Heterocyclic Building Blocks-piperazine

25057-77-6, 1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,25057-77-6

A mixture of 4-(9-(4-fluorophenyl)-3-oxo-3,7,8,9-tetrahydro-2H-pyrido[4,3,2-de]phthalazin-8-yl)benzaldehyde (200 mg, 0.52 mmol), 1,2-dimethylpiperazine (311 mg, 1.56 mmol) in methylene chloride (10 mL) was stirred at room temperature overnight, then NaBCNH3 (129 mg, 2.08 mmole) was added and the mixture was stirred for another 5 hours. After removal of solvents, the residue was purified by column chromatography (silica gel, petroleum ether/ethyl acetate=3:1 to 1:1) to give the title compound (70 mg, 26%). LC-MS (ESI) m/z: 484 (M+1)+. 1H-NMR (400 MHz, CDCl3) delta (ppm): 1.43 (d, J=5.2 Hz, 3H), 2.84 (s, 3H), 3.29 (m, 1H), 3.33-3.44 (m, 6H), 4.03 (s, 2H), 4.22 (m, 1H), 4.65 (m, 1H), 6.91 (m, 1H), 6.97 (m, 1H), 7.00 (d, J=8 Hz, 2H), 7.23-7.37 (m, 4H), 7.65 (m, 1H), 7.77 (d, J=7.2 Hz, 1H), 9.92 (s, 1H).

The synthetic route of 25057-77-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Compound P42: 5-(Morpholin-4-yl)-2-nitroaniline To the flask 2-amino-3-nitro-6-chloropyridine (1.50 g, 8.47 mmol), potassium carbonate (1.30 g, 9.32 mmol) and morpholine (10.5 ml, 119 mmol) were added. The reaction was carried out under argon flow at 130°C overnight. The progress of the reaction was monitored by TLC (system: heptane/ethyl acetate, 1 /1 ). The mixture was cooled to room temperature and poured into the ice-water. A precipitated yellow solid was filtered and dried. 1.789 g of the title product were obtained (yield 94.2percent). Compound P48: 5-[(3R,5S)-3,5-dimethylpiperazin-1 -yl]-2-nitroaniline; The compound was obtained by the method analogous to that described for Compound P42. Starting from 5-chloro-2-nitroaniline (0.800 g, 4.64 mmol), potassium carbonate (0.705 g, 5.10 mmol) and cis-2,6-dimethylpiperazine (1.620 g, 13.9 mmol) in 5 ml of DMF, 1.144 g of the title product in the form of a yellow solid were obtained (yield 98.6percent). MS-ESI: (m/z) calculated for C12H19N4O2 [ + H]+: 251.15, found 251.1.

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

Reference：
Patent; CELON PHARMA S.A.; ZDZALIK, Daria; LIPNER, Joanna; WIECZOREK, Maciej; DZWONEK, Karolina; YAMANI, Abdellah; DUBIEL, Krzysztof; LAMPARSKA-PRZYBYSZ, Monika; GRYGIELEWICZ, Paulina; STANCZAK, Aleksandra; WO2014/141015; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.509073-62-5,tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,509073-62-5

Step b – terf-butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate; A solution of tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate (1.0Og, 3.00mmol) in MeOH (60ml) was hydrogenated at 2O0C at atmospheric pressure using an H-Cube (flow rate at 1 ml/min and full hydrogen mode) using a Pd/C cartridge. The solvent was removed in vacuo Xo afford te/f-butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate (0.85g, 2.79mmol, 93%) as a white solid. 1H NMR (CDCI3) delta 1.41 (9H, s), 3.38 (4H, m), 3.53 (4H, m), 4.07 (2H, br. s), 6.55 (2H, d), 7.17 (2H, d). LCMS (2) Rt: 2.14min; m/z (ES+) 306.

The synthetic route of 509073-62-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SAREUM LIMITED; WO2008/139161; (2008); 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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

The 100 mg compound II, 75 mg compound III by adding 5 ml dichloromethane (DCM) in, stirring, 40 C reaction 2 hours, TLC monitoring, after the reaction, the solvent turns on lathe does, the reactant putting into the 100 ml water, ethyl acetate (20 ml × 3) extraction, standing liquid, organic phase are respectively 5% of NaHCO3 (20 Ml × 3), saturated salt water (20 ml × 3) washing, then drying water-free magnesium sulfate, filtered, reduced pressure to remove the ethyl acetate to get the yellow oily compound IV 83 mg.

20327-23-5, The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Southern Medical University; Chen Jianjun; Cheng Binbin; (22 pag.)CN109456284; (2019); A;,
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Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In N2 Under protection, three-necked flask with stirring and the funnel was added dropwise 150ml of n-hexane and isopropyl piperazine 100mmol, under ice-cooling, and the dropping funnel was slowly added dropwise 100mmol n-butyllithium, was added dropwise after the reaction warmed to room temperature after 2h.50mmol tetramethoxysilane was added dropwise under ice-cooling and reacted at room temperature after the completion of the dropwise addition 8h, and finally through G4Funnel, the solid residue was washed repeatedly with tetrahydrofuran and filtered, the filtrate was collected.Distilled off on a rotary evaporator, tetrahydrofuran solvent, vacuum distillation, collecting 144 ~ 147°C / 100pa fraction.Vacuum distillation, collecting 144 ~ 147°C / 100pa distillate, heavy 5.5g, 98.8percent yield,

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Institute of Chemistry Chinese Academy of Sciences; Li, Huayi; Chang, Hefei; Zhang, Liaoyun; Hu, Youliang; (19 pag.)CN102977133; (2016); B;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To compound 4 (183mg , 0.8 mmol) in DCM (3 ml), was added DIPEA ( 0.278 ml, 2 eq) and then propionyl chloride (130mg, 1 mmol) . The reaction was stirred at room temperature for lhr. The mixture was concentrated and partitioned between ethyl acetate and water, ethyl acetate layer was separated and dried, concentrated, then HC1 in dioxane ( 4N, 2 ml) was added. The mixture was stirred at room temperature for lhr, concentrated to afford crude 5a. It was then diluted with dry DMF ( 5 ml), was added, followed by addition of DIPEA (0.278ml, 1.6 mmol) and then (Biotin-LC-LC-NHS ( 454mg, O.Smmol). The mixture was stirred at room temperature for 12 hrs. The mixture was diluted with water, extracted with ethyl acetate. The organics were concentrated and then purified by HPLC to yield the desired product 6a ( 390 mg). NMR: pass, 192130-34-0

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NESTEC S.A.; SELVARAJ, Fabiyola; PRINCEN, Fred; SINGH, Sharat; WO2014/188377; (2014); 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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

General procedure: To a solution of9(0.16g,0.58mmol) ini-PrOH(5mL),substituted phenylamine(0.64mmol)wasadded. The reaction mixture was stirred at reflux for4h under N2atmosphere. After the reaction was completed, the mixture wasnaturally cooled to room temperature.Themixture was filtered and the solid was collectedto giveintermediate12or15. 1.2.1 (4-((6-Bromoquinazolin-4-yl)amino)phenyl)(4-methylpiperazin-1-yl)methanone (12a)Yellow solid; yield:73 %.MS (ESI)m/z: [M+H]+=426.1/428.1.

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

Reference：
Article; Xin, Minhang; Hei, Yuan-Yuan; Zhang, Hao; Shen, Ying; Zhang, San-Qi; Bioorganic and Medicinal Chemistry Letters; vol. 27; 9; (2017); p. 1972 – 1977;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.112984-60-8,6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Synthesis of 6-Ffuoro-7-{4-[5-hydroxy-6-(2-methyl-5-nitro- imidazoi-I-yi)-hexyl]-piperazin-I-yi}-l -methyS-4-oxo-4H-2-thia-8b-aza- cyclobu a[a]naphthaSene-3-carboxylic acid (1 15): To a stin-ed solution of 6- Fluoro- 1 -methy-4-oxQ-7-piperazin- 1 -yl-4H-2-thia-8P-aza- cyclobuta[a]naphthalene-3-carboxylic acid, (HI) ( 1 .10 g, 3.16 mmol) in dimethylformamide (30ml) was added potassium carbonate (0.43g, 3.16 mmol) followed by addition of compound (II) (0.85g, 2.63 mmol) and the reaction 1 26 mixture was stirred at RT for 1 6h. The reaction mixture was diluted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while euting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (115) with 20% isolated yield. 1 H-NMR (400 MHz, DMSO) delta ppm: 1 .61 – 1 -68(6H, m, CH2), 2.1 (3H, d, J = 6 Hz, CH3), 2.44 (3H, s, CH3) , 2.54 (4H, m, 2 xCH2), 3.2 (4H, m, 2 xCH2), 3.9-4. 1 (2H. m, 2 x CH2N), 4.38( 1 H, d, J = 14, CHOH). 5.2 1 1 H, d, J = 4.4, OH), 6.38 ( 1 H, d, J = 5.6Hz, CHSN) 6.9 ( 1 H, d, J = 6.8, Ar-H). 7.78 ( 1 H, d, J = 1 4 Hz, Ar-H). 8.02 ( 1 H, s, Ar-H). ESI-MS (m/z): 575(M+H)

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-METHYLPIPERAZINE-1-CARBOXYLIC acid test-butyl ester (160 mg; 0.80 MMOL ; 2 eq.) (prepared as reported in J. Med. Chem. 1993,36, 690-698), cesium carbonate (195 mg; 0.6 MMOL ; 1.5 eq. ), palladium acetate (9 mg; 0.04 MMOL ; 0.10 eq. ) and 2,2′- bis (diphenylphosphino)-1, 1′-binaphthyl (38 mg; 0.06 MMOL ; 0.15 eq. ) were added to a solution of 2-METHYLQUINOLIN-5-YL-TRIFLUOROMETHANESULFONATE (D1) (117 mg, 0.4 MMOL ; 1 eq) in dry toluene (2.5 mL) under nitrogen. The reaction mixture was stirred at reflux under nitrogen for 10 h. The reaction was cooled and filtered through a pad of celite which was then washed with DCM (50 mL). The filtrates was concentrated in vacuo and the crude product was purified by SPE cartridge (Si, 2g), eluting with 5percent ethylacetate in cyclohexane to afford 3-methyl-4-(2-methylquinolin-5-yl)piperazin-1- carboxylic acid tert-butyl ester as a yellow oil (84 mg; yield 62percent). MS; (ES) m/z: 341.45 [MH] +. C2OH27N302 requires 342. 4.APOS;H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.8-3. 6, m/m, 2H), 3. 4- 3. 3 (m, 1 H), 3. 2- 3. 1 (m, 1 H), 3.1-2. 9 (m, 2H), 2.74 (s, 3 H), 1.45 (s, 9H), 1.36 (d, 3H). This compound (84 mg) was dissolved in a mixture 3: 1 of trifluoroacetic acid: DCM (4 mL) and stirred at r. T. for 6h. The solvent was evaporated in vacuo and the residue purified on SCX cartridge (1G) to afford the title compound (D14) (44 mg; yield 76percent) MS; (ES) m/z: 241.45 [MH] +. C15H19N3 requires 242.4. 1H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.3 (m, 4H), 3.15 (m, 4 H), 2.74 (s, 3 H), 1.9 (m, 2H)., 120737-59-9

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

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/46124; (2004); 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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A mixture of acetoxymethyl 4-nitrophenyl carbonate (1 mmol) and PDBTZ (1 mmol) in hexamethylphosphoramide (1.3 mL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide title compound., 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics