Heterocyclic Building Blocks-piperazine

5271-27-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

(0667) A mixture of 4-iodobenzonitrile (300 mg, 1.31 mmol), 1-methyl-3-phenylpiperazine (346 mg, 1.96 mmol), cesium carbonate (1.28 g, 3.93 mmol) and chloro(2-dicyclohexylphosphino- 2′,6′-dimethoxy-1,1′-biphenyl)[2-(2-aminoethylphenyl)]palladium(II) dichloromethane adduct (176 mg, 0.262 mmol) in tert-amyl alcohol (5 mL) was stirred at 100 ¡ãC for 16 h under N2. After cooling to ambient temperature, the mixture was concentrated under reduced pressure to give a residue, which was diluted with H2O (10 mL). The water layer was extracted with EtOAc (20 mL x 2). The collected organic layers were washed with brine (10 mL) and dried over anhydrous Na2SO4. The mixture was filtered and the filtrate was concentrated under reduced pressure. The residue was purified by flash silica gel chromatography (ISCO?; 4 g SepaFlash? Silica Flash Column, Eluent of 065percent EA/PE gradient (at) 40 mL/min) to give 4-(4-methyl-2- phenylpiperazin-1-yl)benzonitrile as an oil. ESI-MS m/z [M+H]+: 277.9.

5271-27-2 1-Methyl-3-phenylpiperazine 2760009, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; WALJI, Abbas; BERGER, Richard; STUMP, Craig, A.; SCHLEGEL, Kelly Ann, S.; MULHEARN, James, J.; GRESHOCK, Thomas, J.; WANG, Deping; FRALEY, Mark, E.; JONES, Kristen, G.; (273 pag.)WO2017/222951; (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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

129799-08-2, To 1-(1,1-dimethylethyl) 3-methyl piperazine-1,3-dicarboxylate (1.00g, 4.09 mmol) in dry toluene (15 mL) was added 3-bromo-chlorobenzene (653 mg, 3.41 mmol), Pd2(dba)3 (93.0 mg, 0.102 mmol), BINAP (191 mg, 0.307 mmol), and cesium carbonate (1.11 g, 4.77 mmol). The reaction mixture was stirred at 100 C for 42 h, then cooled to room temperature and filtered through celite. The filter cake was washed with ethanol, and the filtrate was concentrated. Column chromatography on silica (hexanes:ethyl acetate 3: 1) provided 1-(1,1-dimethylethyl) 3-methyl 4-(3-chlorophenyl)piperazine-1,3- dicarboxylate (310 mg, 21% yield) as a colorless oil. ?H NMR (400 MHz, CDC13) 8 7.20- 7.13 (t, 1H), 6.84-6.79 (m, 2H), 6.73-6.78 (d, 1H), 4.63-4.50 (br s, 1H), 4.41-4.32 (br s, 1H), 4.24-4.02 (br s, 2H), 3.71-3.65 (s, 3H), 3.55-3.46 (br s, 1H), 3.42-3.26 (br s, 1H), 3.16-2.97 (br s, 1H), 1.49-1.42 (s, 9H); MS (ESI) for C17H23ClN204: 355 (MH(at)).

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EXELIXIS, INC.; WO2005/117909; (2005); A2;,
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4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 2 (General procedure A); 2-(4-lsopropylpiperazin-1-yl)-6-methoxybenzothiazole, hydrochloride; A mixture of 2-chloro-6-methoxybenzothiazole (0.20 g, 1.0 mmol) and 1-isopropylpiperazine (0.26 g, 2.0 mmol) was stirred at 120 0C for 2 h. The reaction mixture was allowed to cool and worked up by extraction with ethyl acetate. The organic extract was washed with a Na- HCO3 solution and water (3 x). The organic phase was extracted with 0.25 M hydrochloric acid (10 ml_). The acidic aqueous extract was concentrated and re-evaporated with ethanol. The residue was crystallized from a mixture of ethanol and ethyl acetate to give 260 mg (80 percent) of 2-(4-isopropylpiperazin-1-yl)-6-methoxybenzothiazole, hydrochloride. 1H-NMR (400MHz, DMSO-d6) delta 11.7 (brs, 1 H), 7.52 (d, 1 H), 7.49 (d, 1 H), 6.97 (dd, 1 H), 4.23-4.15 (m, 2H), 3.88-3.75 (m, 5H), 3.55-3.47 (m, 3H), 3.28-3.15 (m, 2H), 1.32 (d, 6H).

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVO NORDISK A/S; WO2007/110364; (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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

129799-15-1, Step 3 4-(4-Chloro-phenyl)-piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester 4-Chloro phenyl boronic acid (2.0 equiv, 3.68 mmol) and piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (1.0 equiv, 1.84 mmol) were dissolved in dichloromethane followed by the addition of copper acetate (1.0 equiv), 4 A molecular sieves and pyridine (2.0 equiv). The reaction mixture was stirred at room temperature for 72 h. The reaction mixture was concentrated in vacuo, dissolved in ethyl acetate, filtered through celite and concentrated. The crude product was purified using gradient elution from hexane/ethyl acetate (5%) to hexane/ethyl acetate (20%). ESI-MS m/z: 354 (M+1), UV retention time: 2.88 min.

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; Millennium Pharmaceuticals, Inc.; Kyowa Hakko Kirin Co., Ltd.; LULY, Jay R.; NAKASATO, Yoshisuke; OHSHIMA, Etsuo; HARRIMAN, Geraldine C.B.; CARSON, Kenneth G.; GHOSH, Shomir; ELDER, Amy M.; MATTIA, Karen M.; (190 pag.)US2016/31908; (2016); 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.

To a stirred solution of 1 ,1-dimethylethyl (2S)-2-methyl-1-piperazinecarboxylate (0.2g, 1 mmol) in DCM (5mL) was added triethylamine (0.35ml_) and 4- chlorobenzenesulphonyl chloride (0.42g, 2mmol). The mixture was stirred overnight at ambient temperature under argon. To the reaction was added 4- chlorobenzenesulfonyl chloride (0.2g, 0.95mmol) and the reaction stirred for a further 2 hours. The solvent was evaporated and the crude taken up in DCM (25ml_). To the solution was added PS-trisamine (3g) and the mixture stirred at room temperature for 2hours. To the mixture was then added PS-isocyanate (1.5g) and the mixture stirred for a further 30minut.es. The reaction was filtered and the solvent removed by evaporation. The crude product was taken up in DCM, washed twice with water (2 x 5OmL), dried (MgSO4) and filtered. The solvent was evaporated to yield crude product which was dried at 4O0C under vacuum for 1 hour to yield the title compound as an off-white solid (0.284g, 76%).1H NMR (CDCI3) 51.27 (3H, d, J=I), 1.42 (9H, s), 2.24 (1 H, m), 2.42 (1 H, dd, J=11 ,4), 3.16 (1 H, m), 3.49 (1 H, dt, J=11 , 2), 3.67 (1 H, m), 3.93 (1 H, m), 4.34 (1 H, br s), 7.52 (2H, m), 7.67 (2H, m)., 169447-70-5

Big data shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; BESWICK, Paul, John; CAMPBELL, Alister; CRIDLAND, Andrew; GLEAVE, Robert, James; PAGE, Lee, William; WO2010/102663; (2010); A1;,
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475272-54-9, (S)-1-Boc-3-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 4 (2.2 mmol) and tert-butyl (35)-3-isopropylpiperazine-l-carboxylate (0.5 g, 2.2 mmol) in DMF (10 mL) and DIPEA (0.34 g, 2.63 mmol) were heated at 110C for 6 h. The reaction mixture was allowed to cool, then stirred overnight at room temperature. The reaction mixture was concentrated in vacuo, then partitioned between EtOAc and water. The organic layers were dried over sodium sulfate and concentrated in vacuo, then the crude material was purified by column chromatography (silica gel: 100- 200 mesh, isohexanes:EtOAc, gradient 50% to 100% EtOAc) to give an off- white foam. This was taken up in 4N HC1 in 1 ,4-dioxane (5 mL) and methanol (1 mL), and stirred for 1 h. The reaction mixture was concentrated in vacuo and triturated with diethyl ether to give the title compound (0.08 g, 12%).

475272-54-9, The synthetic route of 475272-54-9 has been constantly updated, and we look forward to future research findings.

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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21091-98-5, (4-Methylpiperazin-1-yl)(4-nitrophenyl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 3a (1.20 g, 4.81mmol) and Pd/C (0.102 g, 0.096 mmol) in MeOH (25 mL) was stirred under H2 overnight.The suspension was filtered through a pad of Celite and the pad was washed with EtOH(10 mL¡Á3). The combined filtrates were concentrated and the crude was purified bycolumn chromatography on silica gel (DCM: MeOH =20:1) to give the title compound3b (1.0 g, 95 % yield). LCMS: 220.1 [M+H]+., 21091-98-5

The synthetic route of 21091-98-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Ding, Xiao; Stasi, Luigi Piero; Ho, Ming-Hsun; Zhao, Baowei; Wang, Hailong; Long, Kai; Xu, Qiongfeng; Sang, Yingxia; Sun, Changhui; Hu, Huan; Yu, Haihua; Wan, Zehong; Wang, Lizhen; Edge, Colin; Liu, Qian; Li, Yi; Dong, Kelly; Guan, Xiaoming; Tattersall, F. David; Reith, Alastair D.; Ren, Feng; Bioorganic and Medicinal Chemistry Letters; vol. 28; 9; (2018); p. 1615 – 1620;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

15g of compound 6,150 ml of dichloromethane was added to the reaction flask.Cool down to 0 ¡ã C,Dissolve in 100 mL of dichloromethane16.5g of Boc-anhydride was added to the reaction flask and stirred for 1 hour.Point plate monitoring, after the reaction, filtering,The filtrate was spun dry, added with 100 mL of water, stirred, filtered, and the filtrate was added with saturated 10 g of potassium carbonate and stirred with methyl tert-butyl ether ether.Extract, dry over sodium sulfate, spin dry,Adding petroleum ether, stirring and crystallizing under cooling to obtain 25 g of compound 7;, 75336-86-6

75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Tonghua Normal College; Geng Xiaoyu; Xue Mingxing; Zang Hao; Liu Xuekun; Sun Renshuang; Xue Changsong; Zhang Haifeng; (13 pag.)CN109438423; (2019); A;,
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21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A:6-Bromo-2-(4-cyclopentylpiperazin-1-yl)benzothiazole; To a solution of 6-bromo-2-chlorobenzothiazole (3 g, 12.1 mmol) in ethanol (50 mL) was added triethylamine (5.04 mL, 36.3 mmol) and 1-cyclopentylpiperazine (1.86 g, 12.1 mmol). The reaction mixture was heated at reflux for 16 h and then concentrated under reduced pressure. The residue was extracted with ethyl acetate and the combined organic extracts were washed with brine, dried (Na2SO4) and concentrated under reduced pressure to afford 4.3 g (99 %) of 6-bromo-2-(4-cyclopentylpiperazin-1-yl)benzothiazole., 21043-40-3

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

Reference£º
Patent; NOVO NORDISK A/S; WO2007/110364; (2007); A1;,
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Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 123. N-(2-(piperazin-l-yl)ethyl)-6,7-dihydro-5H-cyclopenta[4,5]thieno[:d]pyrimidin-4-amine. (1-147)Synthesis of tert-butyl 4-(2-((6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4- yl)amino)ethyl)piperazine-l-carboxylate.A mixture of compound D (189 mg, 0.9 mmol, 1 eq) and compound 1 (200 mg, 0.9mmol, 1 eq) in 5 mL of isopropanol was added K2CO3 (248 mg, 1.8 mmol, 2 eq). The reaction mixture was heated at reflux overnight. The mixture was poured into 30 mL of water and extracted with DCM (20 mLx3). The combined organic layer was washed with brine, dried over anhydrous Na2SC>4 and concentrated. The residue was purified by column chromatography on silica gel(DCM/MeOH = 20/1) to give tert-butyl 4-(2-((6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3- d]pyrimidin-4-yl)amino)ethyl)piperazine-l-carboxylate as white solid (100 mg, 25percent).Synthesis of Compound 1-147.A mixture of Compound 2 (100 mg, 0.25 mmol, 1 eq) in MeOH/HCl (2N, 3ml) was stirred at rt for 12h. The solvent was removed under vacuum and the residue was purified by Prep-HPLC to give N-(2-(piperazin- 1 -yl)ethyl)-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-arnine as a yellow solid (62 mg, 82percent). NMR (400 MHz, D20) delta 2.25-2.29 (m, 2H), 2.72-2.79 (m, 4H), 3.26-3.34 (m, 1 1 H), 3.80 (t, J = 6.0 Hz, 1H), 8.24 (s, 1H). LC/MS calcd for C,5H2iN5S: 303.15. Found: 304.1., 192130-34-0

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NIMBUS IRIS, INC.; ROMERO, Donna L.; WESSEL, Matthew David; ROBINSON, Shaughnessy; GREENWOOD, Jeremy Robert; WATTS, Karl Shawn; FRYE, Leah Lynn; HARRIMAN, Geraldine C.; CORIN, Alan Franklin; MASSE, Craig; WO2012/97013; (2012); A1;,
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