Heterocyclic Building Blocks-piperazine

928025-56-3,928025-56-3, (S)-tert-Butyl 3-ethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of tert-butyl (3S)-3-ethylpiperazine-l -carboxylate (0.5 g, 2.3 mmol) and 2-amino-4,6-dichloropyrimidine-5-carbaldehyde (0.45 g) in 1,4-dioxane (8.0 mL) was added DIPEA (1.2 mL, 7.0 mmol). The reaction mixture was heated at 120C overnight in a sealed Wheaton vial, then cooled and stirred at room temperature over the weekend. The solvent was removed in vacuo, and the residue was partitioned between water and DCM. The organic layers were phase separated and concentrated in vacuo to give the title compound (0.85 g, 99%) as a yellow glass. LCMS (ES+) [M+H]+ 370, RT 1.81 minutes (method 2).

As the paragraph descriping shows that 928025-56-3 is playing an increasingly important role.

Reference：
Patent; UCB PHARMA S.A.; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D; FORD, Daniel James; FRANKLIN, Richard Jeremy; GHAWALKAR, Anant Ramrao; HORSLEY, Helen Tracey; HUANG, Qiuya; REUBERSON, James Thomas; VANDERHOYDONCK, Bart; WO2014/96423; (2014); A1;,
Piperazine – Wikipedia
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59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, This compound was prepared according to the procedure described for the synthesis of Example 187 using methylpiperazin-2-one in place of L-proline-tert-butyl ester. Into a 50-mL round-bottom flask, was placed a solution of (S)-N1-methyl-N1-(2-oxoethyl)-N3-(4-(piperidin-1-yl)-2-(4-(1,2,3,4-tetrahydronaphthalen-1-ylcarbamoyl)pyridin-2-yl)phenyl)isophthalamide (100 mg, 0.16 mmol, 1.00 equiv) in ethanol (2 mL). This was followed by the addition of a solution of 1-methylpiperazin-2-one (18 mg, 0.16 mmol, 1.00 equiv) in ethanol (2 mL), two drop of acetic acid. To this was added NaBH3CN (20 mg, 0.32 mmol, 2.00 equiv). The resulting solution was stirred for 2 h at room temperature. The resulting solution was diluted with 50 mL of ethyl acetate. The resulting mixture was washed with 2*20 mL of brine. The mixture was dried over anhydrous sodium sulfate and concentrated under vacuum. The crude product (100 mg) was purified by Prep-HPLC with the following conditions (1No.-Waters 2767-3): Column, SunFire Prep C18, 19*150 mm 5 um; mobile phase, water with 0.05percent TFA and CH3CN (22percent CH3CN up to 38percent in 6 min); Detector, Waters2545 UvDector 254&270 nm. 70 mg product was obtained. This resulted in 70 mg (61percent) of (S)-N1-methyl-N1-(2-(4-methyl-3-oxopiperazin-1-yl)ethyl)-N3-(4-(piperidin-1-yl)-2-(4-(1,2,3,4-tetrahydronaphthalen-1-ylcarbamoyl)pyridin-2-yl)phenyl)isophthalamide as a yellow solid. LC-MS (ES, m/z): 728 [M+H]+ H-NMR (300 MHz, DMSO, ppm): 12.25 (s, 1H), 9.18 (d, J=8.4 Hz, 1H), 8.80 (d, J=5.1 Hz, 1H), 8.29 (d, J=13.8 Hz 2H), 7.99 (t, J=6.9 Hz, 2H), 7.86 (d, J=4.8 Hz, 1H), 7.57-7.67 (m, 3H), 7.10-7.28 (m, 5H), 5.25 (d, J=5.4 Hz, 1H), 3.92-3.85 (m, 4H), 3.30-3.54 (m, 10H), 2.78-2.95 (m, 9H), 1.99 (d, J=3.6 Hz, 2H), 1.72-1.80 (m, 6H), 1.60 (s, 2H).

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Ardelyx, Inc.; Lewis, Jason G.; Jacobs, Jeffrey W.; Reich, Nicholas; Leadbetter, Michael R.; Bell, Noah; Chang, Han-Ting; Chen, Tao; Navre, Marc; Charmot, Dominique; Carreras, Christopher; Labonte, Eric; (323 pag.)US9301951; (2016); B2;,
Piperazine – Wikipedia
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161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 0.20 mL of 2 N NaOH was added to a solution of 31 (46 mg, 0.10 mmol), prepared in a similar manner as described for 10c, in 2 mL of THF. The resulting medium was refluxed for 5 h. Additional 0.20 mL of 2 N NaOH was added to the reaction solution. Then the reaction was stirred for another 3 h under reflux. After concentration, the remaining residue was acidified to pH 2-3 by adding 1 N HCl and extracted with EA. The organic layer was dried over anhydrous Na2SO4 and concentrated under vacuum to give a crude acid (43 mg). The crude acid was dissolved in 2 mL of DMF and the solution was cooled in an ice bath. To the solution was successively added HATU (0.10 mmol), DIPEA (36 muL, 0.20 mmol) and dimethylamine hydrochloride (10 mg, 0.12 mmol). The resulting medium was stirred at room temperature for 1 h and quenched with 2 mL of saturated NaHCO3. The mixture was extracted with 50 mL of EA. The organic layer was washed with water (2 × 10 mL), brine, dried over anhydrous Na2SO4 and concentrated under vacuum. The crude product was purified by flash column chromatography (0-3% MeOH/EA gradient) to afford compound 10g in 48% yield., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Zhang, Dengyou; Zhang, Xiaowei; Ai, Jing; Zhai, Yun; Liang, Zhongjie; Wang, Ying; Chen, Yi; Li, Chunpu; Zhao, Fei; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6804 – 6820;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 26A (3R)-3-methyl-1-pyridin-2-ylpiperazine (R)-(-)-2-Methylpiperazine (0.50 g, 0.005 mol, Aldrich) and 2-bromopyridine (5 mL, 0.05 mol) were combined and heated at 120° C. for 14 hours. The reaction mixture was allowed to cool to 23° C. and partitioned between a large volume of ethyl acetate and water. The layers were separated, and then additional water was added to the ethyl acetate solution. Drops of 1 N HCl solution were added to the water/ethyl acetate mixture with vigorous mixing. The layers were separated, and the combined aqueous phases were basified to pH ~11 with a solution of saturated sodium bicarbonate and solid sodium carbonate. Sodium chloride was added, and the saturated aqueous solution was extracted with chloroform containing a few drops of isopropyl alcohol (5*). The combined organic extracts were dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure to afford 0.79 g (89percent yield) of the title compound. 1H NMR (400 MHz, DMSO-d6) delta 1.02 (d, J=6.0 Hz, 3H), 2.27 (dd, J=10, 12 Hz, 1), 2.67 (m, 3H), 2.92 (m, 1H), 4.07 (m, 2H), 6.58 (dd, J=6, 8 Hz, 1H), 6.77 (d, J=8 Hz, 1H), 7.49 (m, 1H), 8.08 (m, 1H); MS (ESI) m/e 178 (M+H)+.

75336-86-6, The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Abbott Laboratories; US6960589; (2005); B2;,
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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation of tert-buty 4-(4-(3-(lH-indol-5-yl)-l-tosyl-lH-pyrrolo[2,3-6]pyridin-5- yl)benzyl)-2-methylpiperazi -l-carboxylate[0411] Intermediate 1 (50 mg) was dissolved in anhydrous dichloromethane (3 mL) and treated with 41 mg of tert-butyl 2-methylpiperazine-l-carboxylate. To the resulting solution was added activated 4 A molecular sieves, and the mixture was stirred 2 hrs at room temperature. 33 mg of sodium triacetoxy borohydride was added, and the reaction was stirred overnight, after which it was diluted with dichloromethane, washed with water and brine, and dried over MgS04 to yield the title compound., 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; UNIVERSITY OF ROCHESTER; GELBARD, Harris, A.; DEWHURST, Stephen; GOODFELLOW, Val, S.; WIEMANN, Torsten; RAVULA, Satheesh, Babu; LOWETH, Colin, J.; WO2011/149950; (2011); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Benzyl piperazine-1-carboxylate (1.00 g, 4.54 mmol) and K2CO3 (1.255 g, 9.08 mmol) were dissolved in acetonitrile (12.87 ml) to form a suspension. 1-bromo-2-chloroethane (2.3 ml, 27.24 mmol) was added to the reaction mixture at r.t and the resulting mixture was stirred at this temperature for 96 hours.The reaction mixture was filtered, and the filtrate concentrated under reduced pressure.Purification by column chromatography (ISCO, silica gel column, eluting with 0?100percent EtOAc in hexanes) gave the title compound (0.64 g, yield: 50percent).1H NMR (300 MHz, CHLOROFORM-d) d ppm 7.28-7.43 (m, 5H) 5.15 (s, 2H) 3.48-3.65 (m, 6H) 2.76 (t, 2H) 2.42-2.57 (m, 4H).LCMS: (ESI) m/z 283 [M+H]+.

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; US2012/35134; (2012); 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.1403898-64-5,(2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of (2R ,5R)-5-hydroxymethyl-2-methyl-piperazine- 1 -carboxylic acid tert-butyl ester(which may be prepared as described in Preparation 4) (3.48 g, 15.1 mmol), benzaldehyde(1.76 g, 16.6 mmol), sodium triacetoxyborohydride (3.84 g, 18.1 mmol) and 1,2-dichloroethane(30 mL) was stirred at 20 C for 18 h, then partitioned between saturated aqueous NaHCO3(150 mL) and DCM (3 x 50 mL). Combined organic extracts were dried (Na2SO4) thenevaporated in vacuo to give an oil. Chromatography (Si02, 0 – 30% EtOAc in petrol) gave the title compound (4.588 g, 74%) as a colourless solid. MS: [M+H] = 321., 1403898-64-5

As the paragraph descriping shows that 1403898-64-5 is playing an increasingly important role.

Reference：
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; HOWARD, Steven; DAY, James Edward Harvey; BUCK, Ildiko Maria; GRIFFITHS-JONES, Charlotte Mary; SAXTY, Gordon; TAMANINI, Emiliano; WILSHER, Nicola Elisabeth; WO2015/92420; (2015); 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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

694499-26-8, 3-Iodo-4-methy1-N-(4-((4-methy1piperazin-1-y1)methy1)-3-(trfluoromethy1)pheny1)Benzamide: 3-Iodo-4-methylbenzoyl chloride (0.48 g, 1.7 mmol), prepared from the reaction of3-iodo-4-methylbenzoic acid and SOCI2 (as previously described), was added to a solution of 4-((4-methylpiperazin-1 -yl)methyl)-3-(trifluoromethyl)aniline (0.47 g, 1.7 mmol), N,N5 diisopropylethylamine (0.26 g, 2.0 mmol), and a catalytic amount of DMAP in THF (10 mL).After stirring at rt for 2 h, the reaction was quenched with water. EtOAc was added and the layers separated. The combined organic layers were concentrated to dryness and purified by silica gel chromatography (eluted with 5% MeOH/DCM, MeOH was pre-saturated with ammonia gas), to provide 0.51 g of product as an off-white solid.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ARIAD PHARMACEUTICALS, INC.; GOZGIT, Joseph, M.; RIVERA, Victor, M.; SHAKESPEARE, William, C.; ZHU, Xiaotian; DALGARNO, David, C.; WO2013/162727; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3 (General procedure A); 2-(4-Cyclopropylpiperazin-1-yl)-6-methoxybenzothiazole, hydrochloride; A mixture of 2-chloro-6-methoxybenzothiazole (0.20 g, 1.0 mmol) and 1-cyclopropyl- piperazine (0.25 g, 2.0 mmol) was stirred at 120 0C overnight. The reaction mixture was allowed to cool and dissolved in a mixture of ethyl acetate a NaHCO3 solution. The phases were separated and the organic phase was washed with water (3 x) and then extracted with 0.25 M hydrochloric acid (20 ml_). The acidic aqueous extract was concentrated and re- evaporated with ethanol. The residue was crystallized from a mixture of ethanol and ethyl acetate to give 60 mg (18 %) of 2-(4-cyclopropylpiperazin-1-yl)-6-methoxybenzothiazole, hydrochloride. 1H-NMR (400MHz, DMSO-d6) delta 11.3 (brs, 1 H), 7.48 (d, 1 H), 7.45 (d, 1 H), 6.93 (dd, 1 H), 4.18-4.06 (m, 2H), 3.89-3.75 (m, 5H), 3.68-3.52 (m, 2H), 3.44-3.33 (m, 2H), 2.94-2.86 (m, 1 H), 1.21-1.15 (m, 2H), 0.85-0.79 (m, 2H).

20327-23-5, 20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NOVO NORDISK A/S; WO2007/110364; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

General procedure: 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoic acid (5) was synthesized by the method reported. [Nat Med. 2013, 19(2): 202-8] To a solution of compound 5 (100 mg, 0.175 mmol) in anhydrous dichloromethane, compound 4g (68 mg, 0.175 mmol), EDCI (167 mg, 0.875 mmol) and DMAP (25.6 mg, 0.21 mmol) were added. Afterwards, the mixture solution was stirred for 24 h at room temperature. Completion of the reaction was confirmed by TCL. The reaction mixture was washed with HCl (1 M), NaHCO3 saturated solution and brine, concentrated and purified to afford 6g (160 mg, 85% yield) as a yellow solid.

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

Reference：
Article; Zhou, Ruolan; Fang, Shaoyu; Zhang, Minmin; Zhang, Qingsen; Hu, Jian; Wang, Mingping; Wang, Chongqing; Zhu, Ju; Shen, Aijun; Chen, Xin; Zheng, Canhui; Bioorganic and Medicinal Chemistry Letters; vol. 29; 3; (2019); p. 349 – 352;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics