Heterocyclic Building Blocks-piperazine

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.,314741-40-7

Step E: tert-butyl(3S)-4-[2-(5-cyano-4-methylthiophen-3-yl)-2-hydroxyethyl]-3-(hydroxymethyl)piperazine-1-carboxylate: A mixture of 3-methyl-4-(oxiran-2-yl) thiophene-2-carbonitrile (1.3 g, 7.9 mmol) and tert-butyl (3S)-3-(hydroxymethyl)piperazine-1-carboxylate(2.0 g, 9.5 mmol) in 5 mL ofEtOH was heated in a microwave apparatus at 140 C for 90 minutes and then cooled down. The reaction mixture was concentrated, and the residue waspurified by column chromatography (DCM : MeOH = 10 :1) to afford the title compound.

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

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
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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.

2,4-Dichloro-5-(trifluoromethyl)pyrimidine (2.39 g, 11.0 mmol) was stirred in a 1 :1 f- BuOH: ,2-dichloroethane mixture (80 mL) at 0 C and a 1 .0 M ZnCI2 solution in diethyl ether (12.6 mL, 12.6 mmol) was added cautiously over 20 minutes and the reaction was left stirring at 0 C for 30 minutes. A solution of ferf-butyl 4-(4- aminophenyl)piperazine-1-carboxylate (/2) (2.92 g, 10.5 mmol) in 1 :1 f-BuOH.1 ,2- dichloroethane (40 mL) was added drop-wise over 15 minutes at 0 C followed by a solution of triethylamine (1.76 mL, 12.6 mmol) in 1 : 1 f-BuOH: 1 ,2-dichloroethane (40 mL) and the reaction was allowed to warm to room temperature and was stirred for 18 hours. The organic solvents were evaporated in vacuo and the crude yellow oily solid was suspended in water (400 mL), the suspension was sonicated for 30 minutes and the product was collected by filtration, the solid was washed with water (10 x 20 mL) and dried under a high vacuum to give the title compound (13) (4.75 g, 98% yield) as a beige solid; 1H NMR (400 MHz, oVDMSO) delta 10.45 (s, 1 H), 8.72 (s, 1 H), 7.50 (d, J = 8.5 Hz, 2H), 6.96 (d, J = 9.0 Hz, 2H), 3.50 – 3.42 (m, 4H), 3.09 – 3.02 (m, 4H), 1 .42 (s, 9H). LCMS Method C: H 6.56 min; m/z 456.2, 458.1 [M-H]”.

170911-92-9, The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CANCER THERAPEUTICS CRC PTY LIMITED; HOLMES, Ian, Peter; BERGMAN, Ylva; LUNNISS, Gillian Elizabeth; NIKAC, Marica; CHOI, Neil; HEMLEY, Catherine Fae; WALKER, Scott Raymond; FOITZIK, Richard Charles; GANAME, Danny; LESSENE, Romina; WO2012/110773; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example Al 6; a) Preparation of intermediate 43; A mixture of intermediate 11 (0.918 g; 3 mmol), EDCI (0.843g; 4.4 mmol), HOBt (0.594 g; 4.4 mmol) and 10 ml of DMF was stirred at room temperature for 15 minutes. Phenylacetic acid hydrazide (1 g; 6.65 mmol) was added. The mixture was stirred at room temperature for 18 hours. The solvent was evaporated. The residue was stirred in water and extracted with CH2Cl2. The organic layer was dried, filtered and evaporated. The residue was purified by reversed-phase high-performance liquid chromatography (Shandon Hyperprep C 18 BDS (Base Deactivated Silica) 8 mum, 250 g, LD. 5 cm). A gradient with the following mobile phases was applied. Phase A: a 0.25 % NH4HCO3 solution in water; phase B (optional): CH3OH; phase C: CH3CN). The desired fractions were collected and the solvent was evaporated. The residue was dried, yielding 0.802 g of intermediate 43., 162046-66-4

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148840; (2008); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

70261-82-4, A solution of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid (154 mg, 0.605 mmol), TBTU (232 mg, 0.725 mmol), 4-[(4-methylpiperazin-1-yl)methyl]aniline (150 mg, 0.725 mmol) and DIPEA (0.155 mL, 0.907 mmol) inDMA (7 mL) was let under stirring at rt overnight. The mixture was diluted with EtOAc, washed with a saturated solution of NaHCO3, water and brine, dried over Na2SO4, filtered and taken to dryness under reduced pressure. After treatment with Et20, the solid was filtered and used without any further purification.HRMS (ESI+): calcd. for 025H35BN303 [M + H] 436.2766; found 436.2762.

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; CASALE, Elena; CORTI, Emliana; GNOCCHI, Paola; NESI, Marcella; ORRENIUS, Sten, Christian; QUARTIERI, Francesca; RICCARDI SIRTORI, Federico; (138 pag.)WO2018/19681; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

77290-31-4, tert-Butyl 4-(cyanomethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

77290-31-4, Step B: Tert-butyl 4-(lH etrazoi-5-ylmethyl)piperazine-l-carboxylate (i-18); To a stirred suspension of 1.50 g (6.66 mmol) of the title compound from Step A above in 25 mL of anhydrous toluene was added 1.38 g (10.0 mol) of triethylaminehydrochloride followed by 0.65 g (10 mmol) of sodium azide. The resuling mixture was heated to 80 C for 12 h then cooled to ambient temperature. All volatiles were removed in vacuo, and the residue suspended in 5 mL of brine and 1.0 N aqueous hydrogen chloride solution was added until pH of ~4 was achieved. The aqueous phase was extracted with chloroform and the combined organics were dried over magnesium sulfate and evaporated to dryness in vacuo. The residue was purified by silica gel chromatography eluting with a 0-100% acetone in hexanes gradient to afford the title compound (i-18) as white solid (1.1 g, 63%). 1H-NM (500 MHz, DMSOPatent; MERCK SHARP & DOHME CORP.; MORRIELLO, Gregori, J.; WENDT, Harvey, R.; EDMONDSON, Scott, D.; WO2012/12314; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57184-25-5, 1-(Cyclopropylmethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,57184-25-5

First, 5-amino-2-(2-furyl)[1,2,4]triazolo[1,5-c]pyrimidine-7-carboxylic acid (500 mg, 2.04 mmol) produced in Example 77 was dissolved in DMF (50 mL), and 4-cyclopropylmethylpiperazine (429 mg, 3.06 mmol), 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide monohydrochloride (782 mg, 4.08 mmol), and 1-hydroxybenzotriazole (312 mg, 2.04 mmol) were added to the resulting solution, followed by stirring at room temperature for 12 hours. Then, THF (30 mL), acid chloride resin [3.0 g, the acid chloride resin being prepared by the method described in the document (Tetrahedron Letters, Vol. 37, No. 40, p. 7193 (1996))] and polyvinylpyridine resin (produced by Aldrich Co., 3.0 g) were added to the reaction solution, followed by further stirring at room temperature for 12 hours. The resins were filtered off from the reaction solution, and the filtrate was concentrated. The residue was recrystallized from a mixed solvent of ethanol (10 mL) and DMF (10 mL) to obtain Compound 96 (420 mg, 1.14 mmol) as white crystals in a yield of 56%.1H NMR (delta ppm, DMSO-d6): 8.18 (brs, 2H), 7.95 (d, J=1.7 Hz, 1H), 7.22 (d, J=3.3 Hz, 1H), 7.00 (s, 1H), 6.73 (dd, J=3.3 Hz, 1.7 Hz, 1H), 3.50-3.65 (m, 2H), 3.40-3.45 (m, 2H), 2.40-2.50 (m, 4H), 2.21 (d, J=6.6 Hz, 2H), 0.83 (m, 1H), 0.43-0.49 (m, 2H), 0.06-0.08 (m, 2H) Mass (m/z): 368 (M++1) IR (KBr, cm-1): 1656, 1641, 1633, 1616, 1610, 1558, 1003 [] Elemental Analysis: as C18H21N7O2¡¤0.4 H2OObservedC 57.56%,H 5.95%,N 26.59%CalculatedC 57.71%,H 5.87%,N 26.17%Melting point: 299.2 – 299.8C

As the paragraph descriping shows that 57184-25-5 is playing an increasingly important role.

Reference£º
Patent; KYOWA HAKKO KOGYO CO., LTD.; EP1544200; (2005); 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.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 a solution of 3-iodo-4-methylbenzoyl chloride obtained above in dry DCM (10mL) at 0C was added Et3N (0.28mL, 2.0mmol) and 4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) aniline (328mg, 1.2mmol). The mixture was stirred at room temperature for 5h, and then the solvent was removed under reduced pressure. The residue was purified by using column chromatography to afford the corresponding product 6-1 (439mg, 2 steps yield: 85%)., 694499-26-8

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

Reference£º
Article; Liu, Yang; Peng, Xia; Guan, Xiaocong; Lu, Dong; Xi, Yong; Jin, Shiyu; Chen, Hui; Zeng, Limin; Ai, Jing; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 122 – 132;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics