Heterocyclic Building Blocks-piperazine

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
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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;,
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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;,
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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;,
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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;,
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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
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

[Referential Example 158] 1-Benzyl-4-tert-butoxycarbonylpiperazine In acetonitrile (80 ml), tert-butyl 1-piperazine carboxylate (2.50 g) was dissolved. Under ice cooling,benzyl bromide (1.59 ml) and triethylamine (1.87 ml) were added dropwise to the resulting solution, followed by stirring at room temperature for 90 minutes. After the solvent was distilled off under reduced pressure, distilled water and dichloromethane were added to the residue to separate the organic layer. The organic layer was washed with saturated aqueous NaCl solution and dried over anhydrous sodium sulfate. The residue obtained by distilling off the solvent under reduced pressure was purified by chromatography on a silica gel column (ethyl acetate: hexane = 1:20 to 1:5), whereby the title compound (3.12 g, 84%) was obtained as colorless powder. 1H-NMR (CDCl3) delta: 1.45(9H,s), 2.38(4H,t,J=4.9Hz), 3.42(4H,t,J=4.8Hz), 3.51(2H,s), 7.25-7.29(1H,m), 7.30-7.33(4H,m). MS (EI) m/z: 276M+.

57260-71-6, As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1104754; (2001); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

?To a solution 6-chiora-M-(3-nitrophenyl)pvrimidin-4-amine (1.0 g, 4.00 minol) in2 -hutanol (10 mL) and trifluoroacetic acid (0.3 mL) was added 2-methoxv-4.4-niethylpiperazin-i-yl)anihne (6o6irig, 4.39 inmol). The reaction mixture was stilTed at 120 C for 10 hrs and the solvent concentrated undcr reduced pressure. The reaction mixture was diluted with dichloromethane and washed with saturated aqueous potassium carbonate solution and brine. The organic layer was dried over Mg504, filtered through a pad of celiteand concentrated under reduced pressure. The residue was purified by column chromatography on silica gel (1:99 to 3:97, ammonia solution 7.0 N in methanol/dichloromethane) to afford N4-(2-methoxy-4-(4-methyipiperazin- 1 -yi)phenyl)-N6- (3-nitrophenyflpyrimidine-4,6-dianiine (1.3 g, 75% yield) as an solid. Rt = 2.73 mm; ?H NMR 600 MHz (DMSO-d6) d 9.50 (s, lH), 8.72 Cc, lH), 8.24 (s, 1H), 8.22 (s, IH), 7.91 (dd, J::: 1.2 Fiz,J 8.4 Hz, iLl), 7.27 (d,J 8.4 Hz, HI), 7.50 (j,J::: 8.4 Hz, iLl), 7.21 (d,J 8.4 Hz, 1H), 6.49 (d,J= 2.4 Hz, 1H). 6.51 (dd,J= 2.4 Hz,J= 9.0 Hz, 1H), 5,76 (s, 1H), 3,77 (s, 3W). 3.16 (in, 4ff). 2,46 (rn, 4ff), 2.32 (s, 3H,); MS mAr: 436.45 [M+i].

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael; CHOI, Hwan Geun; TAN, Li; WO2015/6492; (2015); 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.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

To a solution of 4- (4-methylpiperazin-1-yl) benzylamine (43 mg, 0.21 mmol) in toluene (4 mL) under nitrogen protection was added trimethylaluminum (0.2 mL, 1 M n-hexane solution), The reaction system was stirred at room temperature for 15 minutes, and 4,9-dioxo-4,9-dihydrothiazolo [5,4-g] isoquinoline-2-carboxylic acid ethyl ester (20 mg, 0.07 mmol) was added. The reaction system Stir at 90 C for 5 hours.The reaction solution was concentrated under reduced pressure andpurifiedby prep-HPLC (NH4HCO3system) to obtain compound 8 (2 mg, yield: 7%) as a yellow solid.

216144-45-5, 216144-45-5 4-(4-Methylpiperazin-1-yl)benzylamine 2776493, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shanghai Dinuo Pharmaceutical Technology Co., Ltd.; Zhao Zhiming; (42 pag.)CN110467629; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics