Category: 59878-57-8

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.,59878-57-8

INTERMEDIATE 46(S)-N-(I – (2- r4-(Cyclopropanecarbony?piperazin- 1 -yl] -8-methylquinolin-3 -yl) ethvD- 2,2,2-trifluoroacetamideIntermediate 45 (100 mg, 0.32 mmol), cyclopropyl(piperazin-l-yl)methanone (0.09 mL, 0.63 mmol), NMP (2 mL) and DIPEA (0.10 mL, 0.80 mmol) were combined in a sealed tube and heated to 1400C for 4 days. After cooling, Et2O (50 mL) was added to the reaction mixture. The organic layer was washed with water (5 x 50 mL) and brine. The organic layer was dried (MgSO4), filtered and the solvent was removed in vacuo. Purification by column chromatography on silica, eluting with 0-30% EtOAc in isohexane, gave the title compound (82 mg, 60%) as a pale yellow gum. delta? (CDCl3) 8.01 (IH, s), 7.75-7.65 (IH, m), 7.59 (IH, d, J 8.1 Hz), 7.55-7.48 (IH, m), 7.40-7.31 (IH, m), 5.58-5.47 (IH, m), 4.00-3.86 (3H, s), 3.85-3.72 (IH, s), 3.54-3.30 (2H, m), 3.18 (2H, m), 2.71 (3H, s), 1.84-1.76 (IH, m), 1.64 (3H, d, J6.8 Hz), 1.09-0.97 (2H, m), 0.84-0.75 (2H, m).

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MACDONALD, Jonathan, David; MATTEUCCI, Mizio; NASH, David, John; OWENS, Andrew, Pate; RAPHY, Gilles; SAVILLE-STONES, Elizabeth, Anne; SHARPE, Andrew; WO2010/100405; (2010); 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

59878-57-8, (4) The product of the previous step (0.3 g, 1 mmol) was weighed, dissolved in 5 mL of dichloromethane, and trimethylacetyl chloride (121 yL, 1 mmol) and triethylamine (208 mL, 1.5 mmol) were stirred at room temperature. The reaction was clarified until the solution was clarified. 1 – (cyclopropylcarbonyl)-pyridazine (0.3 g, 2 mmol) was dissolved in 5 mL of ethanol, added dropwise to the above clear solution, reacted at room temperature for 4 h, and extracted with dichloromethane (15 mL). The organic phase was washed with water, and the organic layer was dried over anhydrous sodium sulfate, and then evaporated to dryness to afford ololani (0.4 g, 0.9 mmol), yield 91.5%, purity 99.8%.

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Patent; Beijing Yaocheng Huiren Technology Co., Ltd.; Qiao Hongwei; Bian Weiguang; Li Qiaoying; (9 pag.)CN108129397; (2018); A;,
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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, To a stirred suspension of 4-(bromomethyl)-6-(trifluoromethyl)pyridin-2-amine hydrobromide (2.10 g, 6.25 mmol) in acetonitrile (13 mL) was added potassium carbonate and cyclopropyl(piperazin-1-yl)methanone (1.06 g, 6.88 mmol). The mixture was stirred atr.t. for 14 h. Water was added and the mixture was extracted with ethyl acetate. The organic phase waswashed with half-saturated sodium chloride solution, dried (sodium sulfate) and the solvent was removed in vacuum. Ssilicage chromatography gave 2.00 g (98 % yield) of the title compound.LC-MS (Method 2): R = 0.94 mm; MS (ESipos): m/z = 329 [M+H]

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

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; SCHULZE, Volker; HEINRICH, Tobias; PRINZ, Florian; LEFRANC, Julien; SCHROeDER, Jens; MENGEL, Anne; BONE, Wilhelm; BALINT, Joszef; WENGNER, Antje; EIS, Knut; IRLBACHER, Horst; KOPPITZ, Marcus; BOeMER, Ulf; BADER, Benjamin; BRIEM, Hans; LIENAU, Philip; CHRIST, Clara; STOeCKIGT, Detlef; HILLIG, Roman; (1256 pag.)WO2017/102091; (2017); 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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.,59878-57-8

To a solution of 4 (0.5g, 2.5mmol) in THF was added Et3N (0.52mL, 3.76mmol) and N-(2-aminoethyl)acetamide (0.25g, 2.5mmol). The mixture was stirred at 30C for 1h, cooled to room temperature and concentrated in vacuo. The residue was suspended in water and extracted with EtOAc. The organic phase was dried over MgSO4 and concentrated by evaporation in vacuo. Solid was recrystallized from toluene to afford 12. Recrystallized from acetonitrile as a white solid (55% yield).

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Article; Bolteau, Raphael; Caignard, Daniel H.; Delagrange, Philippe; Descamps, Florian; Ettaoussi, Mohamed; Melnyk, Patricia; Yous, Said; European Journal of Medicinal Chemistry; vol. 189; (2020);,
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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.,59878-57-8

3-((4-oxo-3,4-dihydro-phthalazin-1-yl-oxyl) benzoic acid (54 mg, 0.3 mmol) was dissolved in N, N-dimethylformamide, and then 1-(3-dimethylaminopropyl) -3-ethylcarbodiimide hydrochloride (EDCI) (220 mg, 1.2 mmol), triethylamine(150 muL, 1.2 mmol) and 1-hydroxy-7-azabenzotriazole (HOAt)(165 mg, 1.2 mmol) were added successively. The mixture was stirred at room temperature for half an hour, and then N-(cyclopropanecarbonyl) piperazine was added and reacted at room temperature overnight, and then the reaction was quenched with water, extracted with ethyl acetate, and washed with water for three times. The organic phases were combined and washed with saturated saline, dried with anhydrous sodium sulfate, and concentrated for column chromatography isolation (dichloromethane:methanol=20:1) to give Compound 7. A white solid was obtained. 1H NMR (600 MHz, DMSO-d6): delta 11.98 (s, 1H), 8.27 (d, 1H, J = 7.38 Hz), 8.10 (d, 1H, J = 7.74 Hz), 7.99-8.01 (m, 1H), 7.94-7.96 (m, 1H), 7.52 (t, 1H, J= 7.86 Hz), 7.39-7.38 (m, 2H), 7.28 (d, 1H, J = 7.62 Hz), 3.33-3.81 (m, 8H), 1.96 (brs, 1H), 0.69-0.74 (m, 4H); ESI-MSm/z: calculated for 418.16, found 417.89 [M-H]+.

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

Reference£º
Patent; Chengdu Di’ao Pharmaceutical Group Co. Ltd.; JI, Jianxin; GUO, Na; XUE, Ting; KANG, Bingqiang; YE, Xinfa; CHEN, Xin; ZHANG, Tao; EP2799435; (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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, 0.62g to 1.0g of Intermediate VI and cyclopropylmethyl – piperazin-1-yl – methyl ketone was added to a 100mL one-neck flask was added10mLDMF clear solution was stirred, then add 2.05gHBTU, 0.82g triethylamine, room temperature for 5h. After completion of the reaction the reactionIt was poured into water, extracted with ethyl acetate, dried over anhydrous sodium sulfate spin column chromatography to give 1.1g solid.

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

Reference£º
Patent; Warwick Nanjing Pharmaceutical Technology Co., Ltd.; Zhang, Xiaoqing; Song, Zhinchun; Bao, Jinyuan; Jiang, Yuwei; (25 pag.)CN105254628; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8,59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add Compound III 25.82 g to the reaction flask.Purified water 100ml,Stir at room temperature,Then add 22.4M sodium hydroxide 92.4ml,The mixture temperature was heated to 100 C,Stir 12h, cool to room temperature, filter, wash,The combined filtrate was acidified with 46.2 ml of 2M diluted hydrochloric acid for 30 min,Then, 500 ml of methanol, 18.70 g of triethylamine, and 14.25 g of 1-cyclopropanecarbonylpiperazine are added successively.At a reaction temperature of 20-25C, the reaction is stirred for 10 hours. After the reaction is completed, it is cooled to 0C and filtered.38.66 g of solids were obtained with a yield of 96.2% and a purity of 99.89%. The refining of olaparib (I)30g of crude oleapani was placed in a dissolving tank81.82 ml of isopropanol and 818.2 ml of acetone were added and the temperature was controlled at 45-50C.Stir and dissolve. After the crude product is completely dissolved, add charcoal to decolorize it for 30 minutes.The decolorization reaction was followed by hot filtration and the filtrate was stirred at room temperature for crystallization.Then cool down to 0 ~ 10 C for 4 hours, filter, and wash with acetone,Filtration, drying, that is, olaparib 28.35g,The yield was 94.5%, the purity was 99.99%, the mononuclear 0.05%, and the total heterologous 0.11%.

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

Reference£º
Patent; Shandong Yuxin Pharmaceutical Co., Ltd.; Liu Zhenteng; Chen Yu; Sun Heng; Wang Chunyan; (6 pag.)CN108101852; (2018); A;,
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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, To a round bottom flask containing Methyl-5-((4-oxo-3-((2-(trimethylsilyl)ethoxy) methyl)- 3,4-dihydrophthalazin-l-yl) methyl)-2-(4,4,5,5-tetramethyl-l,3,2-dioxa borolan-2- yl)benzoate and bis(pinacolato) diboron (2.00 g) was added THF (100 mL) before cooling to 0C. Upon cooling, 2M lithium hydroxide (7 mL, 14 mmol) was added dropwise before allowing to reaction to stir for 30 minutes at 0C. 1M HC1 was then added dropwise to the reaction mixture at 0C until reaching pH 4. The mixture was then extracted with EtOAc (3 x 80 mL) and washed with Brine (3 x 50 mL). The organic phases were combined and the excess solvent removed in vacuo. The crude material (1.4 g) was transferred to a round bottom flask upon which DCM (100 mL), HBTU (2.97 g, 7.84 mmol) and DIPEA (1.36 mL, 7.84 mmol) was added. After stirring at room temperature for 30 minutes, N- cyclopropylcarbonylpiperazine (1.11 mL, 7.85 mmol) was added and the reaction stirred overnight. After stirring for 16 hours, the excess solvent was removed in vacuo and the crude material isolated by flash column chromatography (Pure EtOAc) before purification by reverse phase HPLC was carried out to afford 4-(3-(4-(cyclopropanecarbonyl) piperazine- 1- carbonyl)-4-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2-yl)benzyl)-2-((2-trimethlsilyl) ethoxy)methyl)phthalazin-l(2/7)-one (419 mg, 0.62 mmol, 22% – three steps) as a white solid in a mixture of rotamers. In each case the shift relating to the minor rotamer has been donated with an asterisk.* *H NMR (400 MHz, CDCb) d = 8.46 (dd, J = 7.8, 1.6 Hz, 1H + 1H*), 7.79 – 7.55 (m, 4H + 4H*), 7.32 – 7.28 (m, 1H + 1H*), 7.14 (bs, 1H + 1H*), 5.59 (s, 2H + 2H*), 4.33 (s, 2H + 2H*), 3.87 – 3.04 (m, 10H + 10H*), 1.28 (s, 12H + 12H*), 1.04 – 0.97 (m, 4H + 4H*), 0.90 – 0.85 (m, 1H + 1H*), 0.83 – 0.71 (m, 2H + 2H*), 0.00 (s, 9H + 9H*); 13C NMR (100 MHz, CDCb) d = 172.3 (1C + 1C*), 171.0 (1C + 1C*), 160.0 (1C + 1C*), 144.7 (1C + 1C*), 142.9 (1C + 1C*), 141.3 (1C + 1C*), 136.3 (1C + 1C*), 133.3 (1C + 1C*), 131.5 (1C + 1C*), 129.2 (1C + 1C*), 128.4 (1C + 1C*), 128.2 (1C + 1C*), 127.7 (1C + 1C*), 125.4 (1C + 1C*), 125.2 (1C + 1C*), 84.1 (2C + 2C*), 79.0 (1C + 1C*), 67.3 (1C + 1C*), 47.3 (1C*), 46.9 (1C), 45.2 (1C*), 44.8 (1C), 41.9 (1C*), 41.7 (2C), 41.4 (1C*), 39.1 (1C + 1C*), 24.9 (4C + 4C*), 18.1 (1C + 1C*), 11.1 (1C + 1C*), 7.66 (2C + 2C*), -1.36 (3C + 3C*) (the carbon bearing the boron substituent is not observed); IR (v, cm 1): 2981, 2889, 2360, 2341, 1641, 1382, 1354, 1146, 1087, 956; HRMS (ESI) for C36H49N4O610B23Na28Si [M+Na]+ requires 694.34429 found 694.34418; Mp: 78 – 80C.

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

Reference£º
Patent; OXFORD UNIVERSITY INNOVATION LIMITED; GOUVERNEUR, Veronique; CORNELISSEN, Bart; WILSON, Thomas Charles; (152 pag.)WO2019/186135; (2019); 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

General procedure: To a solution of compound 19 (100 mg, 0.33 mmol) in anhydrous DMF (3 mL) was added appropriate amine (0.43 mmol), EDC (82 mg, 0.43 mmol), 1-hydroxybenzotriazole monohydrate (66 mg, 0.43 mmol), and triethylamine (43 mg, 0.43 mmol). The reaction mixture was stirred at rt overnight, and partitioned between methylene chloride and brine. The organic phase was washed with brine, water, and concentrated. The residue was separated by HPLC to provide compounds 20. For compounds 20f, 20g, and 20h whose syntheses involved the use of BOC-protected amine, the coupling product was then treated with TFA (0.5 ml) in CH2Cl2 (2 mL) at rt for 1 h. Removal of the volatiles provided the crude 20 that can be further purified by HPLC to give the title products., 59878-57-8

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Article; Zhu, Gui-Dong; Gong, Jianchun; Gandhi, Viraj B.; Liu, Xuesong; Shi, Yan; Johnson, Eric F.; Donawho, Cherrie K.; Ellis, Paul A; Bouska, Jennifer J.; Osterling, Donald J.; Olson, Amanda M.; Park, Chang; Luo, Yan; Shoemaker, Alexander; Giranda, Vincent L.; Penning, Thomas D.; Bioorganic and Medicinal Chemistry; vol. 20; 15; (2012); p. 4635 – 4645;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8,59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The synthetic route is: Piperazine cyclopropyl ketone (1.1g, 0.0071mol)Soluble in 25ml anhydrous acetonitrile,Add potassium carbonate (4.0g, 0.029mol), cool to 0 , nitrogen protection,Stir vigorously. Compound 5 (2.1g, 0.0066mol),Dissolve with 20ml of anhydrous acetonitrile and slowly add dropwiseAfter the addition, the temperature was raised to room temperature, a small amount of DMAP (0.5g, 0.0041mol) was added, and the reaction was carried out for 6h.Concentrate under reduced pressure, add 40ml of water, adjust the pH to 8 with sodium bicarbonate, extract with ethyl acetate, concentrate under reduced pressure to remove the solvent, recrystallize with ethyl acetate, filter to obtain light red solid, decolorize with a small amount of activated carbon, filter and concentrate It was dried to obtain a white solid (2.8g, yield 93%).

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

Reference£º
Patent; Southeast University; Cai Jin; Ren Jinghui; Hu Xinyi; Wei Lili; Yu Ping; Huang Mingqi; (8 pag.)CN110790710; (2020); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics