Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.

Step 2. 4-(4-Amino-phenyl)-piperazine-1-carboxylic acid tert-butyl ester [0166] A mixture of 4- (4-NITRO-PHENYL)-PIPERAZINE-1-CARBOXYLIC acid TERT-BUTYL ester (11) (18. 9 MMOL), 10% palladium-on-carbon (600mg), ethanol (100 mL), and ethyl acetate (100 mL) is hydrogenated at room temperature and 40 psi for 2 hrs. The mixture is filtered through celite, washing with ethyl acetate (2 x 100 mL), and concentrated in vacuo to give 4- (4-AMINO-PHENYL)-PIPERAZINE-1-CARBOXYLIC acid tert-butyl ester (12) as a brown oil.

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

Reference£º
Patent; CELLULAR GENOMICS, INC.; WO2005/14599; (2005); A1;,
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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.

The 4- chloropyrimidine SG2-022 was prepared using the previously reported method.1 A solution of 2,4-dichloro-5-trifluoromethylpyrimidine (120 mg, 0.550 mmol) in i-BuOH/DCM (1:1, 4 mL) was cooled to 0 C. Zinc chloride (1 M in diethyl ether, 0.633 mL, 0.633 mmol) was added dropwise over 10 minutes at 0 C and the solution stirred at the same temperature for 30 minutes. A solution of iPatent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE, INC.; SCHOeNBRUNN, Ernst; LAWRENCE, Nicholas J.; LAWRENCE, Harshani R.; (293 pag.)WO2017/66428; (2017); A1;,
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5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Method 20 Synthesis of 3-[1-(4-iodophenyl)-1,2-dimethyl-propyl]-1-[2-(4-methylpiperazin-1-yl)ethyl]indole (Intermediate 26) To a solution of I-11 (150 mg, 0.39 mmol) in anhydrous DMF (4.5 mL) is added NaH (60percent dispersion in mineral oil) (18 mg, 0.46 mmol). The mixture is stirred at room temperature for 10 minutes and then methanesulfonyl chloride (0.032 mL, 0.42 mmol) is added and stifling continued for 18 h. The reaction is retreated with more methane sulfonyl chloride (0.03 mL) and NaH (60percent dispersion in mineral oil) (18 mg) and stirring is continued for another 2 h before quenching with water. The reaction is partitioned between saturated aqueous NaHCO3 and DCM. The combined organics are washed with brine, dried over anhydrous Na2SO4, and concentrated in vacuo to give I-25 (193 mg). To a solution of 1-(2-hydroxyethyl)-4-methylpiperazine (54 mg, 0.37 mmol) in toluene (3 mL) is added NaH (60percent dispersion in mineral oil) (18 mg, 0.45 mmol) and the suspension stirred at room temperature for 10 min. A solution of I-25 (175 mg, 0.37 mmol) in toluene (1.5 mL) is added and the reaction heated to 110¡ã C. for 3 h. A further 1 eq of 1-(2-hydroxyethyl)-4-methylpiperazine and 1.2 eq of NaH are added and heating continued for 3 h. The reaction is quenched by dropwise addition of water and extracted with DCM. The combined organics are washed with water and brine, and dried over anhydrous Na2SO4. The solvent is removed in vacuo and the crude material purified by flash chromatography (SiO2, 2percent MeOH in DCM) to give the title intermediate I-26 (52 mg) m/z 516.1 [M+H].

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BARTOLOZZI, Alessandra; CHEN, Zhidong; DINES, Jonathon Alan; LO, Ho Yin; LOKE, Pui Leng; OLAGUE, Alan; RIETHER, Doris; TYE, Heather; WU, Lifen; ZINDELL, Renee M.; US2013/196967; (2013); A1;,
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109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: These amines were required for the syntheses of 4 and 20 respectively. To a solution of 4-nitrobenzylchloride (1 mmol) in anhydrous THF (3 mL) was added 1-methylpiperazine or piperidine (1 mmol) and triethylamine (1.5 mmol, 0.21 mL). The solution was heated at 70 C overnight. The reaction mixture was then extracted with dichloromethane and water. The organic fractions were combined, dried over anhydrous Na2SO4, and concentrated under reduced pressure. The residue was purified by column chromatography (hexane/EA 1:4) and characterized by 1H NMR (Supplementary Information). It was dissolved in 10 mL ethanol, PtO2 (0.01 g) was added under nitrogen. Hydrogenation was carried out on a Parr hydrogenator at 50 psi for 16 h. The catalyst was then removed by filtration and the filtrate was concentrated in vacuo to give the amine in quantitative yield.

109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various.

Reference£º
Article; Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2917 – 2929;,
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13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: In the nitrogen atmosphere of the glove box, 3.33 mg of ruthenium complex 1c was dissolved in 50 mL of tetrahydrofuran. After stirring, a catalyst 1c stock solution was formed. 1 ml of the above solution was added to a 125-mL Parr autoclave (0.067 mg, 0.0001 mmol). 1c), And added 9mL of tetrahydrofuran, Morpholine (8.712 g, 100 mmol). After the autoclave is sealed, it is taken out of the glove box. The carbon dioxide gas and hydrogen gas were each charged at 40 atm. The reaction system is heated to 120 C in an oil bath. The pressure rises to about 120 atm, After stirring for 181 hours, The reactor was then cooled to room temperature in a water bath. Slowly release the remaining gas in the fume hood, A pale yellow liquid was obtained. P-xylene (200 muL) was added to the mixture as an internal standard. The yield of N-formylmorpholine was determined by gas chromatography to be 94%.

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

Reference£º
Patent; Chinese Academy Of Sciences Shanghai Organic Chemistry Institute; Ding Kuiling; Qiu Jia; Yan Tao; Zhang Lei; Wang Zheng; (49 pag.)CN109553641; (2019); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 39 GENERAL PROCEDURE: NUCLEOPHILIC DISPLACEMENT WITH 2-CHLORO-3- NITRO-PYRIDINE; Piperazine (2-5 mmol) and 2-chloro-3-nitro-pyridine (1 mmol) were dissolved in DMF or acetonitrile (2-3 mL) and stirred for 5 min at room temperature. A slight exothermic was observed shortly after addition of the solvent. When TLC analysis showed that the reaction was complete, the mixture was diluted with dichloromethane, and washed with water. The organic layer was dried, filtered and concentrated, then chromatographed in 10% methanol in dichloromethane to yield the desired product.

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2005/80356; (2005); A1;,
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655225-01-7, tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

ethyl (7R,21S)-17-{2-[4-(tert-butoxycarbonyl)piperazin-1-yl]ethyl}-19-chloro-1-(4-fluorophenyl)-20-methyl-16-oxo-10-{[2-(3,3,3-trifluoropropoxy)pyrimidin-4-yl]methoxy}-7,8,16,17-tetrahydro-15H-18,21-etheno-13,9-(metheno)-6,14-dioxa-2-thia-3,5,17-triazacyclononadeca[1,2,3-cd]indene-7-carboxylate Example 16L (67.1 mg) was dissolved in N,N-dimethylformamide (0.8 mL). tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate (35.2 mg) and cesium carbonate (78.0 mg) were added. The reaction mixture was stirred at ambient temperature for 40 minutes. The mixture was diluted with ethyl acetate and water. The organics were separated, dried over anhydrous sodium sulfate, filtered, and concentrated. The residue was purified by silica gel chromatography on an AnaLogix IntelliFlash280 system (50-100percent ethyl acetate/heptanes, linear gradient) to provide the title compound. LC/MS (APCI) m/z 1050.3 (M+H)+.

The synthetic route of 655225-01-7 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;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.474711-89-2,Piperazine-1-carboxamide hydrochloride,as a common compound, the synthetic route is as follows.

Example 179 4-[6-(3-Methyl-1-trityl-1H-4-pyrazolyl)-4-quinolyl]-1-piperazine carboxamide A mixture of 150 mg 6-(3-methyl-1-trityl-1H-pyrazolyl)-4-quinolyl trifluoromethane sulfonate obtained in Production Example 91, 83 mg 1-piperazinecarboxamide hydrochloride, 105 mg triethylamine and 10 ML anhydrous tetrahydrofuran was heated overnight under reflux.. Then, 5 ML dimethyl sulfoxide was added to the reaction solution, and the solution was stirred at 80C for 2 days.. The reaction solution was cooled to room temperature, then ethyl acetate, water and brine were added thereto, and the organic layer was separated, washed twice with water and then with brine, and dried over anhydrous magnesium sulfate.. The drying agent was evaporated, and the residue was purified by silica gel column chromatography (hexane/ethyl acetate), to give 96 mg of the title compound as a pale yellow amorphous.1H-NMR (CDCl3) delta: 2.55(s, 3H), 3.24(m, 4H), 3.68(m, 4H), 4.60(brs, 2H), 6.85(d, J=5.2Hz, 1H), 7.24(m, 7H), 7.33 (m, 8H), 7.53 (s, 1H), 7.65(dd, J=8.8,1.6Hz, 1H), 8.00(d, J=1.6Hz, 1H), 8.01(d, J=8.8Hz, 1H), 8.70(d, J=5.2Hz, 1H)

474711-89-2 Piperazine-1-carboxamide hydrochloride 2769700, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Eisai Co., Ltd.; EP1382603; (2004); 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.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

A solution of sodium-2-ethylhexenoate (0.32 g) in ethyl acetate (5 mL) was added to a mixture of 2-((lH-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5, 5-dimethyl-3,4,5,6-tetrahydro[l,l’-biphenyl]-2-yl)methyl)piperazin-l-yl)benzoic acid (1.0 g) in ethyl acetate (5 mL) and stirred at 20-30 degree Celsius. The resulting slurry was filtered, washed with ethyl acetate (5 mL) and the solid was dried under vacuum at 50- 55 degree Celsius for 16 h to furnish sodium 2-((lH-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4- (4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro[l,r-biphenyl]-2-yl)methyl)piperazin-l- yl)benzoate. Yield: 57.80% (0.6g) HPLC Purity: 96.97% 1H NMR (DMSO-d6): d q.93 (s, 6H), 1.37 (t, J= 6.4 Hz, 2H), 1.96 (s, 2H), 2.16 (t, br, 2H) 2.21 (m, 4H), 2.73 (s, 2H), 2.97 (s, 4H), 6.26 (dd, J=2.0, 1.2 Hz, 2H), 6.57 (dd, J=L6, 2.0, Hz, 1H), 7.05 (d, J=8.4, 2H), 7.29 (d, J=2.8 Hz, 1H), 7.34 (d, J=8.4 Hz, 2H), 7.38 (t, J=2.8 Hz, 1H), 7.45 (d, J=8.8 Hz, 1H), 7.94 (d, J=2.8 Hz, 1H), 11.49 (s, 1H, NH).

1235865-77-6 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid 66713100, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; FRESENIUS KABI ONCOLOGY LTD.; GUPTA, Chandan Kumar; DHIMAN, Navdeep; SANGHANI, Sunil; SINGH, Govind; LAHIRI, Saswata; CABRI, Walter; GUPTA, Nitin; (0 pag.)WO2020/3272; (2020); A1;,
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5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

0.36 g of N- [4-tert-butyl-5- (4-methoxybenzylthiazolyl) -2-yl] -2-chloroacetamideAnd 5 mL of tetrahydrofuran were added and stirred at room temperature, 0.24 g of pyridine and 0.23 g were added N-ethylpiperazine; reaction overnight, desolvation, plus dichloromethane,Saturated with salt water, dried over anhydrous sodium sulfate,Plus petroleum ether precipitation solid, suction filter, petroleum ether wash,Dried to give a pale yellow solidN- [4-tert-butyl-5- (4-methoxybenzylthiazolyl) -2-yl]2- (N-ethylpiperazinyl) acetamide in a yield of 65.1%

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hunan University; Hu Aixi; Ding Na; Ye Jiao; (15 pag.)CN106938989; (2017); A;,
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Piperazines – an overview | ScienceDirect Topics