Heterocyclic Building Blocks-piperazine

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2- (5-amino-2- (furan-2-yl) -8H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-8-yl) pentanoic acid (50 mg, 0.15 mmol) , 1- (2, 4-difluorophenyl) piperazine (32 mg, 0.16 mmol) , HATU (69 mg, 0.18 mmol) and DIEA (39 mg, 0.3 mmol) in DMF (5 mL) was stirred at rt for 2 hrs. The solution was added with water (5 mL) , extracted with ethyl acetate (10 mL) and washed with brine (10 mL) . The organic layer was dried, concentrated and purified by column chromatography (PE: EA = 1: 1) to get the desired product (49 mg, 64%) .1H NMR (400 MHz, DMSO-d6) delta 8.76 (s, 1H) , 7.95 (s, 1H) , 7.66 (br. s, 2H) , , 7.19-6.96 (m, 4H) , 6.74-6.73 (m, 1H) , 5.71-5.67 (m, 1H) , 3.78-3.65 (m, 4H) , 2.94-2.83 (m, 4H) , 2.19-1.99 (m, 2H) , 1.33-1.17 (m, 2H) , 0.92 (t, J = 8.0 Hz, 3H) ppm. MS: M/e 522 (M+1)+

115761-79-0, As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference£º
Patent; BEIGENE, LTD.; ZHANG, Guoliang; SUN, Hanzi; ZHOU, Changyou; (253 pag.)WO2020/20097; (2020); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 77; 4-{2-[4-(4-Methanesulfonylphenyl)piperazin-l-yl]ethylidene}piperidine-l- carboxylic acid tert-butyl ester; To a solution of 4-(2-hydroxyethylidene)piperidine-l-carboxylic acid tert-butyl ester (2.2g, 9.7mmol) in DCM (25mL) was added Et3N (2.02mL, 14.5mmol) and the reaction cooled to O0C. To this cooled mixture was added methanesulfonylchloride (0.98mL, 12.6mmol) dropwise. The reaction was stirred at O0C for 20 min then treated with saturated NaHCO3 solution. The two layers were separated and the organic layer washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by flash chromatography with 10% EtOAc / Hexane as eluent to afford 4-(2-chloroethylidene) piperidine-1-carboxylic acid tert-butyl ester and 4-vinyl-3,6-dihydro-2H-pyridine-l-carboxylic acid tert-butyl ester in a 1:1 ratio (0.95Og). The mixture was dissolved in DMF (5mL) and treated with TBAI (0.068g, 0.18mmol). This suspension was thus added to a preformed mixture of l-(4-methanesulfonylphenyl)piperazine (0.487g, 2.03mmol) and sodium hydride (0.1 Ig of a 60% dispersion in mineral oil, 2.77mmol) in DMF (5mL) at rt. The mixture was allowed to stir for 2h then treated with water. The aqueous was extracted with EtOAc and the combined organic layers washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by HPLC to afford the title compound (0.27g, 6%): RT = 2.41 min; m/z (ES+) = 450.2 [M+ H]+, 187669-60-9

As the paragraph descriping shows that 187669-60-9 is playing an increasingly important role.

Reference£º
Patent; PROSIDION LIMITED; WO2007/3964; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of IV-II-l-c (28 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-l- yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in 1.2 mL of t-BuOH was heated at 100 0C in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The dichloromethane was removed in vacuo and the resulting crude product was purified by preparative TLC with 3.5 N ammonia methanol solution and dichloromethane (1/25, v/v) to give the title compound IV-I (8 mg). 1H NMR (600 MHz, CDCl3) delta 8.32 (s, IH), 8.18 (d, J= 8.4 Hz, IH), 7.80 (dd, J= 1.8, 7.8 Hz, IH), 7.61 (s, IH), 7.51 (dd, J= 1.8, 7.8 Hz, IH), 7.40-7.34 (m, 2H), 6.54 (dd, J= 1.8, 8.4 Hz, IH), 6.52 (d, J= 1.8 Hz, IH), 3.85 (s, 3H), 3.55 (s, 3H), 3.23 (s, br, 4H), 2.69 (s, br, 4H), 2.43 (s, 3H). MS (ESI) m/z 463 (M+H)+.

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; DANA FARBER CANCER INSTITUTE; GRAY, Nathanael, S.; DENG, Xianming; KWIATKOWSKI, Nicholas, Paul; WO2010/80712; (2010); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Under an argon atmosphere,2,6-Dibromo-3-nitropyridine (1.18 g, 4.20 mmol) was added to a solution ofWas dissolved in ethanol (20 mL).there Tert-butyl 4- (4-aminophenyl) piperazine-1-carboxylate (1.40 g, 5.04 mmol)Triethylamine (1.14 mL, 8.40 mmol) was added,And the mixture was stirred at room temperature for 18 hours.The resulting precipitate was collected by filtration,After washing with a small amount of ethanol and hexane,And dried to give the title compound (1.91 g, 95%)

170911-92-9, 170911-92-9 tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 11011301, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; YAKULT HONSHA COMPANY LIMITED; ABE, ATSUHIRO; MAE, MASAYUKI; YAMAZAKI, RYUTA; SASAI, TOSHIO; NISHIYAMA, HIROYUKI; NAGAOKA, MASATO; MATSUZAKI, TAKESHI; (47 pag.)JP6023630; (2016); B2;,
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76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

76003-29-7, In reference to the process disclosed in WO2012/031004, 2-nitro-5-bromopyridine (1.01 g, 5.0 mmol), tert-butyl 2-oxo-4-piperazinecarboxylate (1.00 g, 5.0 mmol, and cesium carbonate (3.26 g, 10.0 mmol) were suspended in 1,4-dioxane, and the suspension was bubbled with nitrogen gas for 30 minutes. To the suspension was added Xantphos (246 mg, 0.43 mmol) and tris(dibenzylideneacetone)dipalladium (229 mg, 0.25 mmol), and the mixture was stirred under reflux for two hours. The resultant reaction mixture was cooled to room temperature, and water and ethyl acetate were then added to the mixture, followed by filtration with Celite. The organic phase was separated from the filtrate, and the aqueous phase was extracted with ethyl acetate. The resultant organic phases were combined together and dried over anhydrous sodium sulfate, and the resultant solid was separated by filtration. The filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography to yield the title compound (1.08 g, 67%). 1H-NMR (CDCl3) delta: 8.67 (1H, d, J=2.4 Hz), 8.32 (1H, d, J=8.8 Hz), 8.15 (1H, dd, J=8.8, 2.4 Hz), 4.33 (2H, s), 3.93-3.83 (4H, m), 1.51 (9H, s)

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; Teijin Pharma Limited; MIZUNO, Tsuyoshi; SHIMADA, Tomohiro; UNOKI, Gen; EBISAWA, Masaru; TAKEUCHI, Susumu; MINAMIZONO, Kunio; SASAKI, Kosuke; YOKOSAKA, Takuya; IGARASHI, Junji; MARUYAMA, Akinobu; TAKAHASHI, Hiroshi; HORIE, Kyohei; SAKAI, Yuri; (447 pag.)EP3305785; (2018); A1;,
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169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Chloro-2-fluoro-l-nitrobenzene (0.5 g, 2.85 mmol), (S)-tert-b tyl 2-methylpiperazine-l- carboxylate (0.856 g, 4.27 mmol), and DIEA (0.995 mL, 5.70 mmol) were dissolved in DCM (20 mL). The reaction was stirred at reflux overnight. The mixture was concentrated and the residue was purified by chromatography (0 – 30% EtOAc hexanes) to give the title compound (1.0 g, 98%). LCMS mlz = 356.4 [M+H]+; NMR (400 M Hz, DMSO – d6) delta ppm 1.16 (d, 7 = 6.87 Hz, 3H), 1.41 (s, 9H), 2.76 – 2.90 (m, 1H), 2.97 – 3.23 (m, 4H), 3.66 – 3.79 (m, 1H), 4.12 – 4.23 (m, 1H), 7.18 (d, 7 = 8.65 Hz, 1H), 7.32 – 7.40 (m, 1H), 7.85 (d, 7 = 8.90 Hz, 1H)., 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; ARENA PHARMACEUTICALS, INC.; TRAN, Thuy-Anh; KRAMER, Bryan Aubrey; SHIN, Young-Jun; WO2014/182673; (2014); A1;,
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694499-26-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

General procedure: To amixture of substituted benzoic acid obtained in the last step (0.12 mmol) in 5mL DMF, 2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluroniumhexafluorophosphate (HATU, 0.18 mmol), ethyldiisopropylamine (DIPEA, 0.24 mmol)and 4-((4-methylpiperazin-1-yl)methyl)-3- (trifluoromethyl)aniline (0.1 mmol)was added. The resulting mixture was stirred at room temperature overnight. Thenthe reaction was extracted with ethyl acetate, washed with brine, dried overanhydrous Na2SO4, filtered and concentrated to give thecrude product, which was further purified by column chromatography to affordthe final compounds.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Article; Han, Mei; Li, Shan; Ai, Jing; Sheng, Rong; Hu, Yongzhou; Hu, Youhong; Geng, Meiyu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 23; (2016); p. 5679 – 5684;,
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182618-86-6, 1-Boc-4-(4-Nitrophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

10 g (32.6 mmol) of crude I-e was added to a 500 mL one-necked flask,FeO (OH) / C catalyst 1.0 g and 95% ethanol 100 mL,Heating reflux,A 10 mL mixture of hydrazine hydrate and 20 mL of 95% ethanol were slowly added dropwise,TLC detection of raw materials disappeared (methanol:Chloroform = 1:15). Hot filter,The filter cake was washed twice with hot ethanol (30 mL x 2)The solvent was evaporated under reduced pressure to give a white solid,And dried in vacuo to give 7.86 g of (I-f) in a yield of 87.1%.Products without further purification, directly into the next step., 182618-86-6

The synthetic route of 182618-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; China Pharmaceutical University; Lu Shuai; Wang Yue; Zhi Yanle; Yao Chao; Lu Tao; Li Baoquan; Chen Puzhou; Bao Jiyin; (27 pag.)CN107245073; (2017); A;,
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30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A dichloromethane solution (6mL) of an appropriate piperazine (1 eq) and triethylamine (3 eq) was added drop wise to a suspension of 2-chloro-N-(5-nitrothiazol-2-yl)acetamide (1) in 5mL CH2Cl2 and the reaction was kept at room temperature under a nitrogen atmosphere and stirring for 48h. The reaction solvent was evaporated and the residue was redissolved in ethyl acetate. The inorganic salts were filtered away and the residue was chromatographed on preparative TLC silica gel plates with ethyl acetate/petroleum ether as eluent to obtain the desired pure product as a powder or crystals. Purity was also checked by HPLC and it was ?95%. Orange powder (55%): mp 173-175C; 1H NMR (400MHz, (CDCl3) delta: 8.33 (s, 1H), 7.51 (d, J=8.4Hz, 2H), 6.96 (d, J=8.4Hz, 2H), 3.40 (s, 2H), 3.38 (t, J=5.2Hz, 4H), 2.82 (t, J=5.2Hz, 4H). HRESIMS calcd for C16H16N8O4S m/z [M+H]+ 416.1010, found 416.1005, 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; Papadopoulou, Maria V.; Bloomer, William D.; Rosenzweig, Howard S.; Wilkinson, Shane R.; Szular, Joanna; Kaiser, Marcel; European Journal of Medicinal Chemistry; vol. 117; (2016); p. 179 – 186;,
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300543-56-0, (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2 g of R-I- ( (4-chlorophenyl) (phenyl) methyl) piperazine and 0.88 g of diglycolic acid anhydride were dissolved in 10 ml of dimethylsulphoxide . To the solution 20 ml of tetrabutylammo- nium bromide were added. The solution was stirred for another 10 hours until the reaction was completed. The solution was diluted with 67 ml of water and 15 ml of isopropyl acetate were added. The phases were separated and the water layer was reextracted with isopropyl acetate. The organic layer was mixed with demineralised water (40 ml) and the pH of the suspension was adjusted to 10 with 2 M NaOH. The layers were separated and to the water phase 40 ml of isopropyl acetate were added. The pH of the suspension was adjusted to 3.5. The layers were separated and the water phase was reextracted twice with isopropylacetate . The organic phase was rinsed with water and evaporated to dryness. 2.5 g of product (HPLC (area) was 98.5 %) ) was crystallised. The product was dried at vacuum at 500C., 300543-56-0

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

Reference£º
Patent; KRKA, tovarna zdravil, d.d., Novo Mesto; WO2009/150147; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics