Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

a) 1,4-Bis(tert-butoxycarbonyl)-2-piperazinecarboxylic acid To a solution of piperazine-2-carboxylic acid dihydrochloride (5 g, 24.6 mmol) in 2M sodium hydroxide (40 mL) and ethanol (40 mL) was added di-tert-butyl dicarbonate (11.82 g, 54.1 mmol) and the reaction mixture stirred for 3 days. The organic solvent was removed in vacuo, the aqueous phase basified with 2M sodium hydroxide and extracted with diethyl ether to remove excess di-tert-butyl dicarbonate. The aqueous layer was adjusted to pH 3-4 and extracted with ethyl acetate. The combined organic extracts were dried (MgSO4), filtered and evaporated to yield 1,4-bis(tert-butoxycarbonyl)-2-piperazinecarboxylic acid as a white solid., 3022-15-9

As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference：
Patent; Agejas-Chicharro, Javier; Belen Bueno Melendo, Ana; Camp, Nicholas Paul; Gilmore, Jeremy; Jimenez-Aguado, Alma Maria; Lamas-Peteira, Carlos; Marcos-Llorente, Alicia; Mazanetz, Michael Philip; Montero Salgado, Carlos; Timms, Graham Henry; Williams, Andrew Caerwyn; US2004/122001; (2004); A1;,
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76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 27 (4.0 g, 20 mmol) in dichloromethane (50 mL) is added 28 (4.6 g, 24 mmol) at 25 C and then the reaction mixture is stirred at 25 C for 4 hours. The reaction mixture is concentrated under reduced pressure to give a residue 17 (5.0 g, crude) as yellow oil and used for the next without further processing., 76003-29-7

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BIOVERSYS AG; BHATTACHARJEE, Ashoke; CHOWDHURY, Somenath; DUFFY, Erin, M.; IPPOLITO, Joseph, A.; KANYO, Zoltan, F.; LAU, Wan; TANG, Yuanqing; WU, Yusheng; (0 pag.)WO2019/234509; (2019); 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.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 106; Synthesis of 1,1-dimethylethyl 4-(2-{[(5-{[(5-bromo-2- methyIphenyl)amino]carbonyl}-lH-imidazol-4-yl)carbonyl]amino}-lH-benzimidazol-6-yl)-3-methylpiperazine-l-carboxylate; Synthesis of terf-Butyl 4-(3,4-dinitrophenyl)-3-methylpiperazine-l-carboxylate; [00350] 4-Fluoro-l,2-dinitrobenzene (0.93g, 5.0 mmol, commercially available from Oakwood Products) and rert-butyl 3-methylpiperazine-l-carboxylate (l.Og, 5.0 mmol) were dissolved in 3 mL of DMA, and 3 mL of diisopropylethylamine was added. The mixture was stirred at 50 0C overnight, and then cooled to room temperature, separated between ethyl acetate and water. The combined organic were washed with water, brine, dried with anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. The residue was separated by silica gel column (20percent to 40percent ethyl acetate in hexanes) to give 1.0 g of 4-(3,4- dinitrophenyl)-3-methylpiperazine-l-carboxylate. 1H-NMR (400 MHz, CDCl3): delta 8.05 (d, 2H), 6.84 (m, 2H), 3.90-4.10 (m, 3H), 3.05-3.60 (m, 4H), 1.50 (s, 9H), 1.10 (s, 3H). MS (EI): 367 (MH+).

120737-59-9, The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; EXELIXIS, INC.; WO2008/42282; (2008); A2;,
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Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A – Preparation of Int 44-1 Int 44-1 To a solution of 1-tert-butyl 3-methyl piperazine-l,3-dicarboxylate (2.44 g, 10 mmol) in DCM (50 mL) was added phenylboronic acid (2.35 g, 20 mmol), Cu(OAc)2 (1.82 g, 10 mmol) and pyridine (1.58 g, 20 mmol) in turns with stirring. The reaction mixture was stirred at ambient temperature for 24 hrs under an oxygen atmosphere. The reaction mixture was filtered and filtrate was concentrated. The residue was purified by column chromatography on silica gel (petroleum ether : EtOAc= 3: 1) to afford compound Int 44-1 (2.74 g). MS-ESI (m/z): 321 (M+l)+ R 0.3 (PE : EtOAc= 3 : 1)., 129799-08-2

As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; COBURN, Craig, A.; MALETIC, Milana, M.; LUO, Yunfu; QI, Zhiqi; YU, Tingting; SOLL, Richard; WO2015/73310; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.,21655-48-1

[5013] A solution of (2S,6R)-2,6-dimethylpiperazine (10.000 g, 87.573 mmol) and tri- ethylamine ( 18.309 mL, 131.360 mmol) in dichloromethane (300 inL) was mixed at 0 °C with benzyl chloroformate ( 13.752 mL, 96.331 mmol) and stirred at the same temperature for 2 hr. Then, saturated aqueous potassium bicarbonate solution was added to the reaction mixture, followed by extraction with dichloromethane. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous MgS0 , filtered, and concentrated in vacuo. Benzyl (3S,5R)-3,5-dimethylpiperazine- l -carboxylate was used without further purification ( 1 1.000 g, 50.6 percent, pale yellow oil).

21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; KIM, Yuntae; LEE, Chang Sik; SONG, Hyeseung; GWAK, Dal-Yong; LEE, Jaeyoung; OH, Jung Taek; LEE, Chang Gon; KIM, II Hyang; (1041 pag.)WO2017/23133; (2017); A2;,
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Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 95: l-Methyl-4-[4-(methylsuIfonylmethyl)-6-morpholin-4-yl-pyrimidin-2-yl]piperazin-2- oneA mixture of 2-chloro-4-(methylsulfonylmethyl)-6-morpholin-4-yl-pyrimidine (200 mg), l-methylpiperazin-2-one (157 mg) and sodium carbonate (146 mg) in DMA (4 mL) was heated in a microwave reactor at 16O0C for 10 minutes. The reaction mixture was loaded onto a SCX-2 column and product removed with 7N ammonia in methanol. The solution was evaporated to dryness and chromatographed on silica, eluting with 0 – 2.5percent methanol in DCM, to give the desired material (179 mg) as a white solid. Mass Spectrum; MH+ 370NMR Spectrum: 1H NMR (DMSOd6) 52.89 (3H, s), 3.13 (3H, s), 3.38 (2H, t), 3.55 – 3.56 (4H, m), 3.67 – 3.68 (4H, m), 3.93 (2H, t), 4.19 (2H, s), 4.28 (2H, s), 6.28 (IH, s)

59702-07-7, As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/80382; (2007); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 8Synthesis of [F- 18]- 1 -methyl- l-(4-fluorophenyl)piperazinium saltt-BOC-Protected methylpiperizine was heated in the presence of l-fluoro-4- nitrobenzene under pressure in benzene to give 4-t-BOC-protected 1 -methyl- 1 -(4- nitrophenyl)piperazinium salt. The piperazinium salt was heated in the presence of potassium [18F]fluoride and Krytofx at 2000C for 10 minutes. The oil was treated with aq. 3 M HCl for 20 minutes to give [F-18]- 1 -methyl- l-(4-fluorophenyl)piperazinium chloride., 109-01-3

109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; THE GENERAL HOSPITAL CORPORATION; WO2008/22319; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,13754-38-6

General procedure: A solution of 2-chloroalkyl/aryl substitutedwith or without N-substitution as well as with or without 5 and/or 6-substituted benzimidazole derivative (1.75g,0.01051mol) and 1-[(4-phenyl)carbonyl]piperazine (3g,0.0105mol) in N, N dimethylformamide was taken in a RBF.K2CO3(2gm,) was added to the reaction mixture. The reaction mixture was stirred for 8h at 80C on a magnetic stirrer (heat + stirring). The progress of the reaction was monitored by thin layer chromatography (TLC).Upon completion of the reaction, water was added to the reaction mixture and the product extracted by shaking the reaction mixture with dichloromethane in a separating funnel.The dichloromethane layer was washed successively with water and brine, dried over anhydrous sodium sulfate. Evaporation of the solvent gave theproduct. 11a-l Recrystallized with various solvent like chloroform, ethanol, methanol.

As the paragraph descriping shows that 13754-38-6 is playing an increasingly important role.

Reference：
Article; Kankate, Rani S.; Gide, Parag S.; Belsare, Deepak P.; Oriental Journal of Chemistry; vol. 30; 4; (2014); p. 1855 – 1863;,
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.304897-49-2,tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1. Preparation of tert-Butyl 4-(4-(4-bromobenzamido)benzyl)piperazine-1-carboxylate (3) 4-Bromobenzoic acid (1, 685.0 mg, 3.4 mmol) and HATU (1298.1 mg, 3.4 mmol) are partially dissolved in DMF (10 mL) at rt. DIEA (560 muL, 3.4 mmol) is added to this mixture to give a pale yellow solution. After stirring at rt for 30 min, tert-butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (2, 992.9 mg, 3.4 mmol) is added and the resulting reaction mixture is heated at 60 C. for 20 h, allowed to cool to rt, and poured into water (100 mL). This mixture is extracted with Et2O (3*150 mL). The combined organic extracts are evaporated to dryness to give a white solid, which is washed with water (50 mL) and dried in vacuo. This material is used in the next synthetic step without further purification. HPLC: tR 1.67 min (method 1). LC-MS m/z calcd for C23H2879BrN3O3 ([M]+), 473. found, 474 ([M+H]+). 1H NMR (CD3OD): delta 1.46 (s, 9H), 2.96 (m, 4H), 3.59 (m, 4H), 4.05 (br s, 2H), 7.46 (m, 2H), 7.69 (m, 2H), 7.78 (m, 2H), 7.85 (m, 2H).

304897-49-2, The synthetic route of 304897-49-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ACHILLION PHARMACEUTICALS, INC.; Wiles, Jason Allan; Gadhachanda, Venkat; Chen, Dawei; Wang, Qiuping; Hashimoto, Akihiro; Pais, Godwin; Wang, Xiangzhu; Deshpande, Milind; Phadke, Avinash; US9125904; (2015); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0384] To a solution of l-Boc-4-(2-chloroethyl)piperazine (6.85 g, 27.62 mmol) in methanol (50 ml) was added thiourea (4.12 g, 55.24 mmol). The mixture was heated to reflux for 2 hours. A solution of sodium hydroxide (1.66 g, 41.43 mmol) in water (10 ml) was added, and the mixture was continued to reflux for another hour. Then most solvent was evaporated under reduced pressure. The residue was mixed with ethyl acetate (50 ml) and brine (30 ml) and separated. The ethyl acetate was dried over magnesium sulfate and evaporated under reduced pressure. The residue was dissolved in methanol (20 ml). 4 M hydrochloric acid in dioxane (10 ml) was added. The mixture was stirred at room temperature overnight and most of solvent was evaporated under reduced pressure. The residue was used for the addition reaction without further purification.

208167-83-3, The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SU, Zhuang; LONG, Zhengyu; YANG, Suizhou; WO2014/145686; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics