Heterocyclic Building Blocks-piperazine

54699-92-2, 4-Methyl-1-piperazineacetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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, -CH2-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

As the paragraph descriping shows that 54699-92-2 is playing an increasingly important role.

Reference£º
Patent; Applera Corporation.; US2005/148771; (2005); A1;; ; Patent; Applera Corporation.; US2005/148774; (2005); A1;,
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57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-71-6, The compound 1-tert-butoxycarbonyl piperazine (0.6g, 3.2mmol) and triethylamine (4.6mL, 32mmol) wasdissolved in dry tetrahydrofuran (10 mL), at room temperature, to this solution was added dropwisetrimethylsilyl isocyanate (4.2mL, 32mmol), stirred at rt for 1.5h, ice Water (10 mL), tetrahydrofuran spin, theaqueous phase with ethyl acetate (30mL ¡Á 3). The organic phase was dried over anhydrous Na 2 SO 4, removeThe solvent was concentrated and solid was washed with ethyl acetate (2mL) ultrasonic cleaning 1min, suctionfiltration, to give 0.3g white solid: 4-carbamoyl-piperazine 1-carboxylate, yield: 40%.

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

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
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934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 250 mL round bottom flask equipped with a stir bar was charged with Example 1U (1.96 g) and anhydrous dichloromethane (160 mL) at room temperature under nitrogen. The mixture was cooled to 0¡ã C. in an ice bath, and 2-(4-methylpiperazin-1-yl)ethanamine (0.395 mL) was added via a syringe. The mixture was stirred for 25 minutes at 0¡ã C., and sodium triacetoxyborohydride (156 mg) was added as a solid. The reaction mixture was stirred for 15 minutes at 0¡ã C., and powdered activated 3 angstrom molecular sieves were added (1.96 g). The reaction mixture was stirred 2 hours at 0¡ã C., and was allowed to stir and warm slowly to room temperature overnight. LC/MS indicated one major peak with a mass that corresponded to desired product. The reaction mixture was quenched with dichloromethane and water. The layers were separated, and aqueous layer was extracted with dichloromethane and 10percent methanol/dichloromethane. The aqueous layer was neutralized with saturated aqueous NaHCO3 mixture, and was extracted one more time with 10percent methanol/dichloromethane. The combined extracts were washed with saturated aqueous NaHCO3 and brine, dried with Na2SO4, filtered, and concentrated. The residue was dissolved in dichloromethane and was purified on a Grace Reveleris X2 MPLC using a Teledyne Isco RediSep? Rf gold 750 g silica gel column eluting with a gradient of 0-20percent of methanol/dichloromethane over 40 minutes. The mixed fractions were purified on a Grace Reveleris X2 MPLC using a Teledyne Isco RediSep? Rf gold 330 g silica gel column eluting with a ramp of 0-15percent of methanol/dichloromethane over 40 minutes to collect additional title compound. The material from both columns was combined to provide the title compound. 1H NMR (501 MHz, dimethyl sulfoxide-d6) delta ppm 8.61 (m, 2H), 7.47 (m, 2H), 7.39 (d, 1H), 7.17 (m, 7H), 7.04 (td, 1H), 6.96 (dd, 1H), 6.67 (d, 1H), 6.51 (d, 1H), 5.84 (dd, 1H), 5.06 (m, 2H), 4.07 (ddq, 2H), 3.90 (d, 1H), 3.75 (s, 3H), 3.68 (dd, 2H), 3.50 (d, 1H), 3.17 (m, 1H), 3.08 (m, 1H), 2.90 (m, 2H), 2.65-2.20 (m, 10H), 2.14 (s, 3H), 1.67 (s, 3H), 1.09 (t, 3H). MS (ESI) m/z 928.4 (M+H)+., 934-98-5

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AbbVie Inc.; AbbVie Deutschland GmbH & Co. KG; Brady, Patrick B.; Braje, Wilfried; Dai, Yujia; Doherty, George A.; Gong, Jane; Jantos, Katja; Ji, Cheng; Judd, Andrew S.; Kunzer, Aaron R.; Lai, Chunqiu; Mastracchio, Anthony; Risi, Roberto M.; Song, Xiaohong; Souers, Andrew J.; Sullivan, Gerard M.; Tao, Zhi-Fu; Teske, Jesse A.; Wang, Xilu; Wendt, Michael D.; Yu, Yiyun; Zhu, Guidong; Penning, Thomas D.; (218 pag.)US2019/55264; (2019); A1;,
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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.

0.36 g of N-[4-tert-butyl-5-(4-chlorobenzyl)thiazol-2-yl]-2-chloroacetamide and 5 mL of tetrahydrofuran, Stir at room temperature, 0.24 g of pyridine and 0.23 g of N-ethylpiperazine are added; Reaction overnight, Desolvent, Add dichloromethane, Saturated salt water wash, Drying with anhydrous sodium sulfate, Desolvent, Add petroleum ether to precipitate solids, Suction filtration Wash with petroleum ether, Dry to give a pale yellow solid of N-[4-tert-butyl-5-(4-chlorobenzyl)thiazol-2-yl]-2-(4-ethylpiperazinyl)acetamide, Yield 71.3%, 5308-25-8

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

Reference£º
Patent; Hunan University; Hu Aixi; Wu Zhilin; Ding Na; Ye Jiao; (20 pag.)CN107365280; (2017); A;,
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78818-15-2,78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

-(t-Butyloxycarbonyl)-piperazin-2-one (0.6 g, 3.0 mmol), EXAMPLE 40, is dissolved in THF (80 mL), cooled in an ice bath and treated with tretrabutylammonium iodide (0.23 g, 0.62 mmol) and 60% sodium hydride (0.12 g, 3.0 mmol). The reaction mixture is stir

78818-15-2 Benzyl 3-oxopiperazine-1-carboxylate 736777, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AVENTIS PHARMACEUTICALS INC.; US2004/102450; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: In a flask chargedwith 50 mL of CH3CNwas added 2.5mmol of compound6 and appropriate piperazine derivatives (3a-w, 1.5 eq.) and thereaction mixturewas refluxed for 10-38 h until the complete consumptionof starting material as detected by TLC. After the completion of thereaction, the reaction mixture was treated with ice and the resultingsolid was filtered and washed with water (2 ¡Á 25 mL). The residuewas purified with a silica gel column chromatography and was elutedwith dichloromethane: methanol (40:1) to afford corresponding products7a-w in 49-82% of yields, 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Patel, Rahul V.; Mistry, Bhupendra; Syed, Riyaz; Rathi, Anuj K.; Lee, Yoo-Jung; Sung, Jung-Suk; Shinf, Han-Seung; Keum, Young-Soo; European Journal of Pharmaceutical Sciences; vol. 88; (2016); p. 166 – 177;,
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1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIPEA (5.24 ml, 30.06 mmol) was added to a stirred mixture of ferf-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1.73 g, 7.51 mmol) and 7-bromo-4-chloro-5,8-difluoroquinazoline (2.1 g, 7.51 mmol) in MeCN (100 ml) at room temperature. The resulting solution was stirred at room temperature for 3 hours, a suspension developed after ~30 minutes. The precipitate was collected by filtration, washed with MeCN (3 x 20 ml) and dried under vacuum to afford desired product, 2.64 g. On standing overnight a second crop of desired product, 300 mgs was isolated to afford ferf-butyl 4-(7-bromo-5,8-difluoroquinazolin-4-yl)-3-(2-hydroxyethyl)piperazine-l-carboxylate (2.94 g, 83%), as a white solid, which was used without further purification. 1H NM R (400 MHz, DMSO, 30C) 1.43 (9H, s), 1.71 – 1.82 (2H, m), 2.86 (1H, s), 3.18 (1H, s), 3.37 – 3.51 (2H, m), 3.72 (1H, d), 3.97 (2H, d), 4.36 (1H, s), 4.70 (1H, s), 7.75 (1H, dd), 8.62 (1H, s) OH not observed, m/z (ES+), [M+H]+ 473, 475., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

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;,
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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.

[00307] In a microwaver vial containing 2,6-dichioro-nicotinamide (150.00 mg; 0.79 mmol;1.00 eq.) and (4-amino-phenyl)- (4-methyl-piperazin- 1 -yl)-methanone (206.64 mg; 0.94 mmol;1.20 eq.) was added THF (10.00 ml; 123.43 mmol; 157.18 eq.) and sodiumbis(trimethylsilyl)amide (2.30 ml; 2.36 mmol; 3.00 eq.) at -78C. The reaction was stuffed at rt for 1 .5h before it was quenched with lmL sat. NH4C1 solution and extracted with EtOAc (5mL X 3). The combined organic layers were combined, concentrated and carried to the next step. MS:mlz = 374 [M+H]+

55121-99-8, As the paragraph descriping shows that 55121-99-8 is playing an increasingly important role.

Reference£º
Patent; MERCK PATENT GMBH; QIU, Hui; CALDWELL, Richard D.; NEAGU, Constantin; MOCHALKIN, Igor; LIU-BUJALSKI, Lesley; JONES, Reinaldo; TATE, Devon; JOHNSON, Theresa L.; GARDBERG, Anna; WO2015/61247; (2015); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step A: tert-Butyl (3R)-4¡¤:f2-( 4-cyano-3-:methoxyphenyl)-2-hydroxyethyl]-3 (hydroxymethyl)piperazine1-carboxylate; A Pyrex vessel was charged with magnetic stirring bar, (2.0 g, 11.42mmol) of 2-methoxy-4-( oxiran-2-yl) benzonitrile, (3. 70 g, 17.12 mmol) of tert-butyl (3R)-3-(hydroxymethyl)piperazine-1-carboxylate, and 6 mL ofEtOH. Then it was introduced in themicrowave reactor and irradiated at 150 C for 3 h. The mixture was cooled to room temperatureand the solvent was evaporated and the resulting residue was purified by column chromatography (silica gel, 1- 20% dichloromethane/MeOH) which afforded the product as a mixture of twodiastereomers (1 :1) LC/MS: (IE, m/z) [(M + 1)- t-Bu]+ = 336.41

278788-66-2, The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); 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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

934-98-5, General procedure: A suspension oftert-butyl 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-formyl-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)benzoate5(1 eq.), the corresponding amine (2 eq.) and acetic acid (2 – 5 eq.) in DCE (2 ml) was stirred at RT for 30 min.To this suspension was added sodium triacetoxyborohydride (5 eq.).The resulted mixture was stirred at RT for 18 – 72 hrs.The reaction mixture was diluted with 5 ml of saturated sodium carbonate and extracted with DCM (3 x 10 ml).The combined organic layers were dried over sodium sulfate, filtered and concentratedinvacuo.The crude product was purified by Biotage flash chromatography or was used directly in the next step without further purification.

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chen, Yan; Sit, Sing-Yuen; Chen, Jie; Swidorski, Jacob J.; Liu, Zheng; Sin, Ny; Venables, Brian L.; Parker, Dawn D.; Nowicka-Sans, Beata; Lin, Zeyu; Li, Zhufang; Terry, Brian J.; Protack, Tricia; Rahematpura, Sandhya; Hanumegowda, Umesh; Jenkins, Susan; Krystal, Mark; Dicker, Ira D.; Meanwell, Nicholas A.; Regueiro-Ren, Alicia; Bioorganic and Medicinal Chemistry Letters; vol. 28; 9; (2018); p. 1550 – 1557;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics