Downstream synthetic route of 76003-29-7

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

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

Step A1, 1 -dimethylethyl 4-[2~fluoro~4-(methyloxy)phenyl]-3-oxo-1-piperazinecarboxylate A mixture of 1-Boc-3-oxopiperazine (500 mg, 2.497 mmol), 4-bromo-3- fluoroanisole (512 mg, 2.497 mmol), copper(l) iodide (23.78 mg, 0.125 mmol), frans-Nu,Nu’- dimethylcycIohexane-1 ,2-diamine (0.039 mL, 0.250 mmo.), and potassium carbonate (690 mg, 4.99 mmol) in 1 ,4-dioxane (10 mL) was heated at 120 C for 3.5 days. The mixture was filtered through a pad of Celite and washed with EtOAc (50 mL). The filtrate was washed with saturated aqueous NH4CI (15 mL), brine (15 mL), dried ( gS04), filtered and concentrated. The crude was absorbed on silica gel and purified by silica gelchromatography (10-60% EtOAc in hexanes) to give 1 ,1 -dimethylethyl 4-[2-fluoro-4- (methyloxy)phenyl]-3-oxo~1 -piperazinecarboxylate (581.9 mg, 1 .794 mmol, 72 %) as white solid. MS(ESI) m/z: 325.3 (MH+).

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; MAYNARD, Andy; MILLER, John; PATTERSON, Dan; PEAT, Andrew, James; POWERS, Jeremiah; PRICE, Daniel, J.; ROBERTS, Chris; TAI, Vincent; YOUNGMAN, Michael; WO2011/50284; (2011); A1;,
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New learning discoveries about 120737-59-9

As the paragraph descriping shows that 120737-59-9 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Methyl-bromoacetate (3.06g, 20.0 mmol) was added to a stirred solution of 4-Boc-2-methyl- piperazine (2. [0G,] 10.0 mmol), sodium iodide [(0.] [LG.)] and N, N-diisopropylethylamine (3.48 ml, 20 mmol) in DCM (50ml) at ambient temperature under nitrogen. After stirring for 16h the reaction mixture was washed with water [(30ML),] brine [(30ML),] dried and evaporated to dryness under reduced pressure. The residue was purified by chromatography on silica, eluting with 0-8percent [MEOH/DCM] to give 68 as a yellow oil (2.7g). MS-ESI: 273 (M++H). [H NMR (CDC13) 1. 05] (d, 3H), 1.47 (s, 9H), 2.50-2. 85 (m, 4H), 3.03-3. 13 (m, 1H), 3.34 (d, 1H), 3.44 (d, [1H),] 3.70 (s, 3H), 3.71-3. 82 (m, 2H)., 120737-59-9

As the paragraph descriping shows that 120737-59-9 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/18480; (2004); A1;,
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Brief introduction of 3022-15-9

3022-15-9, The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

Piperazine-2-carboxyilc acid dihydrochloride (5.00 g, 24.6 mmol) was dissolved in H2O (80 mL) and 1,4-dioxane (80 mL), and the solution was brought to pH 11 with 50% aqueous NaOH. A solution of di-tert-butyl dicarbonate (5.36 g, 30.8 mmol) in 1,4-dioxane (40 mL) was added dropwise while maintaining the pH at 11 with 50% aqueous NaOH. After 12 h, the reaction mixture was extracted with Et2O (3 x 125 mL). The aqueous layer was brought to pH 2 with concentrated HCl and was extracted with EtOAc (4 x 100 mL). The aqueous solution was brought to pH 9.5 with 50% aqueous NaOH. Benzyl chloroformate (3.70 mL, 24.6 mmol) was added at 10 0C while maintaining the pH at 9.5 with 50% aqueous NaOH. The solution was allowed to warm to rt. After 2 h, the reaction mixture was extracted with Et2O (2 x 100 mL), brought to pH 1 with concentrated HCl, and extracted with EtOAc (3 x 150 mL). The combined EtOAc extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure. The thick oil was dissolved in THF (100 mL) and cooled to 00C. Borane-THF complex (1.0 M solution in THF, 75 mL, 75 mmol) was added portionwise. After 1 h, the reaction mixture was heated to 50 0C. After 1 h, the reaction mixture was cooled to rt and quenched carefully with MeOH. After evolution of gas ceased, additional MeOH (100 mL) was added and the reaction mixture was heated to 70 0C for 1 h. Upon cooling to rt, the reaction mixture was concentrated under reduced pressure. Purification by column chomatography (20 to 40% EtOAc in Hexanes gradient) gave 4.52 g (52%) of the title compound. Rf = 0.25 in 50% EtOAc/Hexanes; LC-MS: RT = 9.53 min; [M+Na]+ = 373.1; 2.068 g (22%) of dibenzyl 2-(hydroxymethyl)piperazine-l,4-dicarboxylate was also obtained. Rf = 0.18 in 50% EtOAc/Hexanes; LC-MS: RT = 9.47 min; [M+H]+ = 385.1.

3022-15-9, The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 1-Boc-3,3-Dimethylpiperazine

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

tert-butyl 3,3-dimethylpiperazine-1-carboxylate (19.90 g, 92.86 mmol) and (2,2-dimethylpiperazin-1-yl)methanone hydrochloride (Intermediate II) (27.87 g, 84.60 mmol) were dissolved in DMF (300 mL) before HATU (35.45 g, 93.23 mmol) and DIPEA (27.72 g, 37.36 mL, 214.5 mmol) were added. The solution was stirred at room temperature for 3h, and then water was added dropwise. The aq. phase was extracted three times with EtOAc. The combined organic phase was washed with water and brine. The organic phase was then dried over Na2SO4, filtered and the filtrate evaporated under reduced pressure. The crude product was purified passing through a pad of silica gel (25%-33% EtOAc/hexanes affording the title product (34.28 g, 91% yield) as a yellow orange foamy solid, which was used directly in the next step. 1H NMR (400 MHz, Chloroform-d) 7.34 (s, 1H), 7.06 (s, 1H), 3.84 (dd, J = 6.6, 4.8 Hz, 2H), 3.67 – 3.45 (m, 4H), 2.71 (tt, J = 10.3, 5.5 Hz, 1H), 1.85 – 1.77 (m, 4H), 1.77 – 1.71 (m, 1H), 1.57 – 1.51 (m, 2H), 1.49 (s, 9H), 1.49 (s, 9H), 1.43 – 1.31 (m, 3H), 1.01 (s, 3H), 0.97 (s, 3H). ESI-MS m/z calc.525.3567, found 526.61 (M+1)+; Retention time: 3.15 minutes using method A

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; SAYEGH, Camil Elie; STURINO, Claudio; FOURNIER, Pierre-Andre; LACOSTE, Jean-Eric; DIETRICH, Evelyne; MARTEL, Julien; VALLEE, Frederic; (494 pag.)WO2016/154075; (2016); A1;,
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Analyzing the synthesis route of 169448-17-3

As the paragraph descriping shows that 169448-17-3 is playing an increasingly important role.

169448-17-3, (S)-tert-Butyl 2-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Tert-butyl-dimethyl-silyl chloride (3.62 g, 24.02 mmol) and imidazole (3.27 g, 48.03 mmol) were added to a solution of the compound of step 2 (4.609 g, 20.01 mmol) in 75 ml of DCM and the resulting solution was stirred at room temperature for 3 h. The mixture was washed with 50 ml of water and then 50 ml of brine. The aqueous phase was extracted once with DCM. The combined organic phases were dried over sodium sulfate, filtered and evaporated under reduced pressure to give 6.90 g of the title compound as a pale yellow oil., 169448-17-3

As the paragraph descriping shows that 169448-17-3 is playing an increasingly important role.

Reference£º
Patent; SANOFI-AVENTIS; STEINHAGEN, Henning; SCHEIPER, Bodo; MATTER, Hans; MCCORT, Gary; BEGIS, Guillaume; GOBERVILLE, Pascale; THIERS, Berangere; WO2011/12538; (2011); A1;,
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Analyzing the synthesis route of (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

314741-40-7, 4-Methyl-5-oxiran-2-yl-2-benzofuran- 1 (3H)-one (3.00 g, 15.8 mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine (5.12 g. 23.7 mmol) were suspended in ethanol (10 mL) in a 20 m microwaye tube. The reaction mixture was degassedand heated in a microwaye apparatus for 30 min at 150C. The reaction mixture was eyaporated to dryness, then chromatographed through a 330g Redi-sep column and eluted with a solyentsystem of 1:1 EtOAc/hexane to 100% EtOAc to yield the title compound. LC-MS : M+1= 407.

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DE JESUS, Reynalda, Keh; DING, Fa-xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; SHAHRIPOUR, Aurash; PIO, Barbara; TANG, Haifeng; WALSH, Shawn; WO2014/126944; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

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.

General procedure: General procedure for the synthesis of 15b-15u. To a solution ofcompound 13a (0.41 g, 1.06 mmol) in 2-butanol (5 mL), 1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-amine (0.196 g, 1.27 mmol)and trifluoroacetic acid (94 mL) were added in a sealed tube. Thereactionwas heated at 95 C for 18 h. The reaction mixturewas thenallowed to cool to room temperature. The mixture was transferredto a round-bottom flask and then the solvent was removed underreduced pressure. The residue was dissolved in DCM (2.0 mL) andTFA (2.0 mL), and the resulting mixture was stirred for 5 h at roomtemperature. The solvent was removed under reduced pressure,and the residue was neutralized with saturated NaHCO3 aqueoussolution. The water layer was extracted with DCM. The organiclayer was combined and washed with brine, dried over Na2SO4,filtered, concentrated, and purified by silica gel chromatography toafford 15a as a yellow solid (0.264 g, 65% for two steps)., 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Yu, Lei; Huang, Minhao; Xu, Tianfeng; Tong, Linjiang; Yan, Xiao-e; Zhang, Zhang; Xu, Yong; Yun, Caihong; Xie, Hua; Ding, Ke; Lu, Xiaoyun; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 1107 – 1117;,
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Piperazines – an overview | ScienceDirect Topics

Brief introduction of 55121-99-8

55121-99-8, The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

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.

General procedure: To a solution of9(0.16g,0.58mmol) ini-PrOH(5mL),substituted phenylamine(0.64mmol)wasadded. The reaction mixture was stirred at reflux for4h under N2atmosphere. After the reaction was completed, the mixture wasnaturally cooled to room temperature.Themixture was filtered and the solid was collectedto giveintermediate12or15. 1.2.1 (4-((6-Bromoquinazolin-4-yl)amino)phenyl)(4-methylpiperazin-1-yl)methanone (12a)Yellow solid; yield:73 %.MS (ESI)m/z: [M+H]+=426.1/428.1.

55121-99-8, The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Xin, Minhang; Hei, Yuan-Yuan; Zhang, Hao; Shen, Ying; Zhang, San-Qi; Bioorganic and Medicinal Chemistry Letters; vol. 27; 9; (2017); p. 1972 – 1977;,
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Piperazines – an overview | ScienceDirect Topics

Brief introduction of 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 48.1: 2-(2-Methyl-piperazin-1-yl)-nicotinonitrile. A mixture of 3 -methyl-pip erazine-1-carboxylic acid tert-butyl ester (1.00 g, 5.00 mmol), 2-chloro-nicotinonitrile (1.04 g, 7.48 mmol), triethylamine (2 mL) and tetrahydrofuran (8 mL) was heated at 80¡ã C overnight. The reaction mixture was cooled to room temperature and dichloromethane (300 mL) and aqueous saturated sodium bicarbonate (75 mL) were added. The aqueous mixture was separated and extracted further with dichloromethane (2×150 mL), The combined organic layer was washed with water (150 mL), washed with brine (100 mL), dried over sodium sulfate, filtered and concentrated. The residue was dissolved in dichloromethane (10 mL) and trifluoroacetic acid (10 mL) was added. The reaction mixture was stirred at room temperature for 2.5 hours and then concentrated. The residue was dissolved in 1,2-dichloroethane (5 mL) and the mixture was then concentrated. To the residue was added saturated aqueous sodium bicarbonate (150 mL). The mixture was extracted with dichloromethane (3×100 mL) and the combined organic layer was washed with water (50 mL), washed with brine (50 mL), dried over sodium sulfate, filtered and concentrated. The residue was purified on silica gel using dichloromethane:2M ammonia in methanol (95:5 to 92.5:7) to give 2-(2-methyl-piperazin-l- yl)-nicotinonitrile (48 mg, 5 percent). 1H NMR (300 MHz, CDCl3): delta(ppm) 8.33 (dd, IH), 7.76 (dd, IH), 6.71 (m, IH)3 4.62 (m, IH), 4.03 (bd, IH), 3.35 (m, IH), 3.10 (m, 2H)1 2.90 (m, 2H), 1.75 (bs, IH), 1.34 (d, 3H)., 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2008/112440; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about tert-Butyl 4-aminopiperazine-1-carboxylate

118753-66-5, As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: To a well-stirred solution of intermediate 5 (2g, 5.6mmol) in C2H5OH(60mL) was added a drop of AcOH. The resulted mixture was refluxed for 0.5h. Then intermediates 8a (2.95g) was added, followed by stirring for 10hat the same temperature. After cooled to room temperature, The resulting solid was collected by filtration and dried to give the target compounds 9a as a light yellow solid in 82% yield.

118753-66-5, As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

Reference£º
Article; Wu, Yachuang; Ding, Xiudong; Ding, Liang; Zhang, Yongsheng; Cui, Lei; Sun, Lu; Li, Wei; Wang, Di; Zhao, Yanfang; European Journal of Medicinal Chemistry; vol. 158; (2018); p. 247 – 258;,
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Piperazines – an overview | ScienceDirect Topics