Month: September 2020

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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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;,
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.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;,
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.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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics