Month: August 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

[5681 ] 3-(2-bromoethyl)- l-(4-(5-(difluoromethyl)-1 ,4-oxadiazol-2-y )-2-fluorobenzyl)- l-p henylurea (0.050 g, 0.107 mmol) and cyclopropyl(piperazin- l-yl)methanone (0.018 g, 0.1 17 mmol) were mixed at the room temperature in acetonitrile ( 1 mL) and then stirred at 100 C for 18 hr and cooled down to the room temperature to terminate the reaction. Then, water was added to the reaction mixture, followed by extraction with dichloromethane. The bi-phasic mixture was passed through a plastic frit to remove the solid residues and aqueous layer, and the organic layer collected was concentrated in vacuo. The concentrate was purified and concentrated by column chromatography (Si02 plate, 20x20x 1 mm; methanol / dichloromethane = 10 %) to give 3-(2-(4-(cyclopropanecarbonyl)piperazin-l -yl)ethyl)-l-(4-(5-(difluoromethyl)- l ,3,4-ox adiazol-2-yl)-2-fluorobenzyl)- l -phenylurea as white foam (0.024 g, 41.5 %). [5682] NMR (700 MHz, CDC13) delta 7.89 (dd, 1 H, J = 8.0, 1.7 Hz), 7.75 – 7.68 (m, 2H), 7.43 – 7.38 (m, 2H), 7.37 – 7.31 (m, 1 H), 7.21 – 7.16 (m, 2H), 6.93 (t, 1 H, 7 = 51.7 Hz), 5.06 (s, 3H), 3.44 (d, 4H, J = 34.7 Hz), 3.34 (q, 2H, J = 5.7 Hz), 2.45 (t, 2H, J = 6.0 Hz), 2.39 (s, 2H), 2.32 (s, 2H), 1.03 – 0.94 (m, 2H), 0.80 – 0.72 (m, 2H); LRMS (ES) m/z 543.3 (M+ + 1 ).

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; KIM, Yuntae; LEE, Chang Sik; SONG, Hyeseung; GWAK, Dal-Yong; LEE, Jaeyoung; OH, Jung Taek; LEE, Chang Gon; KIM, II Hyang; (1041 pag.)WO2017/23133; (2017); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2 1-Benzyl-piperazin-2-one To a solution of 35 mL of TFA in dichloromethane was added 4-benzyl-3-oxo-piperazine-1-carboxylic acid tert-butyl ester (10.39 g, 35.8 mmol) in portions. After 18 hours the solution was concentrated via rotary evaporator and H20 was added. The pH was adjusted to 12 with 4M NaOH. The mixture was extracted with dichloromethane. The combined organic layers were dried over sodium sulfate, filtered and concentrated in vacuo to give 1-benzyl-piperazin-2-one (6.29 g, 92%) as an oil.

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Roche Palo Alto LLC; US2009/209553; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1214196-85-6, 1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a precooled (0 C) solution of 1-Boc-piperazine-2-carboxylic acid (500. mg, 2.17 mmol) in 1,4-dioxane (11 mL) under N2 atmosphere was added 1 M aq. NaOH until pH 11 achieved. To the resulting mixture was then added dropwise benzyl chloroformate (0.31 mL, 2.17 mmol) followed by additional 1 M aq. NaOH to maintain pH 11. The resulting mixture was allowed to warm to room temperature and stirred for 3 h, then cooled to 0 C before addition of benzyl chloroformate (0.31 mL, 2.17 mmol) and 1 M aq. NaOH to maintain pH 11. The resulting mixture was allowed to warm to room temperature and stirred for 28 h, then cooled to 0 C and acidified slowly with 1 M aq. HCl to pH 2. The aqueous layer was diluted with EtOAc and the layers were separated then the aqueous phase was extracted with EtOAc (3x). The combined organic layers were washed with brine, dried over Na2SO4, and concentrated in vacuo to afford the product, which was carried forward.

As the paragraph descriping shows that 1214196-85-6 is playing an increasingly important role.

Reference£º
Patent; THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA; VAL-CHUM, LIMITED PARTNERSHIP; GRENIER, Melissa Carey; SMITH, Amos B., III; FINZI, Andres; DING, Shilei; CHAPLEAU, Jean-Philippe; (240 pag.)WO2020/28482; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (S)-1-Boc-2-hydroxymethylpiperazine (1.0 g, 4.62 mmol) in DCE (92.47 ml, 4.624 mmol) was added formaldehyde (3.474 ml, 46.24 mmol) (37% in water) followed by sodium triacetoxyborohydride (4.9 g, 23.12 mmol). The mixture was stirred vigorously at room temperature for 2.5 hours. The mixture was treated with saturated sodium bicarbonate (30 mL), stirred for 10 min then extracted with DCM (3 10 mL). The combined organic phases were dried over sodium sulfate, filtered and concentrated. ES+APCI MS m/z 231.1 [M+H] +.

1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

17766-28-8, 1-Cyclohexylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 2Preparation of 4-((3-(4-cvclohexylpiperazin- 1 -yl)-6-oxo-6H-anthra[ I 9-cdIisoxazoI-5- yl)arnino)benzoic acid, About 70g of 4-((3-bromo-6-oxo-6H-anthra[1,9-cd]isoxazol-5- yl)amino)benzoic acid was dissolved in 95OmL of DMSO. About 5OmL of TEA and 50g of 1- cyciohexyl piperazine were added to the reaction. Temperature was raised to 60-70C. After 2-3hours, slowly added 500mL of MTBE and MeOH (10:1) solution and adjusted the temperature to40-50C. The solid was centrifuged and washed by IOOrnL of MTBE and MeOH solution and followed by iOOrnL of MeOH. Solid was dried under reduced pressure at 25-30C for 12-24 hours to obtain the 4-ft3-(4-cyclohexyipiperazin-i-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5- yl)amino)henzoic acid at about 98% purity and about 91% yield.

17766-28-8 1-Cyclohexylpiperazine 87298, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; VM PHARMA LLC; WU, Jay Jie-Qiang; WANG, Ling; (83 pag.)WO2016/43975; (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.

To a stirred solution of tert-butyl 2-methylsulfanyl-4-(trifluoromethylsulfonyloxy)-6,8-dihydro-5H-pyrido[3,4- -d]pyrimidine-7-carboxylate (46.0 g, 107 mmol, 1.00 eq) in DMF (500 mL) was added DIEA (27.7 g, 214 mmol, 37.4 mL, 2.00 eq) followed by benzyl piperazine-1-carboxylate (25.9 g, 117 mmol, 22.7 mL, 1.10 eq). The reaction was heated to 100¡ã C. for 1 hour under a nitrogen atmosphere. The reaction mixture was poured into ethyl acetate (300 mL), washed with H 2O (300 mL 3) and brine (200 mL), dried over anhydrous Na 2SO 4, filtered and concentrated under vacuum. The residue was purified by column chromatography (SiO 2, Petroleum ether/Ethyl acetate=1:0 to 5:1) to give tert-butyl 4-(4-benzyloxycarbonylpiperazin-1-yl)-2-methylsulfanyl-6,8-dihydro-5H-pyr- ido[3,4-d]pyrimidine-7-carboxylate (51.0 g, 96.9 mmol, 90.5% yield, 92.0% purity) as a white solid ESI MS m/z 500.3 [M+H] +.

The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (2019); 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.

Intermediate 6: 4-{[(3S)-3-Meth l-1 -piperazinyl]sulfonyl}benzonitrileTo a solution of 1 ,1 -dimethylethyl (2S)-2-methyl-1 -piperazinecarboxylate (2.5g, supplier Atlantic Scitech) and DIPEA (5.45 ml, 31 .2 mmol) in dry dichloromethane (DCM) (60 ml) at 0C under argon was added 4-cyanobenzenesulfonyl chloride (2.64 g, 13.1 1 mmol) and the resulting clear solution stirred at 0C for 2h. Saturated aqueous NaHC03 (100 mL) was added, the layers separated, then the organic layers washed with 2M aqueous HCI (100 mL) and passed through a hydrophobic frit. The solution in DCM was cooled to 0C, then TFA (8.87 ml, 1 15 mmol) was added. The resulting very pale yellow solution was allowed to warm to room temperature over 1 h, then stirred for 18h. Aqueous 2M NaOH (100 mL) was added cautiously with cooling (0C) and layers were separated. The organic layer was extracted with 1 M aqueous HCI (3X30 mL). With cooling (0C), the combined acidic aqueous layers were adjusted to pH 7 by addition of solid NaOH, and then extracted with EtOAc (2X50 mL). The combined organic layers were washed with brine (30mL), dried (MgS04), filtered and concentrated in vacuo to give the title compound as a white solid (2.35 g)-LCMS (low pH) RT 0.51 min, m/z (ES) 266 [M+H]+

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; HEER, Jag Paul; CRIDLAND, Andrew Peter; NORTON, David; WO2011/86377; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 11 An experiment was carried out as described for Example 9, except that 45.55 g of 1-butanol and 4.61 g of water (water content 9.2 wt%) were used instead of 50.00 g of 1-butanol. As a result, the conversion of 2-methylpiperazine was 94.3%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 85.8% (reaction yield 80.9%).Comparative Example 8 An experiment was carried out as described for Example 9, except that 37.56 g of 1-butanol and 12.67 g of water (water content 25.2 wt%) were used instead of 50.00 g of 1-butanol. As a result, the conversion of 2-methylpiperazine was 81.6%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 70.9% (reaction yield 57.9%).Comparative Example 9 An experiment was carried out as described for Example 9, except that 25.00 g of 1-butanol and 25.00 g of water (water content 50.0 wt%) were used instead of 50.00 g of 1-butanol. As a result, the conversion of 2-methylpiperazine was 81.2%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 41.8% (reaction yield 33.9%).

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

A mixture of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.04 mmol) and an ammonia methanol solution (7 M, 10mL) in a 100 mL of sealing tube was stirred at 60 for 12 h and concentratedto give the title compound as a white solid (450 mg, 95) . 1H NMR (400 MHz, CD3OD): delta ppm 4.01-4.08 (m, 1H) , 3.65-3.88 (m, 1H) , 3.31-3.38 (m, 1H) , 2.90-3.12(m, 3H) , 2.73-2.82 (m, 1H) , 1.47 (s, 9H) and MS-ESI: m/z 130.20 [M+H-100] +.

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-(2-fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (29.1 g, 89.4 mmol) in MeOH (150 mL) and DCM (10 mL) mixture was added Raney Ni (5.5 g) and the Parr shaker was charged with hydrogen to 50 psi for 1 h. The initial yellow solution became clear and the content was filtered, washed with MeOH and the combined filtrate evaporated to dryness. The residue was dissolved in dry dioxane (20 mL) and a 4M HC1 solution in dioxane (30 mL) was added. The solution was warmed to 45 C in a water bath and stirred vigorously overnight producing a white precipitate. After filtering and washing with cold dioxane and diethyl ether and drying in vacuo, 23.1 g (96%) of the title compound was isolated as a white solid. N1HMR (400 MHz, DMSO-4 delta (ppm): 10.5 (br. s., 1 H), 9.63 (br. s., 2H), 8.0 (br. s., 2H), 7.29 (d, J = 12.6 Hz, 1 H), 7.20 – 7.19 (m, 2H), 3.24 (d, J = 4.8 Hz, 4H), 3.19 (br. s., 4H). 19F NMR (376 MHz, DMSO-d6) delta (ppm): – 120.36 (dd, J = 13.6, 7.2 Hz, IF).

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference£º
Patent; ANACOR PHARMACEUTICALS, INC.; HERNANDEZ, Vincent, S.; DING, Charles; PLATTNER, Jacob; ALLEY, Michael, Richard Kevin; ZHANG, Yong-Kang; ZHANG, Yanchen; WO2011/37731; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics