Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

4-Fluorobenzaldehyde15 (619 muL, 5.85 mmol), 1-acetylpiperazine (500 muL, 3.90 mmol) and Na2CO3 (620 mg, 5.85mmol) were dissolved in H2O (25 mL) and the stirred at 100C overnight. After extractionwith DCM, the combined organic layers were concentrated under reduced pressure and silicagel column chromatography (3% MeOH/DCM) yielded 17a (942 mg, 58%). 1H NMR (500MHz, DMSO-d6) delta 9.73 (s, 1H), 7.73 (d, J = 8.9 Hz, 2H), 7.04 (d, J = 8.9 Hz, 2H), 3.65-3.54 (m,4H), 3.50-3.44 (m, 2H), 3.42-3.36 (m, 2H), 2.04 (s, 3H); 13C NMR (126 MHz, DMSO-d6) delta190.2, 168.42, 154.3, 131.4, 126.4, 113.2, 46.3, 46.0, 44.9, 40.3, 21.1; HRMS (ESI-MS): Calculatedfor C13H17N2O2 [M+H]+: 233.12845; found: 233.12871.

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Buehrmann, Mike; Wiedemann, Bianca M.; Mueller, Matthias P.; Hardick, Julia; Ecke, Maria; Rauh, Daniel; PLoS ONE; vol. 12; 9; (2017);,
Piperazine – Wikipedia
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5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5464-12-0

General procedure: To a solution of triphenylphosphine (0.37 mmol) in THF (30 mL) was slowly added diisopropyl azodicarboxylate (0.37 mmol) in 15 min at 0 °C and the mixture was stirred for another 15 min. At the same temperature, to the resulting mixture was slowly added a solution of 20 (0.185 mmol) and corresponding alcohol (0.37 mmol) dissolved in 20 mL THF. The ice bar was removed and the reaction mixture was stirred at room temperature for 12 h. The reaction mixture was evaporated in vacuo, and the residue was purified by column chromatography to afford the product.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Xing, Weiqiang; Ai, Jing; Jin, Shiyu; Shi, Zhangxing; Peng, Xia; Wang, Lang; Ji, Yinchun; Lu, Dong; Liu, Yang; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 95; (2015); p. 302 – 312;,
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21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 38; 2-Chloro-6-(alpha5-3,5-dimethyI-piperazin-l-yImethyl)-4-morphoIin-4-yl-thieno[3,2- d]pyrimidipite; To a solution of 6-bromomethyl-2-chloro-4-morpholin-4-yl-thieno[3,2- djpyrimidine (150 mg, 0.43 mmol) in DMF (4 mL) were added (cz>)-2,6-dimethyl- piperazine (74 mg, 0.648 mmol) and potassium carbonate (117 mg, 0.847 mmol). The resulting mixture was stirred at RT for 17 h, then concentrated in vacuo. The resulting residue was triturated with water to give the title compound as an off-white solid (127 mg, 77 percent). [M + H]+ 382.3, 21655-48-1

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

Reference：
Patent; PIRAMED LIMITED; WO2007/122410; (2007); 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

5317-33-9, 1.5 324.34 mg of 3-(3-aminobenzyl)-5-methoxy-2-benzoxazolinone are suspended in 5 ml of dichloromethane in a reaction vial fitted with a magnetic stirrer, 252.03 mul of triethylamine are added, 145.35 mg of bis-(trichloromethyl) carbonate (triphosgene) are carefully added with cooling and stirring, and the mixture is stirred at RT for 10 minutes. 208.88 mg of 3-(4-methyl-1-piperazinyl)-1-propanol are then added, and the mixture is stirred at RT for 24 h in a tightly sealed reaction vial in a multiple synthesiser. The reaction mixture is diluted with dichloromethane, washed with water, dried and filtered, and the solvent is removed. The residue is adsorbed onto silica gel and chromatographed over a flash column on a FlashMaster with 20 g of LiChroprep 60 (25-40 mum) and dichloromethane+0-50% of methanol. The residue is dissolved in methanol, ethereal hydrochloric acid is added, the salt is precipitated using ether, and the supernatant solution is poured off. The salt is crystallised using methanol/ether, filtered off with suction, washed with ether and dried; m.p. 120, decomposition from 150;ESI: 455 (M+H); HPLC: Rt=4.00 (method A);yield: 383 mg (61%) of ?A1?.

As the paragraph descriping shows that 5317-33-9 is playing an increasingly important role.

Reference：
Patent; MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG; US2010/280030; (2010); 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

General procedure: 6.1.15. General procedure IV, for preparation of 14a-f A mixture of aryl bromide (1.0 mmol), 4-methylpiperazin-2-one (for compounds 15-17)/morpholin-3-one (for compounds 18-20) (2.0 mmol), N,N0-dimethylethylene diamine (0.1 mmol), K2CO3 (2.0 mmol) and CuI (0.05 mmol) in anhydrous toluene was heated to reflux with stirring for 6 h. Then the reaction mixture was cooled to room temperature, poured into water, stirred vigorously and extracted thrice with ethyl acetate, dried over anhydrous Na2SO4, concentrated under reduced pressure and purified by flash chromatography to afford compounds 14a-f in 54-68% yields. 6.1.17 4-Methyl-1-(5-vinylpyridin-2-yl)piperazin-2-one (14b) A mixture of 2-bromo-5-vinylpyridine 3b (0.15 g, 0.81 mmol), 4-methylpiperazin-2-one (0.18 g, 1.63 mmol), N,N’-dimethylethylene diamine (0.007 g, 0.08 mmol), K2CO3 (0.22 g, 1.63 mmol) and CuI (0.007 g, 0.04 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14b (0.11 g) in 62.8% yield. 1H NMR (400 MHz, CDCl3): delta 8.40 (d, J = 2.3 Hz, 1H), 8.12 (dd, J = 8.6, 1.0 Hz, 1H), 7.80 (dd, J = 8.7, 2.4 Hz, 1H), 6.72 (dd, J = 17.7, 11.0 Hz, 1H), 5.81 (dd, J = 17.7, 0.7 Hz, 1H), 5.38 (dd, J = 11.0, 0.8 Hz, 1H), 3.66-3.76 (m, 2H), 3.28 (s, 2H), 2.76-2.82 (m, 2H), 2.41 (s, 3H); LC-MS: 218 (M++1).

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Rakesh; Bruhn, David; Maddox, Marcus; Lee, Robin B.; Yang, Lei; Lee, Richard E.; Madhura, Dora B.; Trivedi, Ashit; Meibohm, Bernd; Scherman, Michael S.; Gilliland, Janet C.; Gruppo, Veronica; McNeil, Michael R.; Lenaerts, Anne J.; Bioorganic and medicinal chemistry; vol. 20; 20; (2012); p. 6063 – 6072,10;,
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.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.

54699-92-2, Example 13; General Method For The Preparation Of Active Esters Of N-Substituted Piperazine Acetic Acid From Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

54699-92-2 4-Methyl-1-piperazineacetic acid 2762732, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Applera Corporation.; US2005/148773; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A/Preparation of N-(2-hydroxyethyl)-N’-methylpiperazine: N-methylpiperazine (10 g; 100 mmol) and 2-chloroethanol (8.05 g; 100 mmol) are stirred at 100° C. for 4 h. The highly viscous reaction medium is supplemented with 250 ml of acetone and the resulting suspension is neutralized with 15 ml of triethylamine. After filtration of the triethylamine hydrochloride, the solvent is evaporated under reduced pressure. The desired compound is obtained after purification by chromatography on an alumina column (Merck.(R).; Aluminum Oxide 90; 63-200 mum, eluent: ethyl acetate) in the form of a colorless oil. Yield: 75percent

109-01-3, As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference：
Patent; Oxis Isle of Man, Limited; US6056965; (2000); A;,
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

General procedure: A mixture of compounds 11 (2.74 g, 10 mmol), amine 12(11 mmol), and K2CO3 (1.66 g, 12 mmol) in CH2Cl2 (10 ml) wereheated at 40 C for 0.5 h. The progress of the reaction was monitoredby TLC, after completion of the reaction, the reaction mixturewas extracted with three portions of CH2Cl2. The orange extractswere washed with brine until neutrality, then dried over anhydrousNa2SO4 and concentrated in vacuo. Then the residue waspurified by a silica-gel column chromatography (PE/EtOAc 3:1) togive the desired compounds.

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

Reference：
Article; Wang, Jin; Xia, Fei; Jin, Wen-Bin; Guan, Jin-Yan; Zhao, Hang; Bioorganic Chemistry; vol. 68; (2016); p. 214 – 218;,
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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

100 g (1.2 mol) of anhydrous piperazine and 240 g (1.5 mol) of piperazine dihydrochloride were heated to 120 C, and 150 g (1.2 mol) of 2-(2-chloroethoxy)ethanol was added dropwise. After the completion of heating and stirring, the temperature was raised to 136-140 C for 1 hour, and TLC showed that the reaction was completed and then the heating was stopped. When the temperature dropped to 80 degrees Celsius, 500ml of 95% ethanol was added, cooled in the refrigerator overnight, and the piperazine dihydrochloride was recovered by filtration the next day. The filter cake was washed thoroughly with a small amount of ethanol, the filtrate was combined, and 200 g of 30% sodium hydroxide solution was added, alkalized, and the insoluble inorganic salt was filtered off, and concentrated to remove the solvent. The residue was extracted with ethyl acetate, dry hydrogen chloride gas was passed, filtered and dried to give a white solid 1-[2-(2-hydroxyethoxy)ethyl]piperazine hydrochloride. The solid content was already above 98%. After recrystallization from a 90% aqueous solution of ethanol, 207 g of white crystals can be obtained, the yield was 70%, and the content can be more than 99.5%., 142-64-3

The synthetic route of 142-64-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Wuxi Qianhao Bio-pharmaceutical Co., Ltd.; Peng Haiyan; (4 pag.)CN109400549; (2019); 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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Synthesis of N-[3-(4-{[4-(2-methoxyethyl)piperazinyI]methyl}phenyl)-4- oxoindeno[2,3-d]pyrazol-5-yl](morpholin-4-ylamino)carboxamide dihydrochloride (compound B16):Acetic acid (5.76 g, 96 mmole) was added to a suspension of aldehyde (10 g, 24 mmole) and piperazine (6.91 g, 48 mmole) in NMP (150 mL). The reaction was stirred at room temp for 16h then treated with NaB(OAc)3H (12.7 g, 60 mmole). The reaction was stirred at room temp for 2Oh during which time the reaction becomes very viscous. IN NaOH (200 mL) was then added and the reaction was stirred for Ih. The reaction was then poured onto H2O (750 mL) and filtered. The solid was washed with H2O (2 x 350 mL), EtOH (100 mL), and Et2O (200 mL). The solid was then dried under vacuum to yield the desired amine as the free base (9.98 g, 76%). The free base was then suspended in EtOH (200 mL) and heated to boiling. The suspension was then treated with 4N HCl in dioxane (15 mL). The suspension clears then after ~15 min, a thick precipitate forms. Additional EtOH (200 mL) was added to facilitate stirring. Once the suspension cooled to room temp, it was filtered and the solid was washed with EtOH (200 mL) and Et2O (200 mL). The solid was then dried under vacuum to yield the desired bis-hydrochloride salt (10.3 g) designated compound B 16.

13484-40-7, 13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GPC BIOTECH, INC.; WO2006/2119; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics