Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, Nitrobenzyl bromide and N- methyl piperazine after the substitutionreaction, and then get by stannous chloride reduction.

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

Reference£º
Patent; CHINA PHARMACEUTICAL UNIVERSITY; YANG, ZHAO; WANG, ZHIXIANG; FANG, ZHENG; GUO, KAI; WEI, PING; (23 pag.)CN103739550; (2016); B;,
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59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,59878-57-8

General procedure: To a solution of 14 (200 mg, 0.63 mmol) in DMA (60 mL), HOBt(170 mg, 1.26 mmol), EDCI (242 mg, 1.26 mmol), and DIPEA(0.208 mL, 1.26 mmol) and then the corresponding piperazine wereadded, and the mixture was stirred overnight. Water (10 mL) wasadded to the mixture, which was stirred for an additional 1 h. Then,the mixture was extracted with ethyl acetate (50 mL x 3). Thecombined organic layers were washed with brine, dried overanhydrous sodium sulfate and concentrated to give the crudeproduct, which was purified by column chromatography to affordthe corresponding compounds in good yields.

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chen, Wenhua; Guo, Ne; Qi, Minghui; Dai, Haiying; Hong, Minghuang; Guan, Longfei; Huan, Xiajuan; Song, Shanshan; He, Jinxue; Wang, Yingqing; Xi, Yong; Yang, Xinying; Shen, Yanyan; Su, Yi; Sun, Yiming; Gao, Yinglei; Chen, Yi; Ding, Jian; Tang, Yun; Ren, Guobin; Miao, Zehong; Li, Jian; European Journal of Medicinal Chemistry; vol. 138; (2017); p. 514 – 531;,
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Piperazines – an overview | ScienceDirect Topics

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

Step 1: Preparation of tert-butyl (2S)-4-[[2-fluoro-4-(morpholin-4-yl)phenyl]methyl]-2- methylpiperazine-l-carboxylate [00251] A 100-mL round-bottom flask was charged with 2-fluoro-4-(morpholin-4- yl)benzaldehyde (0.800 g, 3.82 mmol, 1.00 equiv), tert-butyl (2S)-2-methylpiperazine-l- carboxylate (0.840 g, 4.20 mmol, 1.10 equiv), and 1,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.40 g, 1 1.3 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with 0 (10 mL), and extracted with dichloromethane (3 x 10 mL). The organic layers were combined and washed with brine (50 mL), dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was chromatographed on a silica gel column with ethyl acetate/petroleum ether (25/75) to provide 1.40 g (93% yield) of ter/-butyl (2S)-4-[[2-fluoro-4-(morpholin-4-yl)phenyl]methyl]-2-methylpiperazine-l-carboxylate as a white solid. LCMS (ESI, m/z): 394 [M+H]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Cheryl, A.; JONES, Todd, K.; WANG, Dong-Hui; WEBER, Olivia; CRAVATT, Benjamin, F.; NIPHAKIS, Micah, J.; COGNETTA, Armand; CHANG, Jae Won; WO2013/142307; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step A: tert-Butyl (3S)-4- [2- (4-cyano-3-methoxyphenyl)-2-hydroxyethyl1 -3-(hydroxymethyl)piperazine- 1 -carboxylate: A Pyrex vessel was charged with magnetic stirring bar, (0.350 g, 2.00 mmol) of 2-methoxy-4-(oxiran-2-yl) benzonitrile, (0.457 g, 2.20 mmol) oftert-butyl (3S)-3-(hydroxymethyl)piperazine-1-carboxylate, and 6 mL of EtOH. Then it was introduced in the microwave reactor and irradiated at 150 C for 3 hr. Then the mixture was cooled to room temperature and the solvent was evaporated and the resulting residue was purified by column chromatography (silica gel, 1- 20% dichloromethane/MeOH) which afforded the title compound as a mixture of two diastereomers (1:1). LC/MS: (IE, m/z) [(M + 1) – t-Bu] =336.1., 314741-40-7

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
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350684-49-0, tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The mixture of compound 10a-10e (3.24 mmol), compound 9(1.04 g, 3.4 mmol), Pd(OAc)2 (0.11 g, 0.5 mmol), Xantphos (0.28 g,0.5 mmol), and K3PO41.38 g, 6.48 mmolin DMF (8 mL) was heated 22 h at 125 C under argon followed by cooling to roomtemperature.The mixture was extracted with dichloromethane(20 mL x 3), the combined organic phase was washed with water(15mL x 2), dried over anhydrous Na2SO4 and concentrated toafford the crude product. The crude product was purified by columnchromatography to obtain compounds 11a-11e.

350684-49-0, As the paragraph descriping shows that 350684-49-0 is playing an increasingly important role.

Reference£º
Article; Su, Yue; Li, Ridong; Ning, Xianling; Lin, Zhiqiang; Zhao, Xuyang; Zhou, Juntuo; Liu, Jia; Jin, Yan; Yin, Yuxin; European Journal of Medicinal Chemistry; vol. 177; (2019); p. 32 – 46;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 2: (S)-tert-butyl 2-methyl-4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indol-5-yl)piperazine-1-carboxylate To a solution of 5-bromo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indole (2 g, 6.13 mmol) and (S)-tert-butyl-2-methylpiperazine-1-carboxylate (1.23 g, 6.13 mmol) in toluene (20 mL) was added Pd2(dba)3 (281 mg, 0.31 mmol), BINAP (381 mg, 0.613 mmol), and t-BuONa (1.17 g, 12.26 mmol). The mixture was stirred at 80 C. for 5 hrs under nitrogen. The resulting mixture was concentrated in vacuo and the residue was purified by column chromatography on silica gel to give (S)-tert-butyl-2-methyl-4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indol-5-yl)piperazine-1-carboxylate (645 mg, 1.45 mmol, 16.5%) as a yellow liquid. ESI-MS (EI+, m/z): 446.4 [M+H]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics

54699-92-2,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.

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

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

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

5271-27-2, 1-Methyl-3-phenylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5271-27-2, Example 119 and 120lambda/-Cyclopropyl-4-methyl-3-[3-(4-methyl-2-phenyl-1-piperazinyl)-2-oxo-1(2H)- pyrazinylj-benzamide (Example 119) and 3-[5-bromo-3-(4-methyl-2-phenyl-1 – piperazinyl)-2-oxo-1(2H)-pyrazinyl]-lambda/-cyclopropyl-4-methyl-benzamide (Example 120).A mixture of 3-(3,5-dibromo-2-oxo-2/-/-pyrazin-1-yl)-4-methyl-benzoic acid, methyl ester (Example 1 b, 1 15 mg), 1-methyl-3-phenyl-piperazine (77 mg), lambda/,lambda/-diisopropylethylamine (0.1 mL) and tetrahydrofuran (1 mL) was heated within a microwave for 30 minutes at 100¡ãC before being cooled to room temperature. The mixture was transferred to a mixture of palladium on carbon (10percent, 50 mg) and tetrahydrofuran (1 mL) and 1 ,4-cyclohexadiene (1 mL) was added. The mixture was heated under atmosphere of nitrogen within a microwave for 2.5 h at 120¡ãC. An additional portion of palladium on carbon (50 mg) in tetrahydrofuran (1 mL) was added and the mixture was heated for 1 h at 120¡ãC. After cooling, cyclopropylamine (0.3 mL) was added followed by dropwise addition of a solution of /so-propylmagnesium chloride (2M in tetrahydrofuran, 2.5 mL). The mixture was stirred for 10 min. and quenched with sat. aqueous NH4CI and extracted into ethyl acetate. The organic phase was dried (Na2SO4), filtered and concentrated. Purification by preparative HPLC (Gemini column, 0.1 percent ammonia: acetonitrile eluent) afforded lambda/-cyclopropyl-4- methyl-3-(4-methyl-3′-oxo-2-phenyl-3,4,5,6-tetrahydro-2/-/,3’/-/-[1 ,2′]bipyrazinyl-4′-yl)- benzamide (49 mg) and 3-(6′-Bromo-4-methyl-3′-oxo-2-phenyl-3,4,5,6-tetrahydro-2/-/,3’/-/- [1 ,2′]bipyrazinyl-4′-yl)-lambda/-cyclopropyl-4-methyl-benzamide (8 mg).lambda/-Cyclopropyl-4-methyl-3-[3-(4-methyl-2-phenyl-1-piperazinyl)-2-oxo-1(2H)- pyrazinylj-benzamideMS: APCI(+ve) 444 (M+H+).1H NMR .5(DMSO-Cl6, 400MHz) 8.45 (1 H, m), 7.88-7.83 (1 H, m), 7.75 and 7.71 (1 H, 2 x d), 7.52 – 7.42 (3H, m), 7.37 – 7.28 (2H, m), 7.25 – 7.16 (1 H, m), 6.98 (2H, s), 6.17 and 6.07 (1 H, 2 x br s), 3.27 – 3.10 (1 H, m), 2.90 – 2.70 (2H, m), 2.48 – 2.37 (2H, m), 2.20 (3H, m), 2.15 (2H, m), 2.1 1 and 2.04 (3H, 2 x s), 0.69 (2H, m), 0.55 (2H, m).3-[5-Bromo-3-(4-methyl-2-phenyl-1-piperazinyl)-2-oxo-1(2H)-pyrazinyl]-lambda/- cyclopropyl-4-methyl-benzamideMS: APCI(+ve) 522 (M+H+). 1H NMR 5(DMSO-Cl6, 400MHz) 8.42 (1 H, m), 7.85 (1 H, m), 7.77 and 7.74 (1 H, 2 x d), 7.52 – 7.41 (3H, m), 7.37 – 7.28 (2H, m), 7.27 – 7.19 (2H, m), 6.28 and 6.16 (1 H, 2 x br s), 3.29 (3H, s), 3.18 – 3.03 (1 H, m), 2.89 – 2.72 (2H, m), 2.48 – 2.36 (1 H, m), 2.20 (3H, m), 2.15 and 2.07 (3H, 2 x s), 0.69 (2H, m), 0.55 (2H, m).

The synthetic route of 5271-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/1132; (2008); 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.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

To a mixture of 3-(4-chlorobenzoyl)propionic acid (31.9 g, 150 mmol), DMF (200 ml), and N-hydroxybenzotriazole (40.6 g, 301 mmol) was added a solution of N-ethyl-/V-(3-dimethylaminopropyl)carbodiimide hydrochloride (28.8 g, 150 mmol) in DMF (100 ml). The mixture was stirred at room temperature for 1.5 hour, and a solution of 1-cyclopentylpiperazine (23.2 g, 150 mmol) in DCM (100 ml) was added. The mixture was stirred at room temperature for 4 hours, concentrated under reduced pressure, and the residue was distributed between ethyl acetate (1.0 I) and a saturated, aqueous NaHCO3 solution (1.0 I). Phases were separated, the organic layer was dried (MgSO4), and concentrated, and the residue was redissolved in 1 molar aqueous hydrochloric acid (150 ml). The solution was concentrated, and the residue was dried by coevaporation with ethanol. Recrystallization of the residue from ethanol yielded 31.1 g (54%) of the title compound. Concentration of the mother liquor gave additional 19.4 g (34%) of product., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference£º
Patent; Dorwald, Florencio Zaragoza; Andersen, Knud Erik; Sorensen, Jan Lindy; US2004/19039; (2004); A1;,
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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

Di-tert-butyl azodicarboxylate (0.478 g, 2.08 mmol) was added portionwise to a mixture of product step 6 (1.66 mmol), the appropriate alcohol (1.74 mmol), and triphenyl-phosphine (0.544 g, 2.08 mmol) in dichloromethane (20 mL) at r.t. If necessary, further alcohol was added. After stirring for 2 h, the solution was concentrated to 10 mL, mounted on silica and chromatographed (gradient, dichloromethane to dichloromethane_methanol=3:2) to obtain the desired ethers (73%).The compound was synthesised according to GP 4 from 4-chloro-7-hydroxy-6-methoxy-quinazoline and 3-(4-methylpiperazin-1-yl)-propan-1-ol. LC/ESI-MS: m/z=351 [M+H]., 5317-33-9

5317-33-9 3-(4-Methylpiperazin-1-yl)propan-1-ol 79208, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; 4SC AG; US2006/135782; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics