Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

[Referential Example 16] 1-Methylpiperazin-2-one trifluoroacetic acid salt 4-Methyl-3-oxopiperazine-1-carboxylic acid tert-butyl ester (0.308 g) obtained in step 2) of Referential Example 15 was dissolved in dichloromethane (6 mL). Trifluoroacetic acid (3 mL) was added to the resultant mixture at room temperature, followed by stirring for 1.5 hours. The reaction solvent was evaporated under reduced pressure, and the residue was dried, to thereby give the title compound (0.485 g, quantitative amount). 1H-NMR(400MHz,CDCl3-CD3OD(15:1))delta:2.98(3H,s), 3.39(2H,t-like,J=6.1Hz), 3.54(2H,t-like,J=6.1Hz), 3.72(2H,s). MS(EI) m/z:114(M+).

109384-27-2, The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1762568; (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.

The piperazine-1-carboxylic acid tert-butyl ester (1.50 g, 8.06 mmol) was dissolved in 30 mL of acetonitrile.Trifluoroethyl trifluoromethanesulfonate (2.25 g, 9.68 mmol), cesium carbonate (3.94 g, 12.10 mmol) was added and stirred at room temperature for 3 hr. After the reaction is complete, filter, filterThe solvent was evaporated under reduced pressure to give the title compound.

57260-71-6, As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; Nanjing Shenghe Pharmaceutical Co., Ltd.; Wang Yong; Zhao Liwen; Ge Chongxun; Huang Yiqiang; Cao Chen; Li Qingqing; Hou Shaohua; (63 pag.)CN108276382; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1 – Methyl-piperazin-2-one hydrochloride (0.844 mmol, 127 mg) in dichloromethane was put on a column of Si-Carbonate (Silicycle, 1 g) and eluation with dichloromethane gave the free base 1 -methyl-piperazin-2- one. To this compound in 2-propanol (1 ml) were subsequently added 4-(1-bromo-8-methylimidazo[1 ,5- a]pyrazin-3-yl)cyclohexanone (0.649 mmol, 200 mg) and aluminium isopropoxide (1.469 mmol, 300 mg) and the mixture was stirred at 60 C for one hour. Sodium triacetoxyborohydride (1.298 mmol, 275 mg) was added and the mixture was stirred at 60 C overnight. Then the reaction mixture was diluted with dichloromethane and water, the dichloromethane layer isolated by a phase separation filter and concentrated in vacuo. The crude product was was purified by column chromatography (silica gel; gradient of dichloromethane to dichloromethane / methanol 92/8) to give 4-((trans)-4-(1-bromo-8-methylimidazo[1 ,5- a]pyrazin-3-yl)cyclohexyl)-1 -methylpiperazin-2-one (50 mg)., 109384-27-2

As the paragraph descriping shows that 109384-27-2 is playing an increasingly important role.

Reference£º
Patent; N.V. ORGANON; MAN de,, Adrianus Petrus Antonius; REWINKEL,, Johannes Bernardus Maria; JANS,, Christiaan Gerardus Johannes Maria; RAAIJMAKERS,, Hans Cornelis Andreas; WIJKMANS,, Jacobus Cornelis Henricus Maria; WO2011/95556; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of 4-fluoronitrobenzene (5.00 g, 35.4 mmol) in THF (50 mL), 1- isopropylpiperazine (4.54 g, 35.4 mmol) and K2CO3 (7.35 g, 53.2 mmol) are added. The reaction mixture is stirred at room temperature overnight. The solvent is removed under reduced pressure and the residue is partitioned between EtOAc and water. The organic layer is washed with brine, dried (MgSO4), filtrered and the solvent is removed under reduced pressure. The crude compound is purified by silica gel column chromatography using 99:1 and 98:2 DCM:NH3 (7 M in MeOH) to give the title compound (8.2g, 94percent)

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GALAPAGOS N.V.; WO2008/65199; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1152367-80-0, (S)-1,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: (S)-1,3-Dimethylpiperazine dihydrochloride (0.16 g, 0.85 mmol) was added in oneportion to (2S)-2-bromo-N-(3-{2-[(3-methoxy-1-methyl-1 H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1 Hindol-7-yl)propanamide (0.2 g, 0.43 mmol, Intermediate 32) and potassium carbonate (0.24 g, 1.7 mmol) in DMF (2 mL) at 0C. The resulting solution was stirred at 25C for 16 hours. The crude product was purified by preparative HPLC (X Bridge C18, 5 tim, 19×150 mm; Mobile Phase A: water0.05% TFA, Mobile Phase B: acetonitrile; Flow rate: 20 mLmin; Gradient: 20%B70%B in 10 mm; 254 nm) to afford (2R)-2-[(2S)-2,4-dimethylpiperazin-1-yl]-N-(3-{2-[(3-methoxy-i -methyl-i H-pyrazol-4-yl)amino]pyrimidin-4-yl}-i H-indol-7-yl)propanamide (49 mg, 23%, Example 1) as a white solid;, 1152367-80-0

As the paragraph descriping shows that 1152367-80-0 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAND, Annika, Birgitta, Margareta; GRIMSTER, Neil, Patrick; KAWATKAR, Sameer; KETTLE, Jason, Grant; NILSSON, Magnus, K.; RUSTON, Linette, Lys; SU, Qibin; VASBINDER, Melissa, Marie; WINTER-HOLT, Jon, James; WU, Dedong; YANG, Wenzhan; GRECU, Tudor; MCCABE, James; WOESSNER, Richard, Donald; CHUAQUI, Claudio, Edmundo; (175 pag.)WO2017/50938; (2017); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.,103-76-4

2-(4-Methylpiperazin-l-yl)ethyl 4-nitrophenyl carbonate To a stirred solution of l-(2-hydroxyethyl)piperazine (26.0 g, 0.2 mol) in DMF (200 mL) was added formic acid (752 mL, 0.2 mol) and formaldehyde (16.2 g, 0.2 mol, 37% solution in water) The reaction mixture was cautiously heated at 100 0C for 2 hours and then stirred overnight at room temperature. The solvent was removed in vacuo. This procedure was repeated 3 further times to give -100 g of product. The crude products were combined and distilled under vacuum to give, at ~74 0C, 2-(4-methylpiperazin-l-yl)ethanol (51 g, 44%) as a colourless liquid. Analytical LCMS: (System B, Rtau = 0.70 min), ES+: 145.1 (100%) [MH]+.

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOVITRUM AB (publ); WO2009/71677; (2009); 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.

Step 1 : tert-Butyl 4-benzylpiperazine-l-carboxylate (0754) [00268] To a solution of compound A3-1 (20.0 g, 107 mmol, 1.0 eq) and (0755) bromomethylbenzene (22.0 g, 129 mmol, 1.2 eq) in CH3CN (300 mL) was added K2CO3 (14.8 g, 107 mmol, 1.0 eq). The reaction mixture was stirred at 70 C for 16 hours. The reaction mixture was concentrated under reduced pressure. The mixture was diluted with water (50 mL) and the resultant mixture was extracted with EA (80 mL * 2). The combined organic layers were dried over NaiSO/t, filtered and concentrated to dryness under reduced pressure. The residue was purified by column chromatography over silica gel (petroleum ether: ethyl acetate = 1 :0 to 5: 1) to afford the title compound (16.8 g, 57% yield) as a white solid. ‘HNMR (400MHZ, CDCl3-i/) delta 7.34 – 7.23 (m, 5H), 3.50 (s, 2H), 3.46 – 3.38 (m, 4H), 2.43 – 2.33 (m, 4H), 1.45 (s, 9H), 57260-71-6

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VIVACE THERAPEUTICS, INC.; LIN, Tracy Tzu-Ling Tang; KONRADI, Andrei W.; VACCA, Joseph; SHEN, Wang; COBURN, Craig; (231 pag.)WO2017/58716; (2017); 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.31321-68-3,(R)-Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of (R)-piperazine-2-carboxylic acid (70 g, 344.71 mmol, 1.0 equiv, 2HCl) in dioxane (1120 mL) and H2O (700 mL) was added 50% aq. NaOH until the solution was pH=11. Benzyl chloroformate (156.82 mL, 1.10 mol, 3.2 equiv) was added and the reaction mixture was stirred at room temperature for 12 h. To the solution was then added H2O (1200 mL) and the aqueous layer was washed with MTBE (3 x 800 mL). The aqueous layer was adjusted to pH=2 with concentrated HCl (12N) and extracted with EtOAc (2 x 1000 mL). The combined organic extracts were dried, filtered and the filtrate was concentrated under reduced pressure to afford the desired product (137 g, 99.8% yield) as a yellow solid. LCMS (ESI) m/z: [M + H] calcd for C21H22N2O6: 399.16; found 399.2., 31321-68-3

31321-68-3 (R)-Piperazine-2-carboxylic acid 6558437, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; REVOLUTION MEDICINES, INC.; PITZEN, Jennifer; GLIEDT, Micah James Evans; BURNETT, G. Leslie; AGGEN, James Bradley; KISS, Gert; CREGG, James Joseph; SEMKO, Christopher Michael; WON, Walter; WANG, Gang; LEE, Julie Chu-Li; THOTTUMKARA, Arun P.; GILL, Adrian Liam; MELLEM, Kevin T.; (484 pag.)WO2019/212990; (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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

75336-86-6, To the 1200 L reactor was dissolved (R)-2-methylpiperazine from Example 5 (25 kg) in CH3CN (319 kg) at [15¡ãC] to [25¡ãC] until dissolution was complete (10 min. ) After cooling to [5¡ãC] to [10¡ãC] Et3N (63 kg) was added. To the 1200 L receiver trityl chloride (69.5 kg) was dissolved in CH2C12 (106 kg) at [15¡ãC] to [25¡ãC.] The solution in the receiver was transferred to the reactor over 0.5 h with a CH2C12 rinse (27 kg), and the solution was heated to [20¡ãC] to [30¡ãC.] The reaction was monitored by GLC and was complete in 1 h. The resulting slurry was cooled to [8¡ãC] to [12¡ãC,] filtered onto a 48″Nutsche filter, and rinsed with CH3CN (40 kg at [8¡ãC] to [12¡ãC).] The filter cake was dried using [50¡ãC] to [55¡ãC] nitrogen to afford 25.26 kg of the by-product [ET3NHCL] (74percent yield; easy to filter off the by-product). The filtrate was transferred to the 1200 L reactor and cooled further [TO-8¡ãC] [TO-10¡ãC] for 1 h. The resulting slurry was filtered onto a 24″Nutsche filter and rinsed [WITH-8¡ãC] to-10¡ãC CH3CN (24 kg) sending the filtrate and rinse to the 1200 L receiver. The filter cake was dried with [50¡ãC] to [55¡ãC] nitrogen to afford another 2.98 kg [ET3NHCL] (9percent yield). The filtrate was transferred to the 1200 L reactor with a CH3CN (10 kg) rinse, and distilled under vacuum to an oil of the title compound of 97.99percent GC purity. The yield was quantitative. M. Pt. [134-136¡ãC.] [APOS;H] NMR (400 MHz, CDC13) : [6] 7.55-7. 40 (6H, br s), 7.25 (6H, t, J = 7. 9 Hz), 7.14 (3H, t, [J =] 7.1 Hz), 3.21-3. 13 (2H, [M),] 3. [10-2. 90 (1H,] br s), 2.94 (2H, t, J = 13.0 Hz), 1.60 [(1H,] br s), 1.48 (1H, br s), 1.15 (1H, br s), 0.94 (3H, d, J = 6.1 Hz), 0.00 (TMS, reference). [13C] NMR (100 MHz, CDC13) : [6] 129.41 (d), 127.46 (d), 125.96 (d), 125.83 (s), 56.12 (t), 51.23 (d), 48.73 (t), 46.45 (t), 20.05 (q), 0.00 (TMS, reference). IR (diffuse reflectance) 2964,2835, 2483 (w), 2350 (w), 2339 (w), 1956 (w), 1490,1025, 909,742 (s), 717,710 (s), 703 (s), 697 (s), 629, [CM-1.] HRMS [(EI)] calcd for [C24H26N2] 342.2096, found [342. 2101.] [a] [25D=-12¡ã (C 1. 00, CH2CL2).] Anal. Calcd for [C24H26N2] : C, 84.17 ; H, 7.65 ; N, 8.18. Found: C, 84.12 ; H, 7.64 ; N, 7.94.

75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOVITRUM AB; WO2004/829; (2003); 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.

General procedure: A mixture of 3 (100 mg, 0.28 mmol), arylpiperazines or piperidines,K2CO3, (1.2 equiv), potassium carbonate (6.0 equiv) and CH3CN(25 mL) were placed in 50-mL round-bottomed flask equipped withmagnetic stirrer for 14 h at 85 C (monitored by TLC). After completionof reaction, the reaction mixture was filtered, and the filtrate wasconcentrated in vacuo. Then the residue was purified by chromatographyon silica-gel column (petroleum ether: ethyl acetate=5:1, v/v)to obtain the corresponding products (4-26), and all compounds wererecrystallized from dichloromethane and n-hexane., 115761-79-0

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chen, Hong; Liang, Xue; Sun, Tao; Qiao, Xiaoguang; Zhan, Zhou; Li, Ziyong; He, Chaojun; Ya, Huiyuan; Yuan, Mu; Steroids; vol. 134; (2018); p. 101 – 109;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics