Month: March 2021

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 44 (7R,20S)-ethyl 18-chloro-1-(4-fluorophenyl)-10-{[2-(2-methoxyphenyl)pyrimidin-4-yl]methoxy}-19-methyl-15-[2-(piperazin-1-yl)ethyl]-7,8,15,16-tetrahydro-14H-17,20-etheno-13,9-(metheno)-6-oxa-2-thia-3,5,15-triazacyclooctadeca[1,2,3-cd]indene-7-carboxylate To a mixture of Example 1T (200 mg) in dichloromethane (10 mL) was added tert-butyl 4-(2-aminoethyl)piperazine-1-carboxylate (84 mg). The mixture was stirred at ambient temperature for 30 minutes, and sodium triacetoxyborohydride (104 mg) and 4 A molecular sieves (250 mg) were added. The reaction mixture was stirred overnight and was quenched by the addition of saturated aqueous sodium bicarbonate mixture and ethyl acetate. The layers were separated, and the aqueous layer was extracted with ethyl acetate (50 mL*2). The combined organics were washed with brine, dried over anhydrous sodium sulfate, filtered and concentrated. The residue was dissolved in dichloromethane (5 mL) and trifluoroacetic acid (5 mL) was added. After 1 hour, the reaction mixture was concentrated under reduced pressure. The residue was purified by reverse phase HPLC (Zorbax C-18, 10 to 50percent acetonitrile in water containing 0.1percent v/v trifluoroacetic acid) to provide the title compound. 1H NMR (400 MHz, dimethyl sulfoxide-d6) delta ppm 9.01 (s, 1H), 8.77-8.56 (m, 2H), 7.63-7.37 (m, 3H), 7.34-7.08 (m, 8H), 7.03 (td, 1H), 6.85 (d, 1H), 6.41 (d, 1H), 5.95 (dd, 1H), 5.32-4.88 (m, 2H), 4.46-3.84 (m, 6H), 3.74 (s, 3H), 3.61-3.35 (m, 2H), 3.20 (dt, 8H), 3.04 (q, 4H), 1.75 (s, 3H), 1.00 (t, 3H). MS (ESI) m/z 915 (M+H)+., 192130-34-0

The synthetic route of 192130-34-0 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;,
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

An oven dried 1000 mL 3-necked flask was equipped with a mechanical stirrer, nitrogen in- and outlet and cooled to room temperature under a nitrogen flow. Amine 3 (38.1 g, 173 mmol) was put in the flask and dissolved in dry N-methylpyrollidin-2-one (NMP) (503 g). The solution was cooled for 20 minutes in an ice-water bath after which solid terephthaloyl dichloride flakes (17.53 g, 86.3 mmol, 0.50 eq) were added to the flask in a single portion while stirring at 500 rpm. The addition funnel was rinsed with NMP (40 g) and the suspension was stirred for 1 h at 0 C. followed and 0.5 h at room temperature. Concentrated aqueous ammonium hydroxide (94 g, 30 w %) was slowly added to the reaction mixture which was subsequently poored into demineralized water (3.5 L). The pH of the solution was adjusted to 10 by addition of more ammonium hydroxide solution (130 g, 30 w %). The fine, white precipitate was allowed to settle for about 0.5 hour after which the clear top layer was decanted. The precipitate was suspended, filtered over a Millipore filter (Durapore GV, 0.22 mum pore size) while applying vacuum and washed with demineralized water (3¡Á250 mL). The crude product was further purified by repetitive (4¡Á) suspension of the product in warm, high-purity MilliQ water (1.0 L, T=65 C.) for about 1 hour, cooling to approximately 36-38 C., filtration over a Millipore filter, washing with MilliQ water (2¡Á250 mL) and drying to the air under suction for 5-15 minutes. The wet product was dried overnight under vacuum at 50 C. to give the desired compound as an off-white, fine powder (46.4 g, 95%).

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

Reference£º
Patent; TEIJIN ARAMID B.V.; VAN DEN HEUVEL, Christiaan J.M.; VELD, Martijn Arnoldus Johannes; QUAIJTAAL, Joannes H.M.; VERHOEF, Rene P.; DE JONG, Jorrit; NIJENHUIS, Wido; (12 pag.)US2018/223077; (2018); 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.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78818-15-2, l-(2-Hvdroxy-ethvn-4-r2-(lH-indazol-4-ylV4-morrhoholin-4-yl-thienor3,2- d]pyrimidin-6-ylmethyl”l-piperazin-2-one (87).Prepared via 4-(2-Chloro-4-morpholin-4-yl-thieno[3,2-d]pyrimidin-6- ylmethyl)-l-(2-hydroxy-ethyl)-piperazin-2-one, prepared from l-(2-hydroxy-ethyl)- piperazin-2-one.Amine preparation: to 4-CBZ-piperazin-2-one (1.95g) in DMF (5mL) at O0C was added sodium hydride (60% dispersion in mineral oil, 660mg) in several aliquots. After stirring for 1 h, 2-bromoethylacetate (1.38ml) was added. The reaction mixture was stirred at room temperature overnight; it was then diluted with ethyl acetate, washed with brine, dried (MgSO4) and the solvent was removed in vacuo. The resulting residue was purified using flash chromatography to yield 4-(2-acetoxy- ethyl)-3-oxo-piperazine-l-carboxylic acid benzyl ester (925mg). 1H NMR (400MHz, J6-DMSO): 2.77 (2H, d, J=5.5Hz), 3.16 (2H, s), 3.32-3.36 (2H, m), 3.38-3.42 (2H, m), 3.51-3.55 (2H, m), 3.80-3.85 (4H, m), 3.97 (2H, s), 4.00-4.04 (4H, m), 4.70 (IH, t, J=5.4Hz, OH), 7.45 (IH, t, J=7.7Hz), 7.50 (IH, s), 7.66 (IH, d, J=8.2Hz), 8.22 (IH, d, J=7.3Hz), 8.89 (IH, s), 13.15 (IH, br, NH); MS (ESI+) 494 (MH+).

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

Reference£º
Patent; PIRAMED LIMITED; WO2006/46031; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

301673-16-5, tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Sodium hydroxide (IN aqueous solution, 20 mL, 20 mmol) was added to a solution of Intermediate B (2.59 g, 10.7 mmol) in EtOH (20 mL), and the reaction mixture was heated to 70 0C for 1 h. Upon cooling to rt, the EtOH was removed under reduced pressure. The aqueous solution was diluted with THF (40 mL) and benzyl chloroformate (1.60 mL, 10.7 mmol) was added. After 1 h, the reaction mixture was diluted with water (50 mL) and was extracted with EtOAc (3 x 50 mL). The combined organics were dried over Na2SO4, filtered, and concentrated under reduced pressure. The material was purified by column chomatography (20 to 40percent EtOAc in Hexane gradient) to give 3.16 g (85percent) of the desired product as a thick oil. LC-MS: RT = 8.41 min., [M+H]+ = 373.1.

301673-16-5, As the paragraph descriping shows that 301673-16-5 is playing an increasingly important role.

Reference£º
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); 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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

13754-38-6, Example 18 N-{[1-(2-(4-benzoylpiperazine-1-yl)propane-1-yl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide 400 mg (1 . 07 mmol) N-{[1-(2-hydroxypropyl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide and 0.18 ml (1.29=01, 1.2 eq.) triethylamine described at manufacturing example 6 were dissolved to 20 ml dichloromethane and cooled to 3 C. under argon gas. 135 mg (1.18 mmol, 1.1 eq.) methansulfonyl chloride was slowly added to reaction solution and was stirred at same temperature for 30 min. 20 ml purified water was added and then organic layer was separated and concentrated with decompression. After 10 ml acetonitrile were added to obtained residues and dissolved them, 444 mg (3.21 mmol) potassium carbonate and 202 mg (1.06 mmol) 1-benzoylpiperazine were added. After stirring for 2 hours at room temperature, 15 ml saturated sodium chloride aqueous solution was added to reaction solution and was extracted twice with 15 ml ethylacetate. After organic layer was collected and dried with anhydrous magnesium sulfate, it was concentrated with decompression. 30 mg (51%) target compound as light-yellow solid was yielded by purifying obtained residues with chromatography using silicagel (mobile phase:dichloromethane/methanol=5:1 and 1:1). 1H NMR (400 MHz, DMSO-d6) 1.05 (3H, s), 1.55-1.65 (1H, m), 2.00-2.10 (1H, m), 2.15-2.25 (1H, m), 2.28-2.55 (9H, m), 2.70-2.85 (2H, m), 3.17 (1H, d), 3.54-3.65 (2H, m), 3.87 (2H, d), 4.10-4.20 (1H, m), 7.35-7.40 (2H, m), 7.40-7.47 (3H, m), 7.74 (1H, t), 7.92 (1H, d), 8.14 (1H, s), 8.18 (1H, d), 8.23 (1H, s), 9.01 (1H, t) MS (M)+ 545.6

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; YANG JI CHEMICAL CO., LTD.; US2012/190689; (2012); 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.123987-13-3,(3-(4-Methylpiperazin-1-yl)phenyl)methanol,as a common compound, the synthetic route is as follows.

A mixture of thionyl chloride (87 mg, 0.727 mmol) and (3-(4-methylpiperazin-l- yl)phenyl)methanol (30.0 mg, 0.145 mmol) in DCM (10 mL) was heated to 60 C for 2 h. The mixture was then concentrated under reduced pressure to a foam, which was used for the next step without further purification. MS(ES+) Ci2HisN20 requires: 224, found: 225 [M+H]+., 123987-13-3

As the paragraph descriping shows that 123987-13-3 is playing an increasingly important role.

Reference£º
Patent; JONES, Philip; DIFRANCESCO, Maria, Emilia; PETROCCHI, Alessia; MARSZALEK, Joe; LIU, Gang; KANG, Zhijun; CARROLL, Christopher, L.; MCAFOOS, Timothy; CZAKO, Barbara; WO2014/31928; (2014); A2;,
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Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5308-25-8, A mixture of 5-bromo-2-nitropyridine (1.02 g, 5.02 mmol) and 1 -ethylpiperazine (1 .71 g, 15.0 mmol) in N-methyl-2-pyrrolidinone (5 mL) was stirred at 120 C for 3 h. After this time, the reaction was cooled to room temperature, poured into water (100 mL) and extracted with methylene chloride (2 chi 100 mL). The combined organic layers were dried over sodium sulfate, filtered and the filtrate concentrated under reduced pressure. The resulting residue was purified by chromatography (silica, gradient, 1 :49 methanol/methylene chloride to 1 :9 methanol/methylene chloride) to afford l-ethyl-4-(6-nitropyridin-3- yl)piperazine as a yellow solid: 1H NMR (400 MHz, DMSO- )d 8.25 (d, J = 2.8 Hz, 1 H), 8.14 (d, J = 9.2 Hz, 1H), 7.48 (dd, J = 9.2, 2.8 Hz, 1H), 3.50-3.46 (m, 4H), 2.50-2.38 (m, 4H, merged with DMSO peak), 2.37 (q, J = 7.2 Hz, 2H), 1.02 (t, J= 7.2 Hz, 3H).

5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GILEAD SCIENCES, INC.; BLOMGREN, Peter; CURRIE, Kevin, S; KROPF, Jeffrey, E.; LEE, Seung, H.; MITCHELL, Scott, A.; SCHMITT, Aaron, C.; XU, Jianjun; ZHAO, Zhongdong; WO2011/112995; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3,70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 4-Nitrobenzyl bromide (46.3mmol) was dissolved in dichloromethane (100mL). The solution was added to the mixture of relative amine (47.0mmol) and triethylamine (70.3mmol) in dichloromethane (20ml). The reaction mixture was stirred at r. t. for 24 h and was extracted with dichloromethane (100ml¡Á3). After removal of the solvent, the residue was crystallized from ethanol, giving yellow powder. Compounds 1 and 2 were used for further reaction without purification. To a suspension of compounds 1-2 (36.2mmol) in 95% ethanol (100ml), 85% NH2NH2¡¤H2O (362mmol), 95% ethanol (100ml) and iron (III) oxide hydroxide (FeO(OH)/C, 2.0g) were added and heated to reflux. When TLC analysis showed complete conversion of the starting material, the reaction mixture was filtrate through Cellit and the filtrate was concentrated in vacuum. The crude product was purified by silica gel colum chromatography (DCM/MeOH) to yield the title compound (3 and 4) as white solid. The mixture of compound 4 (1eq, 18.5mmol), 4-Nitro-1H-pyrazole-3-acid (1.1equiv, 20.4mmol), EDC (1.2equiv, 22.2mmol), HOBT (1.2equiv, 22.2mmol) in DMF (50ml) was stirred for 24h. The ice water (100ml) was added to the reaction mixture. A large amount of yellow solid precipitation (compound 8) was acquired. Compound 8 was used without further purification. Compounds 8 was reduced by the same process as compound 4, and then the resulting compound 12 was purified by column chromatography on silica gel, eluted with the appropriate solvent.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Article; Zhi, Yanle; Li, Baoquan; Yao, Chao; Li, Hongmei; Chen, Puzhou; Bao, Jiyin; Qin, Tianren; Wang, Yue; Lu, Tao; Lu, Shuai; European Journal of Medicinal Chemistry; vol. 155; (2018); p. 303 – 315;,
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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of carboxylic acid (50 mmol) in DMF (0.25 mL) in a 48 position Mettler Toledo XT reaction block was added PyBOP (50 mmol, 0.2 mL of 0.3 M solution in DMF) and TEA (75 mmol, 0.05 mL of 1.5 M solution in DMF) followed by the appropriate amine build blocks (55 mmol, 0.55 ml of 1 M solution in DMF). The reactions were stirred at rt 24 h and concentrated by GeneVac HT-4 to remove all reaction mixture including excess amine and DMF. The crude mixtures were dissolved in EtOAc (1 mL) and filtered through silica-packed short-column and washed with EtOAc (3 mL). The collected organic solution was concentrated in GeneVac HT-4 and dissolved in DMSO (1 mL). DMSO solution was subjected to HTAC for pre-purification analysis, purification, and final QC., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Hwang, Jong Yeon; Attia, Ramy R.; Carrillo, Angela K.; Connelly, Michele C.; Guy, R. Kiplin; Bioorganic and Medicinal Chemistry Letters; vol. 23; 6; (2013); p. 1891 – 1895;,
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208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound 11 (248.0 mg, 1 . 0mmol) and sodium iodide (180.0 mg, 1 . 2mmol) is added to methanol (10.0 ml) and stirring, and then adding substituted amine (2.1mmol) and heating to 40 C reaction 3 – 6 hours, TLC monitoring display complete raw material reaction, concentrated, column chromatography to obtain compound 12, wherein R4 With the corresponding product in the definition of the same.

208167-83-3, 208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Yang Chunhao; Miao Zehong; Yue Zhizhou; Liang Yukun; Feng Jianming; Li Jiaxin; He Qian; (30 pag.)CN104250246; (2017); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics