Month: August 2020

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;,
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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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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 B: tert-butyl(9aS)-3-hydroxy-3-( 1 -oxo-3.4-dihydro- 1H-isochromen-6- yl)hexahydropyrazino [2,1-c] [1,41 oxazine-8( 1H)-carboxylate: 6- (Bromoacetyl)-3 ,4-dihydro- 1H- isochromen-1-one (-.1.54 g, -.5.72 mmol, presence of cx-chloroketone was noted, -.10%) and commercially available (S)-4-N-BOC-2-hydroxymethylpiperazine (1.24 g, 5.72 mmol) were added to a round bottom flask and diluted with THF (50 mL). Diisopropylethylamine (1.30 mL,7.44 mmol) was then introduced and the mixture left stirring for 14 h at RT during which time a considerable amount of solid had formed. The reaction mixture was diluted with EtOAc, then washed with saturated NH4C1aq followed by H20. Both aqueous layers were sequentially back extracted once with another portion of EtOAc, the organics were then combined, dried with MgSO4, filtered, and concentrated in vacuo. The recovered crude product was subjected topurification by flash chromatography (Biotage, 50% EtOAc/Hex) to afford the title compound

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; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
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694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

After taking the two 50mL round bottom flask was added sequentially aniline compound 5 (1.10mmol), NaNO2 (2.21mmol), ultrapure water (20 mL), the system was cooled to 0 deg.] C, was slowly added dropwise HCl (3.30mmol) in 5mL aqueous solution The After the addition, maintain the temperature of the reaction system continue to react 1.5h. It was then slowly added dropwise an aqueous solution of NaN3 (1.32mmol). After the addition was complete, maintainingThe reaction temperature of the reaction system, 3h, TLC monitored the reaction. After completion of the reaction, a saturated NaHCO3 solution was added 20mL, extracted with ethyl acetate 30mL ¡Á 2, combined organic phases were dried over anhydrous Na2SO4, and concentrated to give azide 6 directly administered next.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Tianjin International Bio-pharmaceutical Joint Institute; Rao Zihe; Bai Cuigai; Yang Cheng; Chen Yue; Li Huiying; Wang Lei; Gao Yuan; Yang Juan; Sun Tao; Zhong Chuanke; (26 pag.)CN106749278; (2017); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

A mixture of 4-((4-ethylpiperazin- 1 -yl)methyl)-3-(trifluoromethyl)aniline (Intermediate Cl)(500 g, 1.74 mmol) and methyl 3-hydroxybenzoate (Intermediate B2) (317 mg, 1.91 mmol)in anhydrous THF (5.0 mL) was cooled to -20 C and added potassium tert-butoxide (1M, 10 mL, 10.44 mmol). The mixture was stirred at RT for 3 h. The reaction mixture was cooled to-20 C and quenched with saturated sodium bicarbonate solution. The aqueous mixture was extracted twice with ethyl acetate and the combined organic layers were washed with waterfollowed by brine. The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated to yield 220 mg of the desired product. ?H NMR (400 MHz, DMSO-d6) oe 0.98 (t, J = 6.8 Hz, 3H), 2.31-2.50 (m, 8H), 2.51 (br s, 2H), 3.56 (s, 2H), 6.98-7.01 (br d, 1H), 7.3 1-7.35 (m, 2H), 7.39 (d, J = 6.4 Hz, 1H), 7.69 (d, J = 8.8 Hz, 1H), 8.03 (d, J = 8.4 Hz, 1H), 8.21 (s, 1H), 9.79 (s, 1H), 10.42 (s, 1H); ESI-MS (m/z) 408 (M+H).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics