Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of Intermediate 4 (0.38 g, 2.06 mmol) in DMF (20 mL) were added tert-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1 g, 4.12 mmol) and DIPEA (0.4 g, 3.0 mmol). The reaction mixture was heated at 100C for 5 h, allowed to cool, then stirred at room temperature for 2 days. The reaction mixture was concentrated in vacuo, then partitioned between water and DCM. The organic phase was separated and concentrated in vacuo. The resulting crude material was purified by column chromatography (silica gel: 100-200 mesh, MeOH:DCM gradient 0% to 20%) to give a pale yellow foam. The foam was dissolved in DCM (1 mL) and TFA (2 mL) and stirred for 1 h. The reaction mixture was concentrated in vacuo, then triturated with diethyl ether, to give the title compound (0.6 g) as a sticky yellow solid., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference£º
Patent; UCB PHARMA S.A.; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D; BROOKINGS, Daniel Christopher; FORD, Daniel James; FRANKLIN, Richard Jeremy; GHAWALKAR, Anant Ramrao; KULISA, Claire Louise; NEUSS, Judi Charlotte; REUBERSON, James Thomas; WO2013/68458; (2013); A1;,
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414910-15-9, tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1 -Tertbutoxycarbonyl-4-(cyclopropanecarbonyl)piperazine (190 mg, 0.75 mmol) was dissolved in dichloromethane, and then trifluoroacetic acid (1 mE) was added. The reaction mixture was stirred at room temperature until complete reaction, and then washed with saturated sodium bicarbonate solution for three times. The organic phases were concentrated to give 112mg (yield 97%) pale yellow solid of N-(cyclopropanecarbonyl) piperazine for use.

414910-15-9, As the paragraph descriping shows that 414910-15-9 is playing an increasingly important role.

Reference£º
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;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-Butyl (25)-2-methylpiperazine-1-carboxylate ( 43.1 g, 215 mmol) was added to asolution of aldehyde from Preparation 3 (39.0 g, 195 mmol) in dichloromethane (780mL). The reaction mixture was stirred at room temperature for 10 min then sodiumtriacetoxyborohydride (83.1 g, 391 mmol) was added portion-wise. On complete30 addition the reaction mixture was stirred at room temperature for 4 h. The reaction mixture was carefully quenched with water (200 mL) and extracted withdichloromethane (200 mL). The organic layer was dried over sodium sulphate andconcentrated under reduced pressure. Trituration of the crude product with n-pentane afforded the title compound as an off-white solid. (43.0 g, 57.3%)5 1H NMR (300MHz, DM50-d6) o =7.92 (d, 1=2.2 Hz, lH), 7.68 (d, 1=2.2 Hz, lH), 4.09(m, lH), 3.67 (br d, J= 13.1 Hz, lH), 3.52 (s, 2H), 2.88-3.02 (m, lH), 2.69 (br d,J=ll.l Hz, lH), 2.57 (br d, 1=11.3 Hz, lH), 2.35 (s, 3H), 2.15 (dd, 1=11.3, 3.6 Hz, lH),1.98 (td, 1=11.7, 3.4 Hz, lH), 1.39 (s, 9H), 1.13 (d, J=6.7 Hz, 3H). LCM5 Method 1:10m/z 384.66 [M+H+]; RT = 3.47 min

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; LEO PHARMA A/S; JESSIMAN, Alan Stuart; JOHNSON, Patrick Stephen; MAANSSON, Kristoffer; S?RENSEN, Morten Dahl; (156 pag.)WO2018/11201; (2018); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

Example 58(4-cyclopentylpiperazin-1-yl)(7-(methylsulfonyl)-7-azaspiro[3.5]nonan-2-yl)methanone Oxalyl chloride (85 mul, 0.97 mmol) was slowly added to a solution of Intermediate 26 in DCM (12 mL) at 0 C. One drop of DMF was added and the reaction mixture was stirred for 4 h. The solvent was concentrated. The residue was quickly recovered in DCM (5 mL) and added to a solution of 1-cyclopentylpiperazine (54.9 mg, 0.36 mmol) and Et3N (0.135 mL, 0.97 mmol) in DCM (12 mL) at 0 C. The reaction mixture was allowed to warm to ambiant temperature and stirred for 1 h. The solvent was concentrated and the product was purified on silica gel (24 g) by MPLC using MeOH 5%, acetone 10% in DCM as eluent to provide title compound (106 mg, 85%) as a solid. 1H NMR (400 MHz, CHLOROFORM-d) delta ppm 1.32-1.47 (m, 2H) 1.49-1.62 (m, 2H) 1.64-1.73 (m, 4H) 1.73-1.80 (m, 2H) 1.80-1.92 (m, 2H) 1.97-2.07 (m, 2H) 2.10-2.20 (m, 2H) 2.40-2.55 (m, 5H) 2.76 (s, 3H) 3.07-3.14 (m, 2H) 3.15-3.26 (m, 3H) 3.32-3.39 (m, 2H) 3.59-3.67 (m, 2H); HRMS m/z calcd for C19H34N3O3S 384.2315 [M+H]+, found 384.2305., 21043-40-3

21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; US2010/130477; (2010); A1;,
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Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of the product of EXAMPLE SE (300 mg, 1.4 mmol), 2-methoxy-4-(4-methylpiperazin- 1 -yl) aniline (338 mg, 1.53 mmol) andtriethylamine (421 mg, 4.17 mmol) in 1,4-dioxane (30 mL) was stirred at 105 C. under nitrogen for 12 hours. The solvent was removed under vacuum and the residue was washed with sodium bicarbonate solution and ethanol. The crude product was recrystallized from 1 ,4-dioxane to give the title compound.10318] ?H NMR (DMSO-d5) oe ppm 12.66 (s, 1H), 11.35 (s, 1H), 8.31 (d, J=9.0 Hz, 1H), 8.25 (s, 1H), 6.68 (d, J=1.2 Hz, 1H), 6.54 (dd, J=1.2, 9.0 Hz, 1H), 3.89 (s, 3H), 3.21-3.10 (m, 4H), 2.50-2.44 (m, 4H), 2.25 (s, 3H)., 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBVIE INC.; Vasudevan, Anil; Penning, Thomas Dale; Chen, Huanming; Liang, Bo; Wang, Shaohui; Zhao, Zhongqiang; Chai, Dikun; Yang, Leifu; Gao, Yingxiang; Pliushchev, Marina; US2014/171429; (2014); A1;,
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20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 168 N-[2-(4-Cyclopropylpiperazin-1-yl)ethyl]-8-[(2,6-difluorobenzyl)oxy]-2-methylimidazo[1,2-a]-pyridine-3-carboxamide 118 mg of 8-[(2,6-difluorobenzyl)oxy]-2-methyl-N-(2-oxoethyl)imidazo[1,2-a]pyridine-3-carboxamide (Example 194A, 0.16 mmol, 1 equivalent) were suspended in 0.8 ml of dry dichloroethane, 23 mg 1-cyclopropylpiperazine (0.18 mmol, 1.1 equivalents) were added and the mixture was stirred at RT for 3 h. 52 mg of sodium triacetoxyborohydride (0.25 mmol, 1.5 equivalents) were then added, and the mixture was stirred at RT overnight. 1 N aqueous sodium hydroxide solution was then added, and the mixture was extracted three times with dichloromethane. The combined organic phases were washed with water and saturated aqueous sodium chloride solution, dried over sodium sulphate, filtered and concentrated. The residue was dissolved in methanol and purified by preparative HPLC (method: RP18 column, mobile phase: acetonitrile/water gradient with addition of 0.1% TFA). The product fraction was taken up in ethyl acetate and washed twice with saturated aqueous sodium bicarbonate solution. The combined organic phases were dried over sodium sulphate, filtered and concentrated. This gave 33.5 mg (43% of theory) of the title compound. LC-MS (Method 7): Rt=0.60 min MS (ESpos): m/z=470.2 (M+H)+ 1H NMR (400 MHz, DMSO-d6): delta=0.22-0.30 (m, 2H), 0.34-0.43 (m, 2H), 1.53-1.62 (m, 1H), 2.30-2.44 (m, 3H), 3.37-3.46 (m, 2H), 5.30 (s, 2H), 6.93 (t, 1H), 7.01 (d, 1H), 7.23 (t, 2H), 7.55-7.64 (m, 1H), 7.70 (t, 1H), 8.67 (d, 1H), [further signals hidden under solvent peaks].

20327-23-5, The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; VAKALOPOULOS, Alexandros; FOLLMANN, Markus; HARTUNG, Ingo; BUCHGRABER, Philipp; JAUTELAT, Rolf; HAssFELD, Jorma; LINDNER, Niels; WUNDER, Frank; STASCH, Johannes-Peter; REDLICH, Gorden; LI, Volkhart Min-Jian; BECKER, Eva-Maria; KNORR, Andreas; US2014/128372; (2014); A1;,
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13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound of formula 38 (10.0 g, 49.2 mmol) was added to the reaction flask at room temperature,100 mL of N, N-dimethylacetamide,1-acetylpiperazine 16 (8.2 g, 64.0 mmol)N, N-diisopropylethylamine (19.1 g, 147.8 mmol)90 reaction 7 ~ 8h,TLC monitoring reaction is complete,Down to room temperature,The reaction solution was poured into 300 mL of water,Extracted with ethyl acetate (80 mL x 3)Combined organic layer,Washed with saturated brine,Dried over anhydrous sodium sulfate,The compound of formula 41 (9.9 g) was obtained by steaming,As a beige solid (yield 80.6%).

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhengda Tianqing Pharmaceutical Group Co., Ltd.; Zhang Yinsheng; Gao Yong; Ren Jing; Wang Qinglin; Wang Zhao; (67 pag.)CN106905245; (2017); A;,
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Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 99 N- (2-Methoxy-5-methylphenyl)-7- [ (3-methylpiperazin-1-yl) methyl]-1-benzofuran-5- sulfonamide, trifluoroacetate A mixture of 7-formyl-N-(2-methoxy-5-methylphenyl)-1-benzofuran-5-sulfonamide (100 mg, 0,29 mmol; Intermediate 62), 2-methylpiperazine (32 mg, 0,32 mmol) and sodium triacetoxyborohydride (245 mg, 1,16 mmol) in 1, 2-dichloroethane (3 mL) was stirred overnight. Filtration and concentration provided 100 mg of crude material that was purified by preparative HPLC to after concentration give 30 mg (19 %) of the title product. OH NMR (400 MHz, methanol-d4) 8 1.27 (d, 3 H), 2.24 (s, 3 H), 2.33-2. 40 (m, 1 H), 2.46-2. 55 (m, 1 H), 2.91-2. 98 (m, 1 H), 3.05-3. 17 (m, 2 H), 3.32-3. 38 (m, 1 H), 3.39 (s, 3 H), 3.96- 4. 08 (m, 2 H), 6.64 (d, 1 H), 6.87 (dd, 1 H), 6.97 (d, 1 H), 7.28 (d, 1 H), 7.66 (d, 1 H), 7.91 (d, 1 H), 8. 04 (d, 1 H); MS (ESI+) for C22H27N304S m/z 430 (M+H) + ; HPLC 99 %, RT=1. 66 in (System A; 10-97% MeCN over 3 min), 99% RT=1.46 (System B; 10-97% MeCN over 3 min)., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; BIOVITRUM AB; WO2005/58858; (2005); 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.171504-98-6,Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate,as a common compound, the synthetic route is as follows.

To a solution of Ol ,04-di-tert-butyl (92-methyl piperazine-1 ,2,4-tricarboxylate (3.0 g, 8.71 mmol) in THF (60 mL) at -10 C was added dropwise methyl magnesium bromide 3 M (18.5 mL, 55.5 mmol). The reaction was allowed to warm up slowly to room temperature and stirred overnight. The mixture was quenched by dropwise addition of saturated ammonium chloride solution. The reaction mixture was extracted with EtOAc, dried, and concentrated under vacuum then flash chromatographed over silica (loaded in DCM, eluting with cyclohexane to 30% ethyl acetate in cyclohexane), to afford the intermediate di-tert-butyl 2-(l -hydroxy-l -methyl- ethyl)piperazine-l,4-dicarboxylate (2.5 g, 83% yield). This was then dissolved in DCM (15 mL) and the mixture cooled to -20 C under nitrogen and diethylaminosulfur trifluoride (1.15 mL, 8.71 mmol) was added dropwise. The mixture was stirred at -10 C for 1 hour then gradually allowed to warm to -10 C over 1 hour. Saturated sodium bicarbonate was added dropwise then the mixture was partitioned between saturated sodium bicarbonate solution (20 mL) and DCM (20 mL). The organics were dried, concentrated under reduced pressure and the residue purified by flash chromatography on silica gel (eluting with cyclohexane to 20% ethyl acetate in cyclohexane) to afford the title compound (0.97 g, 38% yield) as a colourless oil. LCMS: RT 5.3 min, MI 347, Method (4LCMS1)., 171504-98-6

Big data shows that 171504-98-6 is playing an increasingly important role.

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; CARSWELL, Emma, L.; CHARLES, Mark, David; COCHI, Anne; DUGAN, Benjamin, J.; EKWURU, Chukuemeka, Tennyson; ELUSTONDO, Fred; FOWLER, Katherine, M.; LEROUX, Frederic, Georges, Marie; MONCK, Nathaniel, J.T.; OTT, Gregory, R.; ROFFEY, Jonathan, R.; SIDHU, Gurwinder; TREMAYNE, Neil; (305 pag.)WO2018/55402; (2018); A1;,
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76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

76003-29-7, To a solution of tert-butyl 3-oxopiperazine- 1 -carboxylate (prepared according to procedure reported in W02005504737, 2.0 g, 9.99 mmol), 1-bromo-4- fluorobenzene (1.748 g, 9.99 mmol), N,N-dimethylethylenediamine (0.070 g, 0.799 mmol) and potassium hydrophosphate (KHPO4) (3.13 g, 17.98 mmol) intoluene (10 ml) was added copper (I)iodide (0.101 g, 0.529 mmol) at 25C. The reaction mixture was heated to 80C for 16 h. Progress of the reaction was monitored by TLC. The reaction mixture was cooled to 25C, diluted with ethyl acetate (25 ml) and filtered through a plug of celite and concentrated to give crude product. The crude product was purified over silica gel (100 – 200 mesh)by column chromatography using 30% ethyl acetate in hexane as eluent to obtain the title compound (0.8 g, 27.2 %)?H NMR (400 MHz, CDC13) 6 7.28-7.24 (m, 2H), 7. 14-7.08 (m, 2H), 4.26 (s, 2H), 3.88-3.71 (m, 4H), 1.51(s, 9H). MS: m/z295(M+1).

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; LUPIN LIMITED; JANA, Gourhari; KURHADE, Sanjay, Pralhad; JAGDALE, Arun, Rangnath; KUKREJA, Gagan; SINHA, Neelima; PALLE, Venkata, P.; KAMBOJ, Rajender, Kumar; WO2014/9872; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics