Month: May 2021

76003-29-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

Step 1: tert-butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate To a solution of tert-butyl 3-oxopiperazine-1-carboxylate (prepared according to procedure reported in WO2005504737, 2.0 g, 9.99 mmol), 1-bromo-4-fluorobenzene (1.748 g, 9.99 mmol), N,N-dimethylethylenediamine (0.070 g, 0.799 mmol) and potassium hydrophosphate (KHPO4) (3.13 g, 17.98 mmol) in toluene (10 ml) was added copper (I)iodide (0.101 g, 0.529 mmol) at 25 C. The reaction mixture was heated to 80 C. for 16 h. Progress of the reaction was monitored by TLC. The reaction mixture was cooled to 25 C., diluted with ethyl acetate (25 ml) and filtered through a plug of celite and concentrated to give crude product. The crude product was purified over silica gel (100-200 mesh) by column chromatography using 30% ethyl acetate in hexane as eluent to obtain the title compound (0.8 g, 27.2%) 1H NMR (400 MHz, CDCl3) delta 7.28-7.24 (m, 2H), 7.14-7.08 (m, 2H), 4.26 (s, 2H), 3.88-3.71 (m, 4H), 1.51 (s, 9H). MS: m/z 295 (M+1).

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LUPIN LIMITED; Jana, Gourhari; Kurhade, Sanjay Pralhad; Jagdale, Arun Rangnath; Kukreja, Gagan; Sinha, Neelima; Palle, Venkata P.; Kamboj, Rajender Kumar; US2015/152118; (2015); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Diisopropylethylamine (44.0 mL, 252 mmol) was added to a stirred, room temperature mixture of 72 wt% 3-(2-Bromo-acetyl)-6-fluoro-2- methyl-benzonitrile (69 g, 194 mmol) and (5)-4-N-Boc-2-hydroxymethyl-piperazine (42.0 g, 194 mmol) in THF (1000 mL) and the mixture was stirred at room temperature for 18h. The reaction was diluted with 1 L EtOAc, washed 2x with 500 mL 10% w/w NaHCC”3 aqueous solution, dried over MgS04, filtered and concentrated. The residue was purified by column chromatography on silica gel (40-80%) EtOAc/Hexanes, linear gradient), to give the title compound., 314741-40-7

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); 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.5521-38-0,2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

601 2-(4-(4-nitrophenyl)piperazin-1-yl)ethan-1-ol (0.9 g, 3.58 mmol) was dissolved in 10 mL 6 EtOH, further 10 mL 7 water was added under stirring. 203 Iron powder (0.6 g, 10.75 mmol) and 67 NH4Cl (0.383 g, 7.16 mmol) were then added. The resulting mixture was heated at 90 C. for 1-2 h. The reaction was monitored by LCMS. After completion of reaction, mixture was filtered through celite bed, solvent form the filtrate was removed under reduced pressure. Water was added to the residue and extracted using 30 MeOH: 82 CH2Cl2 (10%), dried over Na2SO4. The solvent was removed under reduced pressure to afford 604 2-(4-(4-aminophenyl) piperazin-1-yl) ethan-1-ol (0.550 g, 70%) as a brown solid. (0626) LCMS: 221 [M+1]+

5521-38-0, 5521-38-0 2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol 2763936, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics