triacetoxyborohydride (500 mg, 2.36 mmol) was added and stirred for 5 hours. The reaction mixture containing product 3 was used directly in the next step.

118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PALATIN TECHNOLOGIES, INC.; BULLINGTON, James; METZGER, Axel; DODD, John, H.; (0 pag.)WO2020/60983; (2020); A2;,
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132710-90-8, 1-Boc-4-(3-hydroxypropyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

C: 4-(3-Bromo-propyl)-piperazine-1-carboxylic acid tert-butyl Ester Under nitrogen atmosphere, a solution of triphenylphosphine (0.94 g) in THF (4 ml) was added slowly to a mixture of 4-(3-hydroxy-propyl)-piperazine-1-carboxylic acid tert-butyl ester (0.80 g) and tetrabromomethane (1.19 g) in THF (15 ml). The mixture was stirred at room temperature for 16 hours, then ethyl acetate (100 ml) and a saturated solution of sodium carbonate (30 ml) were added and the organic layer was washed with brine, then dried over sodium sulfate, filtered and concentrated under reduced pressure. The residue was chromatographed over silica gel (eluent: Cyclohexane/Ethyl acetate 8/2) to afford 4-(3-bromo-propyl)-piperazine-1-carboxylic acid tert-butyl ester (0.66 g). 1H NMR (CD3CN) delta: 3.47 (m, 2H); 3.42 (m, 4H); 2.48 (m, 2H); 2.38 (m, 4H); 2.02 (m, 2H); 1.46 (s, 9H)., 132710-90-8

The synthetic route of 132710-90-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; N. V. Organon; US2009/99172; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile(prepared as described aboye for I-42A and I-42B, Method 1, Steps A-C) (4.80 g, 27.1 mmol)and (R)-4-N-BOC-2-hydroxymethyl-piperazine (8.79g. 40.6 mmol) were suspended in EtOH (30mL) and heated in a microwaye apparatus at 150 C for 1 h. The reaction rnixture was cooled and eyaporated to dryness. The residue was purified by chromatography through a 330 g ISCO Redi-sep column eluting with ethyl acetate to 5% MeOH/ ethyl acetate to yield the titlecompound. LC-MS: M+1= 394;, 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DE JESUS, Reynalda, Keh; DING, Fa-xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; SHAHRIPOUR, Aurash; PIO, Barbara; TANG, Haifeng; WALSH, Shawn; WO2014/126944; (2014); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.,115761-79-0

Take 50mL single-mouthed flask, was successively added 2-(1-(hydroxymethyl)cyclopropyl)methoxy-5-(methylsulfonyl)benzoic acid (150mg, 0.50mmol), 1-(2,4-difluorophenyl)piperazine (120mg, 0.60mmol), HATU (285mg, 0.75mmol), TEA (0.25mL, 1.5mmol), DMF (10mL), the reaction at room temperature overnight, saturated sodium chloride (20 mL), and extracted with ethyl acetate (20mL * 3). The organic phase was dried over anhydrous sodium sulfate and concentrated to dryness to give crude, the crude product was purified by preparative plate 130mg, yield: 55%.

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Hansoh BioMedical Co., Ltd.; Jiangsu Stockhausen Pharmaceutical Group Co., Ltd.; Liao, Jianchun; Yu, Hongping; Xu, Yaochang; Chen, Jianghua; Zhang, Shaobao; Xiu, Wenhua; Liu, Zhaomin; (48 pag.)CN105712952; (2016); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

P-toluenesulfonic acid (150 mg, 0.84 mmol) was added to the solution of 6-(2-chloropyrimidin-4-yl)-4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole (compound 3, 130 mg, 0.42 mmol) and 2-methoxy-4-(4-methylpiperazin-1-yl)aniline (compound 6, 111 mg, 0.50 mmol) in isopropyl alcohol (3 mL), and reacted under microwave at 180 C. for 1 hour. The reaction mixture was concentrated under reduced pressure, the residue was adjusted to basic with saturated sodium bicarbonate, extracted with dichloromethane (30 mL¡Á3), the organic phase was combined, washed with brine (30 mL) and dried over anhydrous sodium sulfate, the solvent was removed, and the filtrate was separated on column chromatography (eluant:dichloromethane/methanol (v/v)=13:1), to afford 40 mg of a pale yellow solid, yield was 19.4%. LC-MS(APCI): m/z=490.3 (M+1); 1H NMR (500 MHz, DMSO-d6) (delta/ppm) 8.42 (d, J=5.2 Hz, 1H), 8.26 (s, 1H), 8.06 (s, 1H), 7.82 (d, J=8.7 Hz, 1H), 7.74 (d, J=12.1 Hz, 1H), 7.44 (d, J=5.2 Hz, 1H), 6.67 (d, J=2.2 Hz, 1H), 6.51 (dd, J=8.7, 2.3 Hz, 1H), 4.90-4.71 (m, 1H), 3.81 (s, 3H), 3.21-3.14 (m, 4H), 2.67-2.53 (m, 7H), 2.32 (s, 3H), 1.59 (d, J=6.9 Hz, 6H).

122833-04-9, The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shenzhen TargetRx, Inc.; Wang, Yihan; Ren, Xingye; Jin, Jian; Li, Huanyin; Ai, Yixin; (162 pag.)US2019/152954; (2019); A1;,
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78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

78818-15-2, [0921] 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 min. Then XXIV-2 (14.3 g, 85.5 mmol) was added. The reaction was stirred at rt overnight. The reaction was quenched with ice-water carefully, and then extracted with EtOAc (100 mL¡Á2). 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).

As the paragraph descriping shows that 78818-15-2 is playing an increasingly important role.

Reference£º
Patent; Buckman, Brad Owen; Nicholas, John Beamond; Ramphal, Johnnie Y.; Emayan, Kumaraswamy; Seiwert, Scott D.; US2014/94456; (2014); A1;,
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129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Int. 149 (0.7 g; 1.51 mmol) and DIPEA (0.77 mL; 4.53 mmol) were dissolved in DMF (8 mL) at 0 C under N2-gas atmosphere. Methanesulfonyl chloride (0.234 mL; 3.02 mmol) was added portionwise (3x 0.078 mL) at intervals of 5 min. The reaction mixture was allowed to warm up to room temperature. The mixture was reacted for 1 h, and then 1 ,2-piperazinedicarboxylic acid, l-(l , l-dimethylethyl) ester (0.738 g; 3.02 mmol) was added. The reaction mixture was heated at 80 C overnight. Subsequently, the mixture was concentrated to dryness. The residue was dissolved in DCM/MeOH 10/1 v/v (25 mL) and this solution was washed with 1 M NaC03solution in H20 (15 mL). The organic layers were combined, dried (MgSC^), filtered and concentrated to dryness. The residue was purified by column chromatography over silica gel eluting with a gradient from 100 % DCM to 100 % DCM/MeOH 9/1 v/v. The desired fractions were collected and the solvent was evaporated. Yield: 0.978 g of Int. 151 (94 %). The intermediates in the table below were prepared according to an analogous reaction protocol as used for Int. 151 :, 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; DIELS, Gaston, Stanislas, Marcella; SCHOENTJES, Bruno; VERSELE, Matthias, Luc, Aime; BERTHELOT, Didier, Jean-Claude; WILLEMS, Marc; VIELLEVOYE, Marcel; EMBRECHTS, Werner, Constant, Johan; WROBLOWSKI, Berthold; MEERPOEL, Lieven; WO2015/150555; (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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

4- (4-Amino-2-fluorophenyl)-1, 2-dimethylpiperazine; 4- (2-Fluoro-4-nitrophenyl)-2-methylpiperazine; To rac-2-methylpiperazine (2.64 g, 23.1 mmol) in acetonitrile (50 mL) was added triethylamine (1.95 g, 2.7 mL, 19.2 mmol) followed by 3,4-difluoronitrobenzene (1 g, 7.7 mmol) dropwise over 5 min under a nitrogen atmosphere. The resulting yellow solution was allowed to stir at room temperature for 3 days. Excess acetonitrile was removed by evaporation under reduced pressure and the residue reconstituted in DCM (50mL), washed with water (2x50mL), dried (MgS04) and concentrated to afford the title compound as a yellow solid. LC-MS (UV 215nm) : 100%; m/z 240. 19; 0.91 min. IH NMR (CDC13) : 1.13 (3H, d, J6. 4), 2.56 (1H, dd, J 10.2 11.7), 2.91-2. 99 (1H, m), 3.00-3. 13 (3H, m), 3.52-3. 59 (2H, m), 6.91 (1H, t, J 8.8), 7.85-8. 01 (2H, m)., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AMGEN INC.; WO2005/42518; (2005); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 126Atert-Butyl 3-methylpiperazine- 1 -carboxylate[00770] To a solution of 2-methyl-piperazine (2.0 g, 0.02 mol) and triethylamine (6 mL) in methylene chloride (15 mL) at 0 C was added (Boc O (4.14 g, 0.019 mol) dropwise. The mixture was stirred at room temperature for 1 hour, and then the solvent was removed by rotary evaporation. The residue was dissolved in methylene chloride, washed with saturated sodium bicarbonate and brine, dried over Na2S04, and purified by column chromatography on silica gel (DCM: MeOH:Et3N = 75 : 1 : 0.2) to give an white solid (1.65 g, 42%). LC-MS (ESI) m/z: 201 (M+l)+., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; CHU, Daniel; WO2011/130661; (2011); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.342405-34-9,4-(4-Methylpiperazino)benzyl Alcohol,as a common compound, the synthetic route is as follows.,342405-34-9

General procedure: To a 25-mL Schlenk tube equipped with a magnetic stirrer, CuCl (0.05 mol, 5 mol%), DABCO (0.10 mol, 10 mol%), 4-HO-TEMPO (0.05 mmol, 5 mol%) were added. Substrates 1 (1 mmol) and NH3 (aq, 25-28%, 3 mmol, 3.0 equiv) in CH3CN (2 mL) were added subsequently. Then the reaction mixture was stirred at room temperature for 24 h in the presence of an air balloon. The progress of the reaction was monitored by TLC. After completion, the reaction mixture was diluted with water and extracted with ethyl acetate. The organic layer was dried over anhydrous MgSO4. Subsequently, the combined organic layer was concentrated under reduced pressure and the crude product was purified by column chromatography to afford the corresponding products.

As the paragraph descriping shows that 342405-34-9 is playing an increasingly important role.

Reference£º
Article; Hu, Yongke; Chen, Lei; Li, Bindong; Chinese Chemical Letters; vol. 29; 3; (2018); p. 464 – 466;,
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Piperazines – an overview | ScienceDirect Topics