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, To a solution of the above compound (68mg, 0.27mmol) in anhydrous DMF (2mL) under N2 at 0C were added WSC (61mg, 0.32mmol) and HOBt (43mg, 0.32mmol). The resulting mixture was stirred for 30min, then it was added with DIPEA (141mul, 0.81mmol) and 1-(cyclopropylcarbonyl)piperazine (115mul, 0.81mmol). Stirring was continued at room temperature for 20h. The residue was partitioned between water and ethyl acetate and the phases were separated. The organic layer was washed with brine, dried, filtered and evaporated. Purification by flash chromatography (CH2Cl2:MeOH 95:5) afforded 85mg (80%) of the title compound. 1H NMR (CDCl3) delta 10.88 (1H, br s); 8.18-7.95 (3H, m); 7.47 (1H, d, J=8.4Hz); 7.34-7.18 (2H, m); 6.50 (1H, m); 3.97-3.73 (4H, m); 3.88-3.72 (2H, m); 3.54-3.34 (2H, m); 1.75 (1H, m); 1.09-0.94 (2H, m); 0.90-0.64 (2H, m). Anal. Calcd for C22H21FN4O2: C, 67.33; H, 5.39; N, 14.28. Found: C, 69.86; H, 5.34; N, 13.88.

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

Reference：
Article; Cincinelli, Raffaella; Musso, Loana; Merlini, Lucio; Giannini, Giuseppe; Vesci, Loredana; Milazzo, Ferdinando M.; Carenini, Nives; Perego, Paola; Penco, Sergio; Artali, Roberto; Zunino, Franco; Pisano, Claudio; Dallavalle, Sabrina; Bioorganic and Medicinal Chemistry; vol. 22; 3; (2014); p. 1089 – 1103;,
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, 3-((4-oxo-3,4-dihydrophthalazin-1-yl-oxyl)methyl)benzoic acid (148 mg, 0.5 mmol) was dissolved in N,Ndimethylformamide, and then 1 -(3-dimethylaminopropyl)-3- ethylcarbodiimide hydrochloride (EDCI) (115 mg, 0.63 mmol), triethylamine (83.6 pL, 0.63 mmol) and 1-hydroxy- 7-azabenzotriazole (HOAt) (81.6 mg, 0.63 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 over-night, and then the reaction was quenched with water. The mixture was extracted with ethyl acetate, and washed with water for two times. The organic phases were combined and washed with saturated saline, dried with anhydrous sodium sulfate, concentrated and then purified by column chromatography (dichloromethane:methanol=20: 1) to give a white solid 173mg (yield 8 8%). ?H NMR (600 MHz, DMSO-d5): oe 11.94 (s, 1H), 8.21 (d, 1H, J=7.68 Hz), 7.99 (d, 1H, J=7.86 Hz), 7.94-7.92 (m, 1H), 7.90-7.88 (m, 1H), 7.61 (d, 1H, J=7.62 Hz), 7.55 (s, 1H), 7.49 (t, 1H, J=7.62 Hz), 7.39 (d, 1H, J=7.62 Hz), 5.38 (s, 2H), 3.87-3.47 (m, 8H), 1.95 (brs, 1H), 0.69-0.72 (m, 4H); ESI-MS mlz: calculated for 432.1. found455.1 [M+Na].

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

Reference：
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;,
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, To a stirred suspension of 4-(bromomethyl)pyridin-2-amine hydrobromide (10.0 g, 37.3 mmol)in acetonitrile (75 mL) was added potassium carbonate (16.0 g, 116 mmol) andcyc?opropyl(piperazin-1-yl)methanone (6.10 g, 39.6 mmol) (CAS-RN 59878-57-8) The mixture was stirred at 75 C for 2 h. Direct silicagel chro matography of the reaction mixture gave a solid which was triturated with ether to give 7.20 g (74 % yield) of the title compound. LC-MS (Method 5): Rt = 0.14 mm; MS (ESIpos): m/z = 261 [M+H]1H-NMR (400 MHz, DMSO-d6) [ppm]: 0.655 (0.49), 0.667 (1.47), 0.674 (3.50), 0.680 (2.08),0.687 (1.70), 0.694 (4.26), 0.699 (3.30), 0.705 (3.66), 0.712 (3.58), 0.717 (4.34), 0.724 (1.98),0.737 (0.54), 1.905 (0.42), 1.917 (0.87), 1.924 (0.93), 1.928 (0.69), 1.936 (1.55), 1.942 (0.73),1.948 (0.90), 1.956 (0.83), 2.304 (1.43), 2.376 (1.45), 2.490 (0.57), 2.495 (1.18), 2.500 (1.61),2.504 (1.18), 2.509 (0.57), 3.332 (16.00), 3.355 (0.68), 3.462 (1.29), 3.599 (0.53), 3.615 (0.43),3.661 (1.28), 5.805 (4.16), 6.408 (3.74), 6.428 (2.21), 6.431 (1.88), 6.441 (2.19), 6.444 (1.89),7.815 (2.34), 7.828 (2.29).

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

Reference：
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

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

To a solution of Intermediate 9 (500 mg, 1.48 mmol) in NMP (6 mL) were added (cyclopropyl)(piperazin-l-yl)methanone (455 mg, 2.95 mmol) and DIPEA (1.3 mL), and the mixture was heated at 140C for 16 h. The reaction mixture was taken up in EtOAc^ (150 mL) and water (50 mL) and the organic layer was washed with water (2 x 50 mL) and brine (50 mL). The organic layer was separated and dried (phase separation cartridge), and the solvent was removed in vacuo. Purification by columnchromatography (Si02, 10-20% EtOAc in isohexane) gave a beige solid (390 mg, 57%). To a solution of this material (390 mg, 0.85 mmol) in DCM (6 mL) was added TFA (3 mL) and the resulting solution was stirred at r.t. for 15 minutes. The solvents were30removed in vacuo. The residue was dissolved in MeOH (5 mL), then placed on an SCX cartridge, washed (MeOH), eluted (7M ammonia in MeOH) and concentrated in vacuo to afford a white solid (304 mg, 100%). To a portion of this material (60 mg, 0.17 mmol) in NMP (1.2 mL) were added DIPEA (0.14 mL) and 4-chloropyrido[3,2-c/]pyrimidine (33 – – mg, 0.2 mmol). The resulting solution was heated under microwave irradiation at 150C for 1 h. Purification by preparative HPLC afforded the title compound (51 mg, 61%) as a beige solid. deltaEta (DMSO-ifc) 8.93-8.88 (2H, m), 8.54 (2H, d, J 11.51 Hz), 8.17 (IH, dd, J 8.46, 1.58 Hz), 7.90 (IH, dd, J 8.46, 4.25 Hz), 7.74 (IH, dd, J 8.94, 6.26 Hz), 7.33 (IH, t, J9.12 Hz), 5.91 (IH, m), 4.05-3.13 (8H, s), 2.58 (3H, m), 2.12-2.07 (IH, m), 1.67 (3H, d, J 6.71 Hz), 0.90-0.73 (4H, m). LCMS (ES+) 486 (M+H)+, RT 2.78 minutes (Method 2).

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

Reference：
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MATTEUCCI, Mizio; OWENS, Andrew, Pate; RAPHY, Gilles; SHARPE, Andrew; WO2011/58108; (2011); 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

To a solution of Intermediate 9 (500 mg, 1.48 mmol) in NMP (6 mL) were added (cyclopropyl)(piperazin-l-yl)methanone (455 mg, 2.95 mmol) and DIPEA (1.3 mL), and the mixture was heated at 140C for 16 h. The reaction mixture was taken up in EtOAc^ (150 mL) and water (50 mL) and the organic layer was washed with water (2 x 50 mL) and brine (50 mL). The organic layer was separated and dried (phase separation cartridge), and the solvent was removed in vacuo. Purification by columnchromatography (Si02, 10-20% EtOAc in isohexane) gave a beige solid (390 mg, 57%). To a solution of this material (390 mg, 0.85 mmol) in DCM (6 mL) was added TFA (3 mL) and the resulting solution was stirred at r.t. for 15 minutes. The solvents were30removed in vacuo. The residue was dissolved in MeOH (5 mL), then placed on an SCX cartridge, washed (MeOH), eluted (7M ammonia in MeOH) and concentrated in vacuo to afford a white solid (304 mg, 100%). To a portion of this material (60 mg, 0.17 mmol) in NMP (1.2 mL) were added DIPEA (0.14 mL) and 4-chloropyrido[3,2-c/]pyrimidine (33 – – mg, 0.2 mmol). The resulting solution was heated under microwave irradiation at 150C for 1 h. Purification by preparative HPLC afforded the title compound (51 mg, 61%) as a beige solid. deltaEta (DMSO-ifc) 8.93-8.88 (2H, m), 8.54 (2H, d, J 11.51 Hz), 8.17 (IH, dd, J 8.46, 1.58 Hz), 7.90 (IH, dd, J 8.46, 4.25 Hz), 7.74 (IH, dd, J 8.94, 6.26 Hz), 7.33 (IH, t, J9.12 Hz), 5.91 (IH, m), 4.05-3.13 (8H, s), 2.58 (3H, m), 2.12-2.07 (IH, m), 1.67 (3H, d, J 6.71 Hz), 0.90-0.73 (4H, m). LCMS (ES+) 486 (M+H)+, RT 2.78 minutes (Method 2).

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

Reference：
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MATTEUCCI, Mizio; OWENS, Andrew, Pate; RAPHY, Gilles; SHARPE, Andrew; WO2011/58108; (2011); 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.

At room temperature 1-cyclopropane carboxylic acid piperazine (2.37g, 15.37mmol) and p-formyl benzene boronic acid (1.92g, 12.81mmol) Was dissolved in dichloromethane (40ml), stirred for 1 hour at room temperature, again was added sodium cyanoborohydride (1.77g, 28.18mmol), Was stirred at room temperature until the reaction is complete as monitored by TLC, water was added 20ml, extracted with dichloromethane, washed with saturated brine twice, The organic phase was dried over anhydrous magnesium sulfate, and concentrated under reduced pressure, to give: (4-benzyl-acid – piperazin-1-yl) – cyclopropyl – methanone, (1.6 g of, White solid), yield: 43.4%, was used directly in the next reaction., 59878-57-8

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

Reference：
Patent; SHANGHAI CDYMAXPHARMACEUTICALS CO LTD; An, Xiao Xia; Bie, Ping Yan; Liu, Jun; Yang, Wuli; (43 pag.)CN103087077; (2016); B;,
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 the reaction flask was added compound 6 (prepared in Example 3-2, 256.5g,0.86mol), CDI (139.45g, 0.86mol), 1.6LTHF, after stirring for 0.5h Compound 7 (138.8g,0.90mol) at room temperature The reaction 3h, after completion of the reaction, water was added to quench the reaction, of THF was distilled off under reduced pressure, theresidue was dissolved in ethyl acetate was added, the organic phase was separated,washed with water three times, the organic phase was dried over anhydrous Na 2SO 4Dried,filtered and concentrated to give Ola Trapani (356.3g, 0.82mol), yield 95%, HPLC purity 99.8%.

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

Reference：
Patent; Shandong Luoxin Pharmaceutical Group Heng Xin Pharmaceutical Co. Ltd.; Li, Hua; Wang, Chunyan; Liu, Shuxin; (8 pag.)CN105820126; (2016); A;,
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, (d) Library Synthesis (5a-h)To a solution of 3-(4-oxo-3,4,5,6,7,8-hexahydro-phthalazin-1-ylmethyl)-benzoic acid (4) (20 mg, 0.07 mmol), in DCM (1 ml) was added HBTU (53 mg, 0.140 mmol), triethylamine (20 muL, 0.140 mol) and amine (0.140 mmol). The reaction mixture was stirred for 18 hours at room temperature and concentrated in vacuo. The crude samples were submitted for preparative HPLC purification.

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

Reference：
Patent; Javaid, Muhammad Hashim; Menear, Keith Allan; Martin, Niall Morrison Barr; Smith, Graeme Cameron Murray; Rudge, David Alan; Roberts, Craig Anthony; US2009/23727; (2009); 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: The appropriate piperazine derivative (1.34mmol) and K2CO3 (180mg, 1.34mmol) were added to a solution of the appropriate 3-(4-(n-iodoalkoxy)phenyl)thiazolidine-2,4-dione (11, 0.67mmol) in MeCN (6mL). The reaction mixture was stirred at room temperature for 9h. The mixture was quenched by addition of water and extracted with DCM. The organic layer was dried over anhydrous MgSO4, filtered and evaporated under reduced pressure. The residue was purified by column chromatography (SiO2, DCM/MeOH= 15/1 v/v including 1% of NH4OH).

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

Reference：
Article; Elkamhawy, Ahmed; Kim, Nam youn; Hassan, Ahmed H.E.; Park, Jung-eun; Yang, Jeong-Eun; Oh, Kwang-Seok; Lee, Byung Ho; Lee, Mi Young; Shin, Kye Jung; Lee, Kyung-Tae; Hur, Wooyoung; Roh, Eun Joo; European Journal of Medicinal Chemistry; vol. 157; (2018); p. 691 – 704;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

(Formula 5-4: methyl 4-((N-(3-(benzo[d][1,3]dioxol-5-yl)phenyl)-4-(cyclopropanecarbonyl)piperazine-1-carboxamido)methyl)benzoate)[1167][1168]Compound ofFormula 5-3(methyl 4-(((3-(benzo[d][1,3]dioxol-5-yl)phenyl)((4-nitrophenoxy)carbonyl)amino)methyl)benzoate; 0.180 g, 0.342 mmol) was dissolved in dimethylformamide (2 mL), and then cyclopropyl(piperazin-1-yl)methanone(0.158 g, 1.03 mmol) and potassium carbonate (0.142 g, 1.03 mmol) were added and stirred at 50 C for 16 hours. After completion of the reaction, the organic layer was extracted with ethyl acetate and saturated ammonium chloride aqueous solution, dehydrated with anhydrous magnesium sulfate, and then filtered. The filtrate was concentrated under reduced pressure, and then the residue was purified and concentrated by column chromatography (silica; ethyl acetate/hexane= 30%) to give the desired compound ofFormula 5-4(0.096 g, 52%) in the form of a yellow liquid.

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

Reference：
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Changsik; YANG, Hyun-Mo; CHOI, Hojin; KIM, Dohoon; KIM, Soyoung; HA, Nina; LIM, Hyojin; KO, Eunhee; YOON, Seongae; BAE, Daekwon; WO2014/178606; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics