Month: June 2021

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 51f (50 mg, 1 eq) in DMSO (0.5 mL), is added 1-cyclopropylpiperazine (38 mg, 2 eq), Et3N (19 muL, 1.1 eq) and heated at 50 C. during 2 h. Ammonium acetate (500 mg) is added and the solution is heated at 140 C. during 1 h. The solution is diluted with H2O/AcOH and purified by prep HPLC to give 5008 (8 mg, 13%)., 20327-23-5

20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2010/261714; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

24860-46-6, 2-(2-Oxopiperazin-1-yl)acetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Palladium (0.161 g, 10% on carbon) was added to a mixture of 2-Oxo-1-piperazineacetic acid (0.497 g, 3.14 mmol) and (2-Oxo-ethyl)-carbamic acid tert-butyl ester (0.503 g, 3.16 mmol) in methanol (6.2 mL) under argon. The flask was evacuated and the reaction placed under a hydrogen atmosphere for 22 h. The reaction was filtered through a Celite -plugged filter frit, washed with methanol and DCM, and concentrated in vacuo to afford crude product which was carried to the next step without purification. ESI-MS m/z 324 (M+Na)+., 24860-46-6

24860-46-6 2-(2-Oxopiperazin-1-yl)acetic acid 23422809, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; VENATORX PHARMACEUTICALS, INC.; BURNS, Christopher, J.; DAIGLE, Denis; LIU, Bin; MCGARRY, Daniel; PEVEAR, Daniel, C.; TROUT, Robert, E. Lee; WO2014/151958; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(2R,6S) and (2S,6R)-1,2,6-Trimethylpiperazine. To a solution of cis-3,5-dimethylpiperazine-1-carboxylic acid t-butylester (2.0 g, 9.22 mmol) in MeOH (25 mL), paraformaldehyde (0.84 g, 28 mmol) and zinc chloride (3.83 g, 28 mmol) were added. Then sodium cyanoborohydride (1.76 g, 28 mmol) was added in portions. The reaction mixture was stirred at rt. for 4 hr. Then insoluble solid was filtered out and the filtrated was concentrated. The residue was participated between saturated NaHCO3 solution and CH2Cl2 (2×50 mL). The organic layers were combined, dried (MgSO4) and concentrated to give a colorless oil. It was then dissolved in CH2Cl2 (10 mL) and TFA (2.5 mL) was added. The reaction mixture was stirred at rt. for overnight. TFA and solvent were evaporated to give a white solid as final product as TFA salt. (2.6 g, 86% yield); MS m/129(MH+). 1H NMR (500 MHz, CHLOROFORM-D) delta ppm 1.41 (d, J=6.41 Hz, 6H) 2.87 (s, 3H) 3.38-3.56 (m, 4 H) 3.71-3.90 (m, 2H).

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

Reference：
Patent; Bristol-Myers Squibb Company; US2007/270406; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

373608-48-1, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,373608-48-1

Step 3: ieri-butyl 4-{3-[(2-oxo-2H-chromen-4-yl)amino]propyl} piperazine-1 -carboxylate (68c). A solution of intermediate 68b (1 .1 g, 4.5 mmoles, 1 .1 eq.), triethylamine (0.674 mL, 4.8 mmoles, 1 .2 eq.) and 2-oxochromen-4-yl trifluoromethanesulfonate 28a (1 .2 g, 4.1 mmoles, 1 eq.) in acetonitrile (20 mL) was heated to 705C for 1 hour. The reaction mixture was concentrated under reduced pressure and the residue was partitioned between dichloromethane and a brine/sodium bicarbonate mixture (1 :1 ). The mixture was filtered through a hydrophobic frit (Phase Separator) washing with dichloromethane. The organic phase was evaporated under reduced pressure and the residue was chromatographed on silica gel (SNAP50) eluting with a gradient of EtOAc in cyclohexane to give ferf-butyl 4-{3-[(2-oxo- 2H-chromen-4-yl)amino]propyl}piperazine-1 -carboxylate 68c (700 mg, Y=44%). LC-MS (M-H+) = 388.3.

373608-48-1 tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate 17750945, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.; OMBRATO, Rosella; GAROFALO, Barbara; MANGANO, Giorgina; CAPEZZONE DE JOANNON, Alessandra; CORSO, Gaia; MAGARO’, Gabriele; FURLOTTI, Guido; IACOANGELI, Tommaso; (108 pag.)WO2016/96631; (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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

694499-26-8, To a solution of 150 58a (30mg, 0.08mmol) in 77 DMF (5mL) were added 147 4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (27.3mg, 0.10mmol), 79 HATU (45.6mg, 0.12mmol) and DIEPA (20.6mg, 0.16mmol). The resulting mixture was stirred at room temperature for 2h. Then it was diluted with EtOAc (50mL), washed with water (50mL×3) and brine (100mL). The organic layers were dried over anhydrous sodium sulfate and concentrated. The residue was diluted with DCM (1mL) and CF3COOH (0.5mL). The reaction mixture was stirred at room temperature for 4h and then the pH value was adjusted to 12 with saturated sodium bicarbonate. The mixture was extracted by 80 EtOAc (50mL) and washed with water (50mL×2) followed by brine (50mL). The organic layers were dried over sodium sulfate, filtered, concentrated and purified by silica gel column chromatography (eluting with 0-10% MeOH in 81 DCM) to afford 151 38 (23mg, 52%) as a gray solid.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Liu, Xuesong; Wang, Beilei; Chen, Cheng; Jiang, Zongru; Hu, Chen; Wu, Hong; Zhang, Yicong; Liu, Xiaochuan; Wang, Wenliang; Wang, Junjie; Hu, Zhenquan; Wang, Aoli; Huang, Tao; Liu, Qingwang; Wang, Wei; Wang, Li; Wang, Wenchao; Ren, Tao; Li, Lili; Xia, Ruixiang; Ge, Jian; Liu, Qingsong; Liu, Jing; European Journal of Medicinal Chemistry; vol. 160; (2018); p. 61 – 81;,
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

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

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 °C for 6-10 h. The solvent was evaporated in vacuo. The residue was dissolved in CH2Cl2 (25 mL), washed with water (20 mL × 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.

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
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

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add cis-2,6-dimethylpiperazine (1.0 g, 8.76 mmol) to a 100 mL single-mouth bottleAnd dichloromethane(20mL),Cool down to 0-5 C.Add triethylamine (2.22 g, 21.89 mmol),A solution of (Boc) 2O (1.92 g, 8.76 mmol) in dichloromethane (10 mL) was added dropwise.Warm to room temperature and stir overnight. The reaction was monitored by TLC. After the reaction was completed, the reaction mixture was concentrated under reduced pressure and purified by column chromatography.Eluent: DCM/MeOH = 30/1,The collected product was concentrated under reduced pressure to give 1.9 g.

21655-48-1, As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference：
Patent; Beijing Purunao Bio-technology Co., Ltd.; Zhang Peilong; Shi Hepeng; Lan Wenli; Song Zhitao; (250 pag.)CN108707139; (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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

To a stirred solution of 1-Z-piperazine (8.5 g, 38.5 mmol) in dry THE (100 mL), 1,1- thiocarbonyldimidazole (12.37 g, 69.4 mmol) was added and the mixture was stirred at 60°C for 5 h. It was concentrated under vacuum and NH3 in EtCH (2 N, 300 mL) was added at 0°C. The resulting mixture was stirred at 55°C for 8 h in an autoclave. It was diluted withwater (100 mL) and extracted with DCM (2 x 100 mL). The DCM layer was washed with water (100 mL), dried over in anhydrous Na2SO4 and concentrated. The resulting crude product was purified by flash chromatography to afford the title product. Yield: 87percent (7 g, white solid). 1H NMR (400 MHz, DMSO-d6): 6 7.51 (5, 2H), 7.38-7.31 (m, 5H), 5.1 (5, 2H), 3.78 (m, 4H), 3.43-3.33 (m, 4H). LCMS: (Method A) 280.2 (M+H), Rt. 2.33 mm, 95.4percent (Max).

31166-44-6, As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference：
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh, S.; GIRI, Awadut, Gajendra; (280 pag.)WO2017/144633; (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.112984-60-8,6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Synthesis of 6-Ffuoro-7-{4-[5-hydroxy-6-(2-methyl-5-nitro- imidazoi-I-yi)-hexyl]-piperazin-I-yi}-l -methyS-4-oxo-4H-2-thia-8b-aza- cyclobu a[a]naphthaSene-3-carboxylic acid (1 15): To a stin-ed solution of 6- Fluoro- 1 -methy-4-oxQ-7-piperazin- 1 -yl-4H-2-thia-8P-aza- cyclobuta[a]naphthalene-3-carboxylic acid, (HI) ( 1 .10 g, 3.16 mmol) in dimethylformamide (30ml) was added potassium carbonate (0.43g, 3.16 mmol) followed by addition of compound (II) (0.85g, 2.63 mmol) and the reaction 1 26 mixture was stirred at RT for 1 6h. The reaction mixture was diluted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while euting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (115) with 20% isolated yield. 1 H-NMR (400 MHz, DMSO) delta ppm: 1 .61 – 1 -68(6H, m, CH2), 2.1 (3H, d, J = 6 Hz, CH3), 2.44 (3H, s, CH3) , 2.54 (4H, m, 2 xCH2), 3.2 (4H, m, 2 xCH2), 3.9-4. 1 (2H. m, 2 x CH2N), 4.38( 1 H, d, J = 14, CHOH). 5.2 1 1 H, d, J = 4.4, OH), 6.38 ( 1 H, d, J = 5.6Hz, CHSN) 6.9 ( 1 H, d, J = 6.8, Ar-H). 7.78 ( 1 H, d, J = 1 4 Hz, Ar-H). 8.02 ( 1 H, s, Ar-H). ESI-MS (m/z): 575(M+H)

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics