Heterocyclic Building Blocks-piperazine

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.

In a 100-mL three necked round bottom flask equipped with magnetic stirrer, thermometer, condenser, charged 15 mL of 2-[(1H-Pyrrolo[2,3-b]pyridine-5-yl)oxy]-4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl]methyl]piperazin-1-yl]benzoic acid in THF (assay: 1 g, 1.75 mmol), heated up to 50-55C and 0.4 mL (5.25 mmol) trifluoroacetic acid in THF (2 mL) was added. The reaction mixture was stirred for 30 min at 50-55C and n-heptane (25 mL) was added dropwise at this temperature. The reaction mixture was cooled to 0-5C, stirred for 30 min and filtered. The wet cake was washed with n-heptane (2.5 mL) and dried under vacuum at 40- 45C overnight to obtain desired compound (assay: 0.85 g, 85%, TFA: 14.8%)., 1235865-77-6

As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference£º
Patent; ASSIA CHEMICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; POTARINE JUHASZ, Zsuzsa; STRUBA, Szabolcs; NEMETHNE RACZ, Csilla; TOTH, Zoltan Gabor; SZILAGYI, Andrea; KERTI-FERENCZI, Renata; MOLNAR, Sandor Janos; PASZTOR-DEBRECZENI, Nora; HAJKO, Janos; (100 pag.)WO2017/156398; (2017); A1;,
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122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0105] To a solution of compound 7 (260 mg, 0.6 mmol) inbutan-2-ol (1 mL) were added 2-methoxy-4-( 4-methylpiperazin-1-yl)aniline (133 mg, 0.6 mmol) and trifluoroacetic acid( 48 flL, 0.6 mmol). The reaction mixture was heated to 110C. and reacted in a sealed tube for 24 h, diluted by DCM,washed by saturated NaHC03 solution, washed by saturatedbrine, dried by anhydrous Na2S04 , evaporated the solventunder reduced pressure, and then purified by colunm chromatographyto yield a yellow solid (151 mg, 44%).[0106] 1H NMR (400Hz, CDCI3 ) o 7.99 (s, lH), 7.48 (d,1=7.5 Hz, lH), 7.44 (s, lH), 7.41 (t, 1=8.0 Hz, lH), 7.35 (s,lH), 6.97 (d, 1=7.5 Hz, lH), 6.63 (s, lH), 6.42 (d, 1=2.0 Hz,lH), 6.16 (d, 1=6.4 Hz, lH), 4.42 (s, 2H), 3.80 (s, 3H), 3.22(m, 4H), 3.08 (s, 3H), 2.79 (m, 4H), 1.47 (s, 9H).[01 07]

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; GUANGZHOU INSTITUTE OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES; Ding, Ke; Chang, Shaohua; Xu, Shilin; Zhang, Lianwen; Tu, Zhengchao; Ding, Jian; Geng, Meiyu; Chen, Yi; US2014/296216; (2014); A1;,
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262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add to the reaction flask(E) -4 – [(2-methoxybenzylidene)Methyl acetate-2-yl]3-nitrobenzoate (III) (3.71 g, 10 mmol),N- (4-aminophenyl) -N-methyl-2- (4-methylpiperazin-1-yl)Acetamide (IV)(2.88 g, 11 mmol)And 50 mL of N, N-dimethylformamide, the temperature was raised to 80-85 C, and the reaction was stirred for 2 hours.The mixture was cooled to room temperature, pyridine (5 mL) was added and the mixture was stirred at room temperature for 2 hours.The reaction solution was poured into 150 mL of water to precipitate a solid. Filtered, the crude product recrystallized from ethanol,A yellow solid was obtained(Z) -4 – {[2- (N-methyl-2- (4-methylpiperazin-1-yl)Acetamidanilide) benzylidene]Methyl-2-yl} -3-nitrobenzoate (V)4.32 g, yield 71.9%., 262368-30-9

262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Suzhou Mirac Pharma Technology Co.,Ltd; Xu, Xuenong; (7 pag.)CN104262232; (2016); B;,
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4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of 3-(4-Isopropylpiperazin-1-yl)benzaldehyde (3): A mixture of 2-(3-bromophenyl)-1,3-dioxane (2, 1.58 g, 6.5 mmol), 1-isopropylpiperazine (1.0 g, 7.8 mmol), rac-BINAP (60 mg, 0.096 mmol), and tert-BuONa (1.06 g, 11.1 mmol) in toluene (15 mL) was degassed under vacuum and flushed with nitrogen. Pd2(dba)3 (30 mg, 0.033 mmol) was added. The reaction mixture was degassed again and flushed with nitrogen and was heated at 100¡ã C. under nitrogen for 16 h. The reaction mixture was poured into cold 1N HCl (30 mL) and stirred for 2 h. It was adjusted to pH 8 with 6N NaOH and extracted with EtOAc (3*50 mL). The combined organic layers were dried (MgSO4), filtered, concentrated, and purified by silica gel chromatography eluting with 0-100percent EtOAc (containing 5percent v/v Et3N) in hexanes to afford the title compound as a viscous yellow oil (1.32 g, 87percent): 1H NMR (500 MHz, CDCl3) delta 9.96 (s, 1H), 7.44-7.37 (m, 2H), 7.34-7.30 (m, 1H), 7.21-7.16 (m, 1H), 3.28 (t, J=5.0 Hz, 4H), 2.73 (sept, J=6.5 Hz, 1H), 2.69 (t, J=5.0 Hz, 4H), 1.10 (d, J=6.5 Hz, 6H); ESI MS m/z 233 [M+H]+.

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; RVX Therapeutics Inc.; Fairfax, David John; Duffy, Bryan Cordell; Martin, Gregory Scott; Quinn, John Frederick; Liu, Shuang; Wagner, Gregory Steven; Young, Peter Ronald; US2014/142102; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.

4-Cyclopropylmethyl-piperazine-1-carboxylic Acid 4-[2-(4-chloro-phenyl)-ethylcarbamoyl]-phenyl Ester The title compound was prepared from 4-[2-(4-chloro-phenyl)-ethylcarbamoyl]-phenyl chloroformate and 1-cyclopropylmethyl-piperazine, yield 18%. White crystals, m.p. 225-226 C.; IR (KBr): nu 1710 (ester C=O), 1661 (amide C=O) cm-1.

57184-25-5, 57184-25-5 1-(Cyclopropylmethyl)piperazine 965875, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); A1;,
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142-64-3, Piperazine Dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: General procedure for the synthesis of compounds (8a, 8b).A solution of anhydrous piperazine (5, 8.6 g, 0.1 mol) and piperazine dihydrochloride (6, 31.8 g 0.2 mol) in ethanol (80 mL) were heated with vigorous stirring at 75 C for 2 h. Then a solution benzylchloride (13.9 g, 0.11 mol) or benzoyl chloride (15.4 g,0.11 mol) was added dropwise over a period of 40 min to the hotsolution. The reaction mixture was refluxed for another 2 h, the progress of the reaction was monitored by TLC. The mixture wascooled and the precipitated piperazine dihydrochloride 6 was collected and washed three times with ethanol. The filtrate combined with the washes was concentrated in vacuo to give the N-benzylpiperazineor N-benzoylpiperazine hydrochloride which was then treated with 6 M NaOH to pH > 12. The aqueous layerof crude N-benzylpiperazine or N-benzoylpiperazine was extractedinto CH2Cl2 (3 50 mL). The combined organic extracts were driedover Na2SO4 and concentrated in vacuo. The crude oily product was purified by flash column chromatography on silica gel (MeOHCH2Cl21:3) to give 8a (18.4 g, 95%) or 8b (17.8 g, 94%)., 142-64-3

142-64-3 Piperazine Dihydrochloride 8893, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Wang, Jin; Xia, Fei; Jin, Wen-Bin; Guan, Jin-Yan; Zhao, Hang; Bioorganic Chemistry; vol. 68; (2016); p. 214 – 218;,
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314741-39-4, (S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,314741-39-4

1-tert-Butyl 3-methyl (3S)-piperazine-1,3-dicarboxylate (10 g, 40.9 mmol), (4-fluorophenyl)boronic acid (11.5 g, 82.1 mmol), copper(II) acetate (7.44 g, 40.9 mmol) and pyridine (6.67 ml, 82.6 mmol) were suspended in anhydrous 1,2-dichloroethane (300 ml) and the mixture was stirred at ambient temperature for 72 hours. A continuous airflow was bubbled through the reaction and the mixture stirred for 44 hours at ambient temperature. The airflow was removed and the reaction stirred at 45 C. for 20 hours, then cooled to ambient temperature. The mixture was filtered through celite, washed with DCM. The filtrate was concentrated in vacuo and the green oil obtained was purified via flash column chromatography eluting with gradient from 0-100% EtOAc in heptane followed by 0-100% MeOH in EtOAc. The product containing fractions were combined and concentrated in vacuo to afford the title compound as a yellow oil (4.29 g, 29%). 1H NMR (500 MHz, Chloroform-d) delta 6.98-6.92 (m, 2H), 6.85-6.80 (m, 2H), 4.47 (d, J=12.7 Hz, 1H), 4.27 (s, 1H), 4.21-3.92 (m, 1H), 3.64 (s, 3H), 3.60-3.47 (m, 1H), 3.37 (d, J=10.6 Hz, 1H), 3.27-2.99 (m, 2H), 1.46 (s, 9H). LCMS Method 3 Tr=1.88 min, (ES+) (M+H+)339.1.

As the paragraph descriping shows that 314741-39-4 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (2018); A1;,
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548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

548762-66-9, To a stirred solution of tert-butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate (0.5 g, 2.33 mmol) in acetonitrile (10 mL) were added sodium bicarbonate (0.98 g, 11.67 mmol) and 1-bromo-4-(1-bromoethyl)-2-fluorobenzene (0.66 g, 2.33 mmol) at room temperature. The reaction mixture was heated at 80 C for 12 h. The reaction mixture was cooled to room temperature and the solvent was removed under reduced pressure to obtain the crude product, which was purified by flash column chromatography (Column: 24 g silica; Solvent run: 40-45% EtOAc in petroleum ether) to obtain a diastereomeric mixture of tert-butyl (2S,5R)-4-(1-(4-bromo-3-fluorophenyl)ethyl)-2,5- dimethylpiperazine-1-carboxylate (0.3 g, 27 % yield) as an off-white solid. LCMS: m/z, 416.2 (M+2); retention time 3.55 min. (LC-MS Method info: Column-KINETEX- XB- C18 (75 x 3 mm- 2.6 ^m ); Mphase A: 10 mM ammonium formate in water: acetonitrile (98:2); Mphase B: 10 mM ammonium formate in water: acetonitrile (2:98); Gradient: 20- 100% B over 4 minutes, flow rate 1.0 mL/min, then a 0.6 minute hold at 100% B flow rate 1.5 mL/min; then Gradient: 100-20% B over 0.1 minutes, flow rate 1.5 mL/min).

The synthetic route of 548762-66-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); 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.1403898-64-5,(2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation 5: (2R,5R)-4-Benzyl-5-hydroxymethyl-2-methyl-pi perazi ne-I -carboxylic acidtert-butyl ester A mixture of (2 R,5R)-5-hydroxymethyl-2-methyl-piperazine- 1 -carboxylic acid tert-butyl ester(3.48 g, 15.1 mmol), benzaldehyde (1.76 g, 16.6 mmol), sodium triacetoxyborohydride (3.84 g,18.1 mmol) and 1,2-dichloroethane (30 mL)was stirred at2O c for 18 h, then partitionedbetween saturated aqueous NaHCO3 (150 mL) and DCM (3 x 50 mL). Combined organic extracts were dried (Na2SO4) then evaporated in vacuo to give an oil. Chromatography (Si02, 0- 30% EtOAc in petrol) gave the title compound (4.588 g, 74%) as a colourless solid. MS:[M+H] = 321., 1403898-64-5

The synthetic route of 1403898-64-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; BUCK, Ildiko Maria; DAY, James Edward Harvey; HOWARD, Steven; SAXTY, Gordon; MURRAY, Christopher William; HOPKINS, Anna; WO2014/60767; (2014); A1;,
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70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,70261-82-4

[00456] The title compound was prepared according to synthesis procedure B described above from 2-chloro-4-(3-chloro-4-fluorophenyl)-5-methylpyrimidine and 4-((4- methylpiperazin-l-yl)methyl)aniline in 84% yield (yellow solid) after purification by flash chromatography (CH2C12/CH30H 99: 1 gradually increasing to 95:5). 1H NMR (400 MHz, CDC13): delta 8.30 (s, 1H), 7.70 (m, 1H), 7.56 (d, 2H, J = 8.6 Hz), 7.51 (m, 1H), 7.25 (d, 2H, J: not calculated due to overlapping peaks), 7.05 (s, 1H), 3.46 (s, 2H), 2.46 (bs, 8H), 2.28 (s, 3H), 2.25 (s, 3H); MS (ESI): 426.3 [M+H]+, 213.7 [M+2H]2+.

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

Reference£º
Patent; UNIVERSITY OF UTAH RESEARCH FOUNDATION; BEARSS, David, J.; VANKAYALAPATI, Hariprasad; MOLLARD, Alexis; WARNER, Steven, L.; SHARMA, Sunil; WO2012/135800; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics