Heterocyclic Building Blocks-piperazine

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 6-chloro-4-cyclopropyl-7-fluoro-1-oxo-1,4-dihydronaphthalene-2-carboxylic acid 1a (1 g, 3.5 mmol) with N-ethylpiperazine 2c (0.6 g, 5.25mmol) was loaded in a small flask fitted with a micro condenser, placed in the microwave reactor and irradiated for 25 min at 150C under solvent free conditions. The reaction progress was monitored by TLC. Upon completion of the process, addition of hot absolute ethanol (10 mL) to the reaction mixture was followed by filtration. The filtrate was concentrated and stored at room temperature for precipitation. The solid was filtered off and recrystallized from absolute ethanol to give compound 3c., 5308-25-8

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

Reference£º
Article; Mirzaie; Lari; Vahedi; Hakimi; Russian Journal of General Chemistry; vol. 86; 12; (2016); p. 2865 – 2869; Zh. Obshch. Khim.; vol. 86; 12; (2016); p. 2865 – 2869,5;,
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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,4318-42-7

General procedure: A mixture of the intermediates 3a-3e (5 mmol) and corresponding secondary amine 4a-4g (5.5 mmol) was added in CH3CN (20 ml) at the presence of anhydrous K2CO3 (6 mmol). The mixture was heated at 65 ¡ãC for 6-10 h. The solvent was evaporated in vacuo. The residue was dissolved in CH2Cl2 (25 mL), washed with water (20 mL ¡Á 3), and the combined organic phases were washed with saturated aqueous NaCl (30 mL), dried over sodium sulfate, and filtered. The solvent was evaporated under reduced pressure. The residue was purified on a silica gel chromatography using mixtures of petroleum/acetone as eluent to get the target products TM-1~TM-28.

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Sang, Zhipei; Wang, Keren; Wang, Huifang; Yu, Lintao; Wang, Huijuan; Ma, Qianwen; Ye, Mengyao; Han, Xue; Liu, Wenmin; Bioorganic and Medicinal Chemistry Letters; vol. 27; 22; (2017); p. 5053 – 5059;,
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196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of 4-thiocarbamoyl-piperazine-1 -carboxylic acid tert-butyl ester (13.3 mmol) in ethanol (60 ml) was added 4-(2-bromoacetyl)-benzoic acid (13.3 mmol) and 4- methylmorpholine (13.9 mmol). The reaction was heated at reflux for 2.5 h. The reaction was concentrated in vacuo and the solid washed with water (200 ml) to yield the title compound as a white solid (3.9 g). 1 H NMR (400MHz, CDCI3) 1.45 (9H, s), 3.58 (8H, m), 4.86 (1 H, s), 6.95 (1 H,s), 7.97 (2H, d, J 8 Hz), 8.1 (2H, d, J 8Hz).

196811-66-2, 196811-66-2 tert-Butyl 4-carbamothioylpiperazine-1-carboxylate 12093220, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MEDIVIR AB; WO2007/6714; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, To a solution of tert-butyl piperazine-1-carboxylate (2.00 g, 10.7 mmol) in 5 wt % aq NaHCO3 (36 mL) and DCM (36 mL) was added 2-bromoacetyl bromide (1.40 mL, 16.1 mmol) at 0 C. The reaction mixture was stirred at 0 C. and then at room temperature for 2 hours. After separation of phase, the organic layer was washed with water, 2 N aq. HCl, water and brine, dried over Na2SO4, filtered and concentrated in vacuo. The residual solid was purified by recrystallization from EtOAc and hexanes to afford tert-butyl 4-(2-azidoacetyl)piperazine-1-carboxylate (2.92 g, 89%) as a white solid. 1H-NMR (CDCl3, Varian, 400 MHz): delta 1.47 (9H, s), 3.42-3.44 (2H, m), 3.46-3.54 (4H, m), 3.58-3.60 (2H, m), 3.86 (2H, s).

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; HANDOK INC.; CMG Pharmaceutical Co., Ltd.; Kim, Moonsoo; Lee, Chaewoon; Lee, Gilnam; Yoon, Cheolhwan; Seo, Jeongbeob; Kim, Jay Hak; Lee, Minwoo; Jeong, Hankyul; Choi, Hyang; Jung, Myung Eun; Lee, Ki Nam; Kim, Hyun Jung; Kim, Hye Kyoung; Lee, Jae Il; Lee, MinWoo; Kim, Misoon; Choi, Soongyu; (124 pag.)US2016/168156; (2016); A1;,
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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

Compound 340 was synthesized from compound 306 using General Method 2. To a microwave vessel were added 3-bromo-6-(3-(4-methylpiperazin-l-yl)azetidin-l-yl)pyrazolo[l,5-a]pyrimidine (80 mg, 0.23 mmol), cyclopropyl(piperazin-l-yl)methanone (49 mg, 0.32 mmol), Pd2(dba)3 (21 mg, 0.023 mmol), t-BuXPhos (39 mg, 0.091 mmol), sodium tert-butoxide (66 mg, 0.68 mmol) and toluene (3 ml). The vessel was purged with nitrogen for 1 min, sealed and subjected to microwave irradiation for 3 hr. The mixture was partitioned between EtOAc and water. The organic layer was separated, washed with brine and dried over Na2S04. After the removal of solvent under vacuum, the residue was directly purified through preparative HPLC to give desired product 339. LC/MS (method 2): tR= 2.92 min, m/z (M + H)+ = 425.4., 59878-57-8

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; THE BRIGHAM AND WOMEN’S HOSPITAL, INC.; THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; YU, Paul, B.; HUANG, Wenwei; SANDERSON, Philip, Edward; JIANG, Jian-kang; SHAMIM, Khalida; ZHENG, Wei; HUANG, Xiuli; TAWA, Gregory; LEE, Arthur; ALIMARDANOV, Asaf; HUANG, Junfeng; (357 pag.)WO2018/200855; (2018); A1;,
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630125-91-6,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.

To a solution of 4-bromo-2- (difluoromethyl) aniline (100 mg 0.450 mmol) in THF (10 mL) was added triphosgene (46.8 mg 0.158 mmol) . The resulting mixture was stirred at 70 . After 30 min LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo to give 4-bromo-2- (difluoromethyl) -1-isocyanatobenzene (110mg 0.417 mmol 93yield) . To a solution of 4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) aniline (153 mg 0.532 mmol) Et3N (0.124 mL 0.887 mmol) and DMAP (10.84 mg 0.089 mmol) in THF (10 mL) was added a solution of 4-bromo-2- (difluoromethyl) -1-isocyanatobenzene (110 mg 0.444 mmol) in THF (10 mL) . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo. The residue was purified by preparative TLC (DCM/MeOH 10/1) to yield a solid of 1- (4-bromo-2- (difluoromethyl) phenyl) -3- (4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) phenyl) urea (130 mg 0.172 mmol 38.9yield) 1HNMR(400 MHz CD3OD) delta 7.86 (s 1H) 7.75 (d J 8.8 Hz 1H) 7.67-7.63 (m 4H) 7.03-6.76 (m 1H) 3.67 (s 2H) 3.20-3.18 (m 2H) 2.96 (m 8H) 1.30 (m 3H) ES-LCMS m/z 535.1 537.1 (M+H)

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R & D COMPANY LIMITED; CHEUNG, Mui; DEMARTINO, Michael P.; EIDAM, Hilary Schenck; GUAN, Huiping Amy; QIN, Donghui; WU, Chengde; GONG, Zhen; YANG, Haiying; YU, Haiyu; ZHANG, Zhiliu; (391 pag.)WO2016/37578; (2016); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

31166-44-6, To a solution of benzyl piperazine-1 -carboxylate (1 .10 g, 4.99 mmol) and 1 -bromo-3-diethoxyphosphoryl-propane (1 .29 g, 4.99 mmol) in CH3CN (40.00 mL) was added K2003 (1 .38 g, 9.98 mmol). The reaction mixture was stirred at 75 00 overnight and then EtOAc (50 mL) and water (30 mL) were added. The layers were separated, and the aqueous phase was extracted again with EtOAc (20 mLx2). The combined organic phases were washed with brine (40 mL), dried over anhydrous Mg504, filtered andconcentrated. The residue was purified by flash column chromatography on silica gel to afford Compound 15.la (EtOAc/MeOH=50:1) to afford (1.80 g, 4.52 mmol, 91percent yield) as an oil. 1H NMR (400 M, ODd3), oe7.35 (m, 5H), 5.13 (s, 2H), 4.12 (m, 4H), 3.52 (m, 4H), 2.42 (m, 6H), 1.78 (m, 4H), 1.32 (m, 6H).

31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; UNITY BIOTECHNOLOGY, INC.; BACKES, Bradley; W. VON GELDERN, Thomas; CHEN, Bing; (121 pag.)WO2017/101851; (2017); 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.

This was obtained by stirring MA2-004 (0.698 g) and 4-(4-i170911-92-9, As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference£º
Patent; 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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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.27561-62-2,Cyclohexyl(piperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

General procedure: 10mM sulfochloride hydrochloride was suspendedin 50 ml ethylacetate and 11mM amine component wasadded with stirring. 2.8 ml triethylamine dissolved in 10 ml ethylacetatewas dropped in with stirring and kept stirring overnight atambient temperature. The reaction mixture was extracted threetimes with water, the organic phase was dried over sodium sulfatefiltered, and then evaporated to dryness. For cases in which an oilyproduct was obtained, the residue was treated with diisopropylether., 27561-62-2

As the paragraph descriping shows that 27561-62-2 is playing an increasingly important role.

Reference£º
Article; Singh, Vinayak; Pacitto, Angela; Donini, Stefano; Ferraris, Davide M.; Boros, Sandor; Illyes, Eszter; Szokol, Balint; Rizzi, Menico; Blundell, Tom L.; Ascher, David B.; Pato, Janos; Mizrahi, Valerie; European Journal of Medicinal Chemistry; vol. 174; (2019); p. 309 – 329;,
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129799-08-2, 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

Benzyl carbonochloridate (6.43 mL, 45.03 mmol) was added to a solution of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (10 g, 40.94 mmol) and DIEA (14.30 mL, 81.87 mmol) in THF (100 mL) at 5C, and the mixture was stirred at room temperature for 14 hr. The reaction mixture was added to water and ethyl acetate. The organic layer was washed with aqueous ammonium chloride solution, dried over magnesium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (solvent gradient; 5?20% ethyl acetate/hexane) to give 1-benzyl 4-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (16.2 g, 42.8 mmol, 105%) as white crystals. 1H NMR (300 MHz, CDCl3):delta 1.44(9H,s), 2.63-3.48(3H,m), 3.74(3H,s), 4.11(2H,s), 4.44-4.86(2H,m), 5.08-5.26(2H,m), 7.22-7.42(5H,m).

129799-08-2, The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; YAMAMOTO, Satoshi; SHIRAI, Junya; ODA, Tsuneo; IMADA, Takashi; KONO, Mitsunori; SATO, Ayumu; TOMATA, Yoshihide; OCHIDA, Atsuko; ISHII, Naoki; SASAKI, Yusuke; FUKASE, Yoshiyuki; YUKAWA, Tomoya; FUKUMOTO, Shoji; (200 pag.)EP3192791; (2017); A1;,
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