Month: September 2020

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound of formula 38 (10.0 g, 49.2 mmol) was added to the reaction flask at room temperature,100 mL of N, N-dimethylacetamide,1-acetylpiperazine 16 (8.2 g, 64.0 mmol)N, N-diisopropylethylamine (19.1 g, 147.8 mmol)90 reaction 7 ~ 8h,TLC monitoring reaction is complete,Down to room temperature,The reaction solution was poured into 300 mL of water,Extracted with ethyl acetate (80 mL x 3)Combined organic layer,Washed with saturated brine,Dried over anhydrous sodium sulfate,The compound of formula 41 (9.9 g) was obtained by steaming,As a beige solid (yield 80.6%).

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhengda Tianqing Pharmaceutical Group Co., Ltd.; Zhang Yinsheng; Gao Yong; Ren Jing; Wang Qinglin; Wang Zhao; (67 pag.)CN106905245; (2017); A;,
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20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 168 N-[2-(4-Cyclopropylpiperazin-1-yl)ethyl]-8-[(2,6-difluorobenzyl)oxy]-2-methylimidazo[1,2-a]-pyridine-3-carboxamide 118 mg of 8-[(2,6-difluorobenzyl)oxy]-2-methyl-N-(2-oxoethyl)imidazo[1,2-a]pyridine-3-carboxamide (Example 194A, 0.16 mmol, 1 equivalent) were suspended in 0.8 ml of dry dichloroethane, 23 mg 1-cyclopropylpiperazine (0.18 mmol, 1.1 equivalents) were added and the mixture was stirred at RT for 3 h. 52 mg of sodium triacetoxyborohydride (0.25 mmol, 1.5 equivalents) were then added, and the mixture was stirred at RT overnight. 1 N aqueous sodium hydroxide solution was then added, and the mixture was extracted three times with dichloromethane. The combined organic phases were washed with water and saturated aqueous sodium chloride solution, dried over sodium sulphate, filtered and concentrated. The residue was dissolved in methanol and purified by preparative HPLC (method: RP18 column, mobile phase: acetonitrile/water gradient with addition of 0.1% TFA). The product fraction was taken up in ethyl acetate and washed twice with saturated aqueous sodium bicarbonate solution. The combined organic phases were dried over sodium sulphate, filtered and concentrated. This gave 33.5 mg (43% of theory) of the title compound. LC-MS (Method 7): Rt=0.60 min MS (ESpos): m/z=470.2 (M+H)+ 1H NMR (400 MHz, DMSO-d6): delta=0.22-0.30 (m, 2H), 0.34-0.43 (m, 2H), 1.53-1.62 (m, 1H), 2.30-2.44 (m, 3H), 3.37-3.46 (m, 2H), 5.30 (s, 2H), 6.93 (t, 1H), 7.01 (d, 1H), 7.23 (t, 2H), 7.55-7.64 (m, 1H), 7.70 (t, 1H), 8.67 (d, 1H), [further signals hidden under solvent peaks].

20327-23-5, The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; VAKALOPOULOS, Alexandros; FOLLMANN, Markus; HARTUNG, Ingo; BUCHGRABER, Philipp; JAUTELAT, Rolf; HAssFELD, Jorma; LINDNER, Niels; WUNDER, Frank; STASCH, Johannes-Peter; REDLICH, Gorden; LI, Volkhart Min-Jian; BECKER, Eva-Maria; KNORR, Andreas; US2014/128372; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

A solution of the product of EXAMPLE SE (300 mg, 1.4 mmol), 2-methoxy-4-(4-methylpiperazin- 1 -yl) aniline (338 mg, 1.53 mmol) andtriethylamine (421 mg, 4.17 mmol) in 1,4-dioxane (30 mL) was stirred at 105 C. under nitrogen for 12 hours. The solvent was removed under vacuum and the residue was washed with sodium bicarbonate solution and ethanol. The crude product was recrystallized from 1 ,4-dioxane to give the title compound.10318] ?H NMR (DMSO-d5) oe ppm 12.66 (s, 1H), 11.35 (s, 1H), 8.31 (d, J=9.0 Hz, 1H), 8.25 (s, 1H), 6.68 (d, J=1.2 Hz, 1H), 6.54 (dd, J=1.2, 9.0 Hz, 1H), 3.89 (s, 3H), 3.21-3.10 (m, 4H), 2.50-2.44 (m, 4H), 2.25 (s, 3H)., 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBVIE INC.; Vasudevan, Anil; Penning, Thomas Dale; Chen, Huanming; Liang, Bo; Wang, Shaohui; Zhao, Zhongqiang; Chai, Dikun; Yang, Leifu; Gao, Yingxiang; Pliushchev, Marina; US2014/171429; (2014); 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.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

Example 58(4-cyclopentylpiperazin-1-yl)(7-(methylsulfonyl)-7-azaspiro[3.5]nonan-2-yl)methanone Oxalyl chloride (85 mul, 0.97 mmol) was slowly added to a solution of Intermediate 26 in DCM (12 mL) at 0 C. One drop of DMF was added and the reaction mixture was stirred for 4 h. The solvent was concentrated. The residue was quickly recovered in DCM (5 mL) and added to a solution of 1-cyclopentylpiperazine (54.9 mg, 0.36 mmol) and Et3N (0.135 mL, 0.97 mmol) in DCM (12 mL) at 0 C. The reaction mixture was allowed to warm to ambiant temperature and stirred for 1 h. The solvent was concentrated and the product was purified on silica gel (24 g) by MPLC using MeOH 5%, acetone 10% in DCM as eluent to provide title compound (106 mg, 85%) as a solid. 1H NMR (400 MHz, CHLOROFORM-d) delta ppm 1.32-1.47 (m, 2H) 1.49-1.62 (m, 2H) 1.64-1.73 (m, 4H) 1.73-1.80 (m, 2H) 1.80-1.92 (m, 2H) 1.97-2.07 (m, 2H) 2.10-2.20 (m, 2H) 2.40-2.55 (m, 5H) 2.76 (s, 3H) 3.07-3.14 (m, 2H) 3.15-3.26 (m, 3H) 3.32-3.39 (m, 2H) 3.59-3.67 (m, 2H); HRMS m/z calcd for C19H34N3O3S 384.2315 [M+H]+, found 384.2305., 21043-40-3

21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; US2010/130477; (2010); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-Butyl (25)-2-methylpiperazine-1-carboxylate ( 43.1 g, 215 mmol) was added to asolution of aldehyde from Preparation 3 (39.0 g, 195 mmol) in dichloromethane (780mL). The reaction mixture was stirred at room temperature for 10 min then sodiumtriacetoxyborohydride (83.1 g, 391 mmol) was added portion-wise. On complete30 addition the reaction mixture was stirred at room temperature for 4 h. The reaction mixture was carefully quenched with water (200 mL) and extracted withdichloromethane (200 mL). The organic layer was dried over sodium sulphate andconcentrated under reduced pressure. Trituration of the crude product with n-pentane afforded the title compound as an off-white solid. (43.0 g, 57.3%)5 1H NMR (300MHz, DM50-d6) o =7.92 (d, 1=2.2 Hz, lH), 7.68 (d, 1=2.2 Hz, lH), 4.09(m, lH), 3.67 (br d, J= 13.1 Hz, lH), 3.52 (s, 2H), 2.88-3.02 (m, lH), 2.69 (br d,J=ll.l Hz, lH), 2.57 (br d, 1=11.3 Hz, lH), 2.35 (s, 3H), 2.15 (dd, 1=11.3, 3.6 Hz, lH),1.98 (td, 1=11.7, 3.4 Hz, lH), 1.39 (s, 9H), 1.13 (d, J=6.7 Hz, 3H). LCM5 Method 1:10m/z 384.66 [M+H+]; RT = 3.47 min

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; LEO PHARMA A/S; JESSIMAN, Alan Stuart; JOHNSON, Patrick Stephen; MAANSSON, Kristoffer; S?RENSEN, Morten Dahl; (156 pag.)WO2018/11201; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

414910-15-9, tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1 -Tertbutoxycarbonyl-4-(cyclopropanecarbonyl)piperazine (190 mg, 0.75 mmol) was dissolved in dichloromethane, and then trifluoroacetic acid (1 mE) was added. The reaction mixture was stirred at room temperature until complete reaction, and then washed with saturated sodium bicarbonate solution for three times. The organic phases were concentrated to give 112mg (yield 97%) pale yellow solid of N-(cyclopropanecarbonyl) piperazine for use.

414910-15-9, As the paragraph descriping shows that 414910-15-9 is playing an increasingly important role.

Reference£º
Patent; CHENGDU DI’AO PHARMACEUTICAL GROUP CO., LTD.; Ji, Jianxin; Guo, Na; Xue, Ting; Kang, Bingqiang; Ye, Xinfa; Chen, Xin; Zhang, Tao; US2015/51211; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of Intermediate 4 (0.38 g, 2.06 mmol) in DMF (20 mL) were added tert-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1 g, 4.12 mmol) and DIPEA (0.4 g, 3.0 mmol). The reaction mixture was heated at 100C for 5 h, allowed to cool, then stirred at room temperature for 2 days. The reaction mixture was concentrated in vacuo, then partitioned between water and DCM. The organic phase was separated and concentrated in vacuo. The resulting crude material was purified by column chromatography (silica gel: 100-200 mesh, MeOH:DCM gradient 0% to 20%) to give a pale yellow foam. The foam was dissolved in DCM (1 mL) and TFA (2 mL) and stirred for 1 h. The reaction mixture was concentrated in vacuo, then triturated with diethyl ether, to give the title compound (0.6 g) as a sticky yellow solid., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference£º
Patent; UCB PHARMA S.A.; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D; BROOKINGS, Daniel Christopher; FORD, Daniel James; FRANKLIN, Richard Jeremy; GHAWALKAR, Anant Ramrao; KULISA, Claire Louise; NEUSS, Judi Charlotte; REUBERSON, James Thomas; WO2013/68458; (2013); A1;,
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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.

5-(bromoacetyl)-2-fluorobenzonitrile (590 mg, 2.44 mmol) and (S)-4-N-BOC-2-hydroxymethyl-piperazine (527 mg,2.44 mmol) were dissolved in THF (40 mL) at 0C then TEA (247 mg, 2.44 mmol) was added. The reaction mixturewas stirred at RT for 16 h, then poured into water and extracted with ethyl acetate. The organic layer was dried overNa2SO4, filtered, and evaporated to dryness. The crude product was purified by MPLC through an 80g Redi-sepcolumn using 0-100% EtOAc/hexane to yield 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.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 2: To a suspension of 26 (2.00 g, 7.3 mmol) in toluene (28 ml) were added N-Boc cis-2,6-dimethylpiperazine (3.13 g, 14.6 mmol), Pd2(dba)3 (254 mg, 0.28 mmol), tri-tert-butylphosphonium tetrafluoroborate (212 mg, 0.73 mmol) and NaO-tert-Bu (1.05 g, 10.9 mmol). The mixture was refluxed under N2 overnight. After cooling to room temperature, the mixture was partitioned between EtOAc (150 mL) and water (100 mL). The insoluble was removed through filtration and washed with EtOAc. The EtOAc layer was separated and washed with brine, dried over anhydrous Na2SO4. After the removal of organic solvent in vacuo, the residue was purified through Biotage chromatography (EtOAc/hexane= 25/100 to 75/100 gradient) to give the desired product 27 (476 mg, 16%) as a faint yellow solid.

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Jiang, Jian-kang; Huang, Xiuli; Shamim, Khalida; Patel, Paresma R.; Lee, Arthur; Wang, Amy Q.; Nguyen, Kimloan; Tawa, Gregory; Cuny, Gregory D.; Yu, Paul B.; Zheng, Wei; Xu, Xin; Sanderson, Philip; Huang, Wenwei; Bioorganic and Medicinal Chemistry Letters; vol. 28; 20; (2018); p. 3356 – 3362;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reaction between N-BOC-piperazine and methane sulfonyl chloride in dichloromethane and triethylamine yielded 4-methanesulfonyl-piperazine-1-carboxylic acid tert-butyl ester. Cleavage of the BOC protecting group using HCl (2M) in dichloromethane yielded 1-methanesulfonyl-piperazine HCl salt. (0366) A mixture of 2-chloro-4-morpholin-4-yl-thieno[3,2-d]pyrimidine-6-carbaldehyde 10 (1.00 g), 1-methanesulfonyl-piperazine (750 mg) and trimethylorthoformate (3.80 mL) was stirred in 1,2-dichloroethane (30 mL) for 6 hrs at room temperature. To this was added sodium triacetoxyborohydride (900 mg) and the reaction mixture was stirred for 24 hours at room temperature. The mixture was then quenched with brine, extracted with dichloromethane, dried (MgSO4) and the solvent removed in vacuo. The residue was triturated with hot ethyl acetate to yield 4-(2-chloro-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine 31 as a white solid (1.01 g)., 57260-71-6

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Genentech, Inc.; Ebens, Jr., Allen J.; Friedman, Lori; (64 pag.)US9335320; (2016); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics