Heterocyclic Building Blocks-piperazine

185110-19-4, 2-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 3: (+/-)-Methyl {3-[4-(trifluoromethyl)phenyl]piperazin-l-yl} acetate; A mixture of the piperazine described in Step 2 above (2.1g, 9mmol), methyl bromoacetate (ImL, 9mmol) and potassium carbonate (2.4g, 18mmol) in acetonitrile (3OmL) was stirred overnight at room temperature. The mixture was filtered, evaporated and purified on silica using 25-50% ethyl acetate in z’s¡ã-hexane as eluant.1H NMR (500MHz, CDCl3): delta 2.22 (IH, t, J 10.6), 2.37-2.43 (IH, m), 2.93 (2H, t, J 9.4), 3.10- 3.17 (2H, m), 3.26 (2H, s), 3.72 (3H, s), 7.52 (2H, d, J 8.1), 7.58 (2H, d, J 8.2).

185110-19-4, The synthetic route of 185110-19-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME LIMITED; MERCK & CO., INC.; WO2007/125364; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2759-28-6,1-Benzylpiperazine,as a common compound, the synthetic route is as follows.

Synthesis of 1-(1,1-dimethylethoxycarbonyl)4-phenylmethylpiperazine STR30 A solution of 3.4 g (0.024 mole) of 1,1-dimethylethoxy carbonylazide in 5 ml of pyridine was rapidly added to a stirred solution of 1-phenylmethylpiperazine (4.2 g, 0.024 mole) in 5 ml of pyridine. An initial exothermic reaction was noted. The mixture was allowed to stir overnight, diluted with water and the product was extracted with two 50 ml portions of ether. The ether extracts were dried (MgSO4), filtered, and evaporated to yield a yellow oil. Column chromatography (2″ diameter column, 500 g of silica gel, ether eluent) followed by sublimation at 110/0.5 mm returned 5.7 g (86%) of white solid, m.p. 64-73. The solid was dissolved in 50 ml of ether and cooled to -70. The resultant white solid was filtered off to yield 4.5 g (68%) of product, m.p. 71-3. Calc. for C16 H24 N2 O2 (276.38): C, 69.53; H, 8.75; N, 10.14. Found: C, 69.44; H, 8.82; N, 10.15.

2759-28-6, 2759-28-6 1-Benzylpiperazine 75994, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ICI Americas Inc.; US4247549; (1981); A;,
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143673-66-9, (R)-3-Isopropylpiperazine-2,5-dione is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0561] To a solution of compound 4-01-4 (11 g, 70 mmol) in dichloromethane (500 mL) was added trimethyloxonium tetrafiuorob orate (41.7 g, 282 mmol). The slurry was stirred vigorously at 20C under a nitrogen atmosphere for 18 hours. The slurry became a clear solution with very viscous yellow oil settled on the bottom of the flask, then another 10.4 g (70 mmol) of trimethyloxonium tetrafiuorob orate was added and the mixture was stirred at 20C for 24 hours. The mixture was cooled in an ice bath, and 200 g of ice and 100 mL of concentrated ammonium hydroxide solution (30%) were added. The reaction mixture was stirred in an ice bath for 1 hour. The layers were separated and aqueous layer was extracted with DCM (500 mL*2). The combined organic layers were washed with saturated sodium bicarbonate solution (300 mL *2) and brine (300 mL), dried over anhydrous sodium sulfate, filtered through a celite pad, and concentrated under reduced pressure. The residue was purified by column chromatography (petroleum ether to petroleum ether: ethyl acetate = 10: 1) to afford compound 4-01-5 (9 g, 69% yield) as yellow oil.

143673-66-9, As the paragraph descriping shows that 143673-66-9 is playing an increasingly important role.

Reference£º
Patent; CORNELL UNIVERSITY; TRI-INSTITUTIONAL THERAPEUTICS DISCOVERY INSTITUTE; LIN, Gang; NATHAN, Carl; KIRKMAN, Laura; ZHAN, Wenhu; MORGAN, Trevor; SATO, Kenjiro; HARA, Ryoma; KAWASAKI, Masanori; IMAEDA, Toshihiro; TOITA, Akinori; OKAMOTO, Rei; YUKAWA, Takafumi; ASO, Kazuyoshi; WONG, Tzu-Tshin; GINN, John, D.; FOLEY, Michael, A.; (296 pag.)WO2019/75259; (2019); A1;,
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2759-28-6, 1-Benzylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Amine (1 mmol) and di-tert-butyl dicarbonate [(Boc)2O] (1.1 mmol) were placed in a microwave reaction vial. The LG microwave oven MG 555f was programmed to 300 W at 100 C. The reaction was monitored using TLC. After the reaction, ice water was added to the reaction mixture which resulted in the precipitation of the product. The solid product was merely filtered off and washed with excess cold water. The product was pure enough for all practical purposes. For characterization purpose, it was further purified by column chromatography (Neutral Alumina as adsorbent, solvent system: Hexane: Ethyl acetate (7.5:2.5)).

2759-28-6, The synthetic route of 2759-28-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Dighe, Satish N.; Jadhav, Hemant R.; Tetrahedron Letters; vol. 53; 43; (2012); p. 5803 – 5806;,
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511254-92-5, (S)-1-Benzyl-2-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

511254-92-5, Step 3: (S)-1-benzyl-2-methyl-4-(1-methylpiperidin-4-yl)piperazine (S)-1-Benzyl-2-methylpiperazine (6.84 g, 36 mmol), 1-methyl-4-piperidone (4.87 g, 43 mmol), and glacial acetic acid (4.32 g, 72 mmol) were successively added to anhydrous ethanol (100 mL). The resultant was stirred for 1 hour, and then cooled to 0C. Sodium triacetoxyborohydride (31.6 g, 150 mmol) was added in portions. The resultant was reacted at room temperature for 6 hours. The solvent was evaporated, and the residue was dissolved by adding ethyl acetate. The resultant was washed by water, dried, concentrated, and purified by silica gel column chromatography to give (S)-1-benzyl-2-methyl-4-(1-methylpiperidin-4-yl)piperazine (7.86 g, 76% yield). MS m/z [ESI]: 288.2 [M+1].

511254-92-5 (S)-1-Benzyl-2-methylpiperazine 28406010, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Chia Tai Tianqing Pharmaceutical Group Co.,Ltd; Centaurus BioPharma Co., Ltd.; Lianyungang Runzhong Pharmaceutical Co., Ltd.; XIAO, Dengming; XU, Xinhe; LIU, Xijie; HU, Yuandong; YU, Honghao; LIU, Zhihua; PENG, Yong; SUN, Yinghui; LUO, Hong; KONG, Fansheng; HAN, Yongxin; SUN, Jian; EP2952510; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.623586-00-5,(R)-1-Cbz-3-methylpiperazine,as a common compound, the synthetic route is as follows.

623586-00-5, A mixture of (R)-benzyl 3-methylpiperazine-1-carboxylate (4.8 g, 20.5 mmol) from step (a) above, 1,3-bis(tertbutoxycarbonyl)-2-methylisothiourea (6.5 g, 23 mmol, Aldrich), and triethylamine (3.4 mL, 24.6 mmol, Aldrich) in DCM (140 mL) was added mercury(II)chloride (5.8 g, 21.6 mmol, Aldrich). The reaction mixture was stirred at RT for 16 h. Then, the mixture was filtered and the solid was washed with DCM (2*100 mL). The combined filtrates were concentrated in vacuo and the residue was purified on silica gel using ISCO Combiflash system with DCM/2M methanolic ammonia gradient to give the title compound as a white solid. MS (ESI, positive ion) m/z: 477 (M+1).

The synthetic route of 623586-00-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Gore, Vijay Keshav; Ma, Vu Van; Norman, Mark H.; Ognyanov, Vassil I.; Xi, Ning; US2006/84640; (2006); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.128019-59-0,4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

61 (B) 4-Methyl-piperazine-1,3-dicarboxylic acid 1-tert-butyl ester The crude piperazine-1, 3-dicarboxylic acid-1-tert-butyl ester (4.92 mmol), prepared as described in 62 (A), was suspended in dry acetonitrile (30 mL) under nitrogen atmosphere and formaldehyde (37% wt. aqueous solution, 367 mL, 4.92 mmol) and Na (OAc) 3BH (2.3 g, 10. 82 mmol) were added. The resulting mixture was stirred at R. T. for 3h, then a saturated aqueous solution of NaHC03 was slowly added until the pH was adjusted to 7. The mixture was concentrated to dryness under reduced pressure to give a yellow solid that was used without further purification for the next step. LCMS (Tr): 3.19 min (Method B); MS (ES+) gave m/z : 245.0., 128019-59-0

As the paragraph descriping shows that 128019-59-0 is playing an increasingly important role.

Reference£º
Patent; ADDEX PHARMACEUTICALS SA; WO2005/44797; (2005); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Example 15.1.2: Preparation of 4-[2-(2-Amino-benzoimidazol-l-yl)-ethyl]- piperazine-1-carboxylic acid tert-butyl ester; 4-[2-(2-Amino-benzoimidazol-l-yl)-ethyl]-piperazine-l-carboxylic acid tert-butyl ester was prepared according to the procedure described in WO2005/058869. 1H NMR (300MHz, CDCl3): delta 7.43 (IH, d, J = 7.5 Hz, Ar-CH), 7.17-7.06 (3H, m, Ar- CH), 5.78 (2H, s, NH2), 3.64 (2H, t, J = 5.7 Hz, NCH2CH2N), 3.46 (4H, m, CH2NCH2), 2.56 (4H, m, CH2NCH2), 2.43 (2H, t, J = 5.7 Hz, NCH2CH2N), 1.46 (9H, s, C[CH3J3). MS (ESI+) m/z 346 (M+ 1)., 208167-83-3

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AVEXA LIMITED; WO2008/77188; (2008); A1;,
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892242-64-7, 4-((3-(4-Cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

892242-64-7, About 21kg of 4-((3-(4-cyclohexylpiperazin-l-yl)-6-oxo-6H-anthra[l,9- cd]isoxazol-5-yl)amino)benzoic acid was slurred in 625L of 0.4 M NaOH in MeOH and purified water (4: 1) solution under about 40-45C for about 2-4 hours. Then slowly cooled the reaction to room temperature and stirred for another 2-4 hours. After confirmed the reaction completion by HPLC, the solid was centrifuged and washed with about 57L of MTBE. The wet cake was re- suspended in about 245L of 0.1M NaOH in MeOH/H20 solution under room temperature. The wet cake was centrifuged and washed with about 56L of MTBE again. The filtered solid was re- suspended in about 250L of MTBE under room temperature for about 1-2 hours. The solid was separated and dried at 25-30C under reduced pressure for 12-24 hours to obtain the final product with purity more than 99.9% (HPLC) and about 90% yield. Mass spectra give [M+l] = 523.2. 1H-NMR (400 MHz, DMSO-d6, see Figure 1), ppm (delta): 11.79 (IH, s), 8.48 (IH, d), 8.20 (IH, d), 7.93 (2H, d), 7.84 (IH, t), 7.72 (IH, t), 7.35 (2H, d), 6.39 (IH, s), 3.85 (4H, m), 2.72- 2.70 (4H, m), 2.28-2.265 (IH, m), 1.72-1.78 (4H, m), 1.55-1.58 (IH, m), 1.08-1.23 (5H, m). Sodium content: 3.8%. The Raman spectrum is shown in Figure 4, and the XRPD data is given in Table 1 below and Figure 2, IR spectra is given in Figure 5 and DSC spectra is given in Figure 3. These data confirm the stable crystalline polymorphic form (Form A) of the compound of Formula I.

The synthetic route of 892242-64-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PURDUE PHARMA L.P.; WU, Jay Jie-Qiang; WANG, Ling; (31 pag.)WO2017/27465; (2017); A1;,
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34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0209] Step 1. To a solution of N-(l-(lH-indol-3-yl)hexan-2-yl)-2-bromothiazole-5- carboxamide (0.10 g, 0.24 mmol) and 4-methylpiperazin-2-one (0.03 g, 0.29 mmol) in dioxane (7 mL), Cs2C03 (0.23 g, 0.72 mmol) and 2-(dicyclohexylphosphino)3,6-dimethoxy-2′,4′,6′- triisopropyl-l,l’-biphenyl (BrettPhos precatalyst; 0.02 g, 0.02 mmol) were added. The reaction vessel was purged with argon for 20 min and the mixture was then heated at 110 C for 16 h. The reaction mixture was filtered through diatomaceous earth, washing with 5% MeOH in DCM (2 x 10 mL). The filtrate was concentrated, and the crude obtained was purified by column chromatography (silica, 100-200 mesh, 1 to 4% MeOH in DCM) and preparative HPLC to afford the title compound (0.03 g, 14%) as a white solid. HPLC Purity: 99.4%; MS (ESI) m/e [M+H]+/Rt/%: 440.00/2.69/98.0%; 1H NMR (400 MHz, DMSO-d6) delta 0.81 (t, 7 = 6.8 Hz, 3H), 1.19-1.35 (m, 4H), 1.47-1.63 (m, 2H), 2.31 (s, 3H), 2.81 (t, 7 = 5.4 Hz, 2H), 2.85-2.97 (m, 2H), 3.34 (s, 2H), 4.03 (t, 7 = 5.6 Hz, 2H), 4.16 (m, 1H), 6.92-6.98 (m, 1H), 7.04 (t, 7 = 7.6 Hz, 1H), 7.11 (d, 7 = 1.5 Hz, 1H), 7.31 (d, 7 = 8.3 Hz, 1H), 7.58 (d, 7 = 7.8 Hz, 1H), 8.13 (s, 1H), 8.24 (d, 7 = 8.8 Hz, 1H), 10.75 (brs, 1H).

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; STOCKING, Emily, M.; HALL, Adrian; MACCOSS, Malcolm; (139 pag.)WO2017/20010; (2017); A1;,
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