Heterocyclic Building Blocks-piperazine

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

In a sealed tube, 7-fluoro-9-methyl-2-(2-methylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one (Intermediate 3; 250 mg, 0.808 mmol), and (S)-2-methylpiperazine (405 mg, 4.04 mmol, 5.0 eq.) were stirred in DMSO (6 mL) and heated at 130 C. overnight. The solvent was removed under high vacuum. The residue was taken up in CH2Cl2 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2SO4 and concentrated in vacuo. The crude was purified by column chromatography (SiO2, CH2Cl2/MeOH=95/5 to 85/15) to afford the title product (135 mg, 43%) as a light yellow solid. MS m/z 390.3 [M+H+].

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Hoffmann-La Roche Inc.; PTC Therapeutics, Inc.; Ratni, Hasane; Green, Luke; Weetall, Maria L.; Naryshkin, Nikolai A.; (33 pag.)US2019/315773; (2019); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.,5308-25-8

a) Ethyl 2-(4-ethylpiperazin-l-yl)acetateTo a solution of 1 -ethylpiperazine (1 g, 8.771 mmol, 1.0 eq) in DMF were added K2C03 (3 g, 21.927 mmol, 2.5 eq.) and ethyl 2-bromoacetate (2.19 g, 13.156 mmol, 1.5 eq.). The mixture was stirred at RT for 16 h. The mixture was quenched and extracted as in Intermediate Example 5(a). The solvent was distilled off to afford the product in 76.4 % yield (1.3g).

As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference£º
Patent; ORION CORPORATION; LINNANEN, Tero; WOHLFAHRT, Gerd; NANDURI, Srinivas; UJJINAMATADA, Ravi; RAJAGOPALAN, Srinivasan; MUKHERJEE, Subhendu; WO2013/53983; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics

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

4-Methanesulfonyl-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 10 mmol of Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester were dissolved in 20 ml methylenchloride. 1.05 eq of DIPEA and mesylchloride were added. The reaction mixture was stirred at room temperature for 30 min. The product was extracted from etylacetate/water. The crude material was redissolved in methanol and treated with 2N NaOH. The reaction mixture was stirred at room temperature for 2 h. The mixture was neutralized with HCl and the product isolated via extraction from ethylacetate/water. MS(ISO): 307.4 (M-H+), 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; Ackermann, Jean; Bleicher, Konrad; Ceccarelli Grenz, Simona M.; Chomienne, Odile; Mattei, Patrizio; Schulz-Gasch, Tanja; US2007/129544; (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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, Cyclopropanoyl chloride (112 muL) was added to a mixture of N-tert-butoxycarbonylpiperazine (200 mg) and an excess of potassium carbonate in anhydrous DCM (10 mL) under a nitrogen atmosphere. The mixture was stirred at r.t. for 18 hours, then it was filtered off from inorganics. The organic phase was diluted with Et2O (20 mL) and washed with 1N hydrochloric acid solution (10 mL). The aqueous phase was made basic with 1N sodium hydroxide solution and extracted twice with DCM. The combined organic layers were dried and concentrated in vacuo to give the title compound (210 mg) as an oil. [0238] T.I.c.: AcOEt, Rf=0.45. [0239] NMR (d6-DMSO): 6 (ppm) 3.64-3.28 (m, 8H); 1.94 (m, 1H); 1.4 (s, 9H); 0.7 (m, 4H). [0240] MS (ES/+): m/z=255 [M+H]+.

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Alvaro, Giuseppe; Di Fabio, Romano; Maragni, Paolo; Tampieri, Marsia; Tranquillini, Maria Elvira; US2004/14770; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,55121-99-8

KOtBu (2.81 g, 25.08 mmol) was dissolved in 20 ml DMSO in a round bottom flask. (4-aminophenyl)(4-methylpiperazin-1-yl)methanone (5.0 g, 22.80 mmol) in 30 ml DMSO was added and the resulting mixture was stirred for 15 minutes at r.t. The mixture was cooled in an iced bath for 5 minutes. 5-bromo-2- fluorobenzonitrile (4.6 g, 23.00 mmol) in 20 ml DMSO was added. The ice bath was removed and the mixture stirred for 5 hours while warming to room temperature. Additional KOtBu (2g, 17.82 mmol) was added and the mixture stirred at room temperature overnight. The mixture was diluted with dichloromethane, extracted twice with water, once with brine, then dried over MgSO4, filtered and concentrated. 8.8 g crude brown oil were isolated. The crude product was recrystallized from dichloromethane + ethyl acetate + hexanes. 5.012 g pale yellow crystals were collected by filtration. The mother liquor was concentrated and purified by chromatography on silica, using a gradient from 100% Solvent A to 50% Solvent A+50% Solvent B. Solvent A: 99% dichloromethane + 1% Triethylamine, Solvent B: 99% Ethylacetate + 1% Triethylamine. Evaporation of product containing fractions gave additional 1.8 g product of -70% purity. MS (ESI) m/z 399/401(M+H). 1H NMR (CDCl3) delta ppm 7.63 (s, 1 H), 7.48 (d, 1H, J= 9.2), 7.42 (d, 2 H, J= 7.9), 7.18- 7.14 (m, 3H), 6.41 (s, 1 H), 3.80-3.40 (bm, 4 H), 2.42 (bs, 4H), 2.32 (s, 3H).

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; PURANDARE, Ashok, Vinayak; BATT, Douglas, G.; LIU, Qingjie; JOHNSON, Walter, L.; MASTALERZ, Harold; ZHANG, Guifen; ZIMMERMANN, Kurt; WO2010/80474; (2010); A1;,
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Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Fluoro-2-methoxy-1-nitrobenzene (2.55 g, 14.9 mmol),N-acetylpiperazine (1.91 g, 14.9 mmol),Potassium carbonate (2.47 g, 17.9 mmol)Was added to N, N-dimethylacetamide (25 mL).The reaction was heated to 120 C for 5 hours. Ethyl acetate (50 mL) was added and the mixture was washed with saturated brine (50 mL). The organic layer was dried, dried and column chromatographed (petroleum ether: ethyl acetate = 5: 1) to give the product as a white solid (1.87 g, yield 45.0 %).

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference£º
Patent; Shandong Xuanzhu Pharmaceutical Technology Co., Ltd; Wu, Yongqian; (68 pag.)CN105884695; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Sodium hydride (0.86 g, 21 mmol) was added to fert-butyl (3S)-3-(hydroxymethyl)piperazine-l-carboxylate (1.244 g, 5.75 mmol) in THF (40 ml) at rt. The resulting mixture was stirred at rt for 10 min. 7-Bromo-8-chloro-5,6-difluoroquinazolin-4-ol (1.7 g, 5.75 mmol) was added slowly and the resulting solution was stirred at 40C for 1 h. The reaction mixture was quenched with water (2 ml). The reaction mixture was adjusted to pH = 7 with 2M HCI. The crude product was purified by C18-flash chromatography (0 to 65% MeOH in water (0.1% TFA)) to afford ferf-butyl (3S)-3-{[(7-bromo-8-chloro-6-fluoro-4-hydroxyquinazolin-5-yl)oxy]methyl}piperazine-l-carboxylate (1.65 g, 58%) as a brown solid. XH NMR (400 MHz, DMSO) 1.35 (9H, s), 2.62-3.07 (2H, m), 3.11-3.19 (2H, m), 3.20-3.76 (1H, m), 3.80-3.88 (1H, m), 3.98-4.29 (3H, m), 8.23 (1H, s). m/z: ES+ [M+H]+ = 491., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl cis-3,5-dimethylpiperazine-1-carboxylate (Combi-Blocks Inc., San Diego, Calif., USA, 130 g, 580 mmol, 1.0 equiv) and triethylamine (100 mL, 700 mmol, 1.2 equiv) in tetrahydrofuran (1250 mL, 10 mL/g) was added acryloyl chloride (56 mL, 700 mmol, 1.2 equiv) at 0 C. The reaction mixture was stirred for 1 h at 0 C. The reaction mixture was diluted with ethyl acetate (2.0 L) and washed with water (2*500 mL). The organic layer was washed with 1 N aqueous HCl (500 mL), saturated NaHCO3 (500 mL), and brine (500 mL). The organic layer was dried over sodium sulfate, filtered, and concentrated in vacuo. The crude material was adsorbed to a plug of silica gel and purified by silica gel column chromatography (30-40% EtOAc/hexane) to provide the title compound as off-white solid (140 g, 91%). MS (ESI, +ve ion) m/z: 269.0 [M+1]; 1H NMR (400 MHz, DMSO-d6) delta 6.78-6.72 (ddd, J=16.7, 10.4, 1.5 Hz, 1H), 6.15-6.11 (dt, J=16.6, 1.9 Hz, 1H), 5.70-5.67 (dt, J=10.6, 1.9 Hz, 1H), 4.35-4.25 (m, 2H), 3.82 (d, J=12.5 Hz, 2H), 3.01-2.95 (m, 2H), 1.43-1.42 (d, J=1.6 Hz, 9H), 1.19-1.14 (m, 6H).

129779-30-2, 129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Amgen Inc.; ALLEN, John Gordon; LANMAN, Brian Alan; CHEN, Jian; REED, Anthony B.; CEE, Victor J.; LIU, Longbin; LOPEZ, Patricia; WURZ, Ryan Paul; NGUYEN, Thomas T.; Booker, Shon; ALLEN, Jennifer Rebecca; CHU-MOYER, Margaret; AMEGADZIE, Albert; CHEN, Ning; GOODMAN, Clifford; LOW, Jonathan D.; MA, Vu Van; MINATTI, Ana Elena; NISHIMURA, Nobuko; PICKRELL, Alexander J.; WANG, Hui-Ling; SHIN, Youngsook; SIEGMUND, Aaron C.; YANG, Kevin C.; TAMAYO, Nuria A.; WALTON, Mary; XUE, Qiufen; US2019/374542; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

169447-70-5, Preparation 15 (S)-tert-Butyl 4-(4-chlorophthalazin-1-yl)-2-methylpiperazine-1-carboxylate Heat a mixture of 1,4-dichlorophthalazine (7.80 g, 39.2 mmol), (S)-tert-butyl 2-methylpiperazine-1-carboxylate (4.98 g, 24.9 mmol) and triethylamine (10.3 mL, 73.9 mmol) in DMSO (110 mL) at 80 C. for 18 h. Pour the reaction mixture into water, rinsing with EtOAc. Extract with EtOAc. Wash the organic layer with water (2*) and brine, and dry over Na2SO4, and concentrate under reduced pressure. Purify the resulting residue by flash silica gel chromatography (gradient of 20% to 80% EtOAc in hexanes) to provide the title compound (4.13 g, 46%). ES/MS m/z (35Cl) 363.0 (M+1).

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ELI LILLY AND COMPANY; US2011/190304; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5317-33-9, 3-(4-Methylpiperazin-1-yl)propan-1-ol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2.94 g (19 mmol) of 3-(N-methylpiperazine)propan-1-ol and 2.63 g (24.8 mmol) of sodium carbonate are added to a solution of 5.68 g (12.4 mmol) of 2,2,2-trichloro-N-{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}acetamide in 25 ml of dimethylformamide, and the mixture is stirred at 100 C. for 20 hours. 50 ml of water are added to the reaction mixture, which is then extracted with dichloromethane. The organic phase is dried over sodium sulfate and evaporated. The residue is chromatographed on a silica-gel column with dichloromethane/methanol as eluent: 3-(4-methylpiperazin-1-yl)propyl{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}carbamate as colourless crystals.

5317-33-9, 5317-33-9 3-(4-Methylpiperazin-1-yl)propan-1-ol 79208, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK PATENT GESELLSCHAFT MIT BESCHRAeNKTER HAFTUNG; US2011/136819; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics