Heterocyclic Building Blocks-piperazine

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

To a solution of the cis-2,6-dimethyl-piperazine (2 g, 17.515 mmol, 1 eq.) in DCM (200 mL) at 0C is added dropwise a solution of di-tert-butyl dicarbonate in DCM (20 mL). After 3.5h, reaction mixture is quenched by a saturated Na2C03 solution, the organic layer is separated, and the aqueous layer is extracted with DCM. The combined organic layers are washed with brine, dried over anhydrous Na2S04, filtered and concentrated in vacuo. Purification by flash chromatography on silica gel (eluting with DCM/MeOH 100/0 to 90/10) affords the expected product., 21655-48-1

21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GALAPAGOS NV; LES LABORATOIRES SERVIER; BREBION, Franck, Laurent; ALVEY, Luke, Jonathan; AMANTINI, David; DEPREZ, Pierre, Marc, Marie, Joseph; GOSMINI, Romain, Luc, Marie; JARY, Helene, Marie; PEIXOTO, Christophe; VARIN, Marie, Laurence, Claire; DE CEUNINCK, Frederic, Andre; POP-BOTEZ, Iuliana, Ecaterina; (317 pag.)WO2016/102347; (2016); A1;,
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68104-63-2, 4-(Piperazin-1-yl)benzonitrile is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

68104-63-2, Under a nitrogen atmosphere, a stirred solution of 3.16 grams (0.017 mole) of 4-piperazinylbenzonitrile, 2.0 mL (0.025 mole) of iodoethane (available from Aldritch Chemical Company), and 7.1 mL (0.051 mole) of triethylamine in 50 mL of THF was heated at reflux for about three hours. At the conclusion of this period, the reaction mixture was allowed to cool to ambient temperature and lOOmL of water was added. The resulting solution was extracted with two 50 mL portions of diethyl ether. The combined extracts were washed with 100 mL portion of water, dried with sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure, yielding 3.2 grams of crude product. The crude product was purified by column chromatography on silica gel, yielding 2.9 grams of tilte compound. The NMR spectrum was consistent with the proposed structure.

As the paragraph descriping shows that 68104-63-2 is playing an increasingly important role.

Reference£º
Patent; BAYER CROPSCIENCE AKTIENGESELLSCHAFT; VELTEN, Robert; ARLT, Alexander; HORSTMANN, Sebastian; VERMEER, Arnoldus; HORN, Karin; (94 pag.)WO2018/202681; (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.

General procedure: To a solution of compound 19 (100 mg, 0.33 mmol) in anhydrous DMF (3 mL) was added appropriate amine (0.43 mmol), EDC (82 mg, 0.43 mmol), 1-hydroxybenzotriazole monohydrate (66 mg, 0.43 mmol), and triethylamine (43 mg, 0.43 mmol). The reaction mixture was stirred at rt overnight, and partitioned between methylene chloride and brine. The organic phase was washed with brine, water, and concentrated. The residue was separated by HPLC to provide compounds 20. For compounds 20f, 20g, and 20h whose syntheses involved the use of BOC-protected amine, the coupling product was then treated with TFA (0.5 ml) in CH2Cl2 (2 mL) at rt for 1 h. Removal of the volatiles provided the crude 20 that can be further purified by HPLC to give the title products., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference£º
Article; Zhu, Gui-Dong; Gong, Jianchun; Gandhi, Viraj B.; Liu, Xuesong; Shi, Yan; Johnson, Eric F.; Donawho, Cherrie K.; Ellis, Paul A; Bouska, Jennifer J.; Osterling, Donald J.; Olson, Amanda M.; Park, Chang; Luo, Yan; Shoemaker, Alexander; Giranda, Vincent L.; Penning, Thomas D.; Bioorganic and Medicinal Chemistry; vol. 20; 15; (2012); p. 4635 – 4645;,
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109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 2-METHYLPIPERAZINE (2 equivalents) in DICHLOROMETHANE AT-10 C, was added di-tert-butyl dicarbonate (1 equivalent). The mixture was stirred for 10 minutes AT-10 C and was then quenched with saturated aqueous NAHC03. The two phases were separated, and the organic layer was extracted with methylene chloride. The organic extracts were collected, dried (NA2SO4), and concentrated to give the desired tert-butyl 3-methylpiperazine-carboxylate (LC/MS M/Z 201.0 (MH +), Rt 1.67 minutes). Conversion to tert-butyl 4- [2- (4-AMINO-5-FLUORO-2-OXO (3- hydroquinolyl)) benzimidazol-6-yl]-3-methylpiperazinecarboxylate was performed according to the procedure in Example 8 (LC/MS M/Z 493.3 (MH+), Rt 2.45 minutes). Subsequent removal of the Boc group was preformed by bubbling HCI gas into a MeOH solution until saturated (LC/MS M/Z 393.2 (MH +), Rt 1.95 minutes). The free amine was subsequently reacted with paraformaldehyde (5 equivalents) in MeOH: AcOH (5: 1) and NaCNBH4 (4 equivalents) over molecular sieves at 80 C. After 10 hours, the mixture was cooled, filtered, and concentrated. The residue was dissolved in CH2CI2, washed with saturated NAHC03, and dried with NA2SO4 to give the desired 4- AMINO-3-[6-(2, 4-DIMETHYLPIPERAZINYL) BENZIMIDAZOL-2-YL]-5-FLUOROHYDROQUINOLIN- 2-one (LC/MS M/Z 407.3 (MH +), Rt 2.03 minutes). Further purification was performed via reverse phase prep. HPLC.

109-07-9, 109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHIRON CORPORATION; WO2004/18419; (2004); A2;,
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30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 15 Preparation of (2S)-(-)-1-(4-indolyloxy)-3-(4-(4-trifluoromethylphenyl)piperazin-1-yl)-2-propanol ethanedioate The title compound was prepared in similar fashion from (S)-(+)-4-(oxiranylmethoxy)-1H-indole and 1-(4-trifluoromethylphenyl)piperazine. The resulting free base was dissolved in ethyl acetate, and precipitated with one equivalent of oxalic acid in ethyl acetate in 89% overall yield. FDMS m/e=419 (M+ of free base)., 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Patent; Eli Lilly Company; US5789402; (1998); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

1-[2-(tert-Butyl-diphenyl-silanyloxy)-ethyl]-piperazine To 2-piperazin-1-yl-ethanol (2 g, 15.36 mmol) in CH2Cl2 (70 mL) and pyridine (1.85 mL, 23.04 mmol) was added DMAP (188 mg, 1.53 mmol) and TBDPS chloride (3.37 mL, 18.44 mmol) and the reaction mixture stirred at RT for 18 h. The reaction mixture was concentrated in vacuo and the crude material was purified by silica gel column chromatography, eluting with CH2Cl2 and increasing the polarity to 10% MeOH/CH2Cl2 to obtain 1-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-piperazine as a colourless oil (1.1 g, 21%). AnalpH2_MeOH-4 min(3): Rt 2.48 min; m/z 369 [M+1]+., 103-76-4

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ashworth, Alan; Lord, Christopher James; Elliot, Richard James Rowland; Niculescu-Duvaz, Dan; Porter, Roderick; Boffey, Raymond John; Bayford, Melanie Jayne; Firth-Clark, Stuart; Jarvis, Ashley Nicholas; Perrior, Trevor Robert; Key, Rebekah Elisabeth; US2015/99732; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Tert-butyl (S)-3-(hydroxymethyl)piperazine-1-carboxylate (887 mg, 4.1 mmol) was added to 53 7-bromo-4,6-dichloro-3-nitroquinoline (600 mg, 1.86 mmol), and 56 DIPEA (0.664 ml, 3.73 mmol) in NMP (4.5 ml) in a microwave tube, which was sealed and heated at 80 C. in a microwave reactor for 60 mins. To the reaction mixture was added 63 DCM (150 ml), and the organic layer was washed with water (3¡Á100 ml), brine, dried and evaporated to give a crude residue. The crude product was purified by flash silica chromatography, elution gradient 10 to 30% 57 EtOAc in 58 heptane. Pure fractions were evaporated to dryness to afford 91 tert-butyl (S)-4-(7-bromo-6-chloro-3-nitroquinolin-4-yl)-3-(hydroxymethyl) piperazine-1-carboxylate (365 mg, 39%) as a yellow solid. 1H NMR (500 MHz, DMSO, 27 C.) 1.44 (9H, s), 3.43-3.48 (2H, m), 3.76 (1H, s), 3.85-3.9 (1H, m), 3.96-4.05 (1H, m), 4.07-4.31 (3H, m), 4.58 (1H, t), 8.38 (1H, s), 8.50 (1H, s), 9.05 (1H, s), 11.15 (1H, s). m/z: ES+ [M+H]+ 501, 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); 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.

At room temperature, 20 g of yufloxacin and 400 ml of a 18% methanol solution of hydrogen chloride (i.e., methanolic hydrochloric acid) were added to a 1000 ml Erlenmeyer flask, and the material was rapidly dissolved by stirring at room temperature for 10 minutes. The resulting solution was colorless and transparent, the reaction was continued stirring for 30 minutes, filtered, and the precipitated crystals were collected. The resulting crystals were collected under vacuum at 20C. The resulting crystals were collected in the proportion of 1g: 2ml water was dissolved in water and heated to dissolve, filtered, the filtrate was collected and allowed to cool to room temperature, the filtrate was added 1 volume filtrate of acetone, stirred precipitation, the precipitation of crystals collected in 20 C under vacuum drying, the sample gradually turned white to pale yellow solid, that is the present invention is water-soluble, The obtained compounds were characterized by X-ray powder diffractometry, differential scanning calorimetry, nuclear magnetic resonance, and infrared spectroscopy, respectively, and their characterization spectra were shown in FIG. 1 to FIG. 6 as crystal B. FIG., 112984-60-8

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 124225, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhaoke Pharmaceutical (Hefei) Co., Ltd.; Li Xiaoyi; Dai Xiangrong; Zhou Guanqun; (20 pag.)CN107383069; (2017); A;,
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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.

A mixture of Methyl 1-Boc-piperazine-2-carboxylate (1.837 g, 7.52 mmol), bromobenzene (0.728 ml, 6.84 mmol), Pd2(dba)3 (0.063 g, 0.068 mmol), DavePhos (0.032 g, 0.082 mmol) and Cs2CO3 (3.34 g, 10.25 mmol) in1,4-Dioxane (15 ml, solvent was degassed for 40 min before using) with molecular sieves (4 A) was heated to 85 C and stirred under argon for 24 hrs. After cooling to room temperature, the mixture was filtered through a plug of celite and concentrated to a yellow oil which was purified via flash chromatography (5%EtOAc/Hexanes) to give a yellow viscous liquid Methyl1-Boc-4-phenylpiperazine-2-carboxylate (2 g, 91 % yield)., 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Zhao, Huanyu; Prosser, Anthony R.; Liotta, Dennis C.; Wilson, Lawrence J.; Bioorganic and Medicinal Chemistry Letters; vol. 25; 21; (2015); p. 4950 – 4955;,
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103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,103-76-4

(1) Preparation of 1-tert-butoxycarbonyl-4-(2-hydroxyethyl)piperazine To a solution of 10.00 g of 1-(2-hydroxyethyl)piperazine in 70 mL of dioxane at room temperature was added dropwise a solution of 16.43 g of di-tert-butyl dicarbonate in 30 mL of 1,4-dioxane with stirring. After completion of the reaction, the mixture was concentrated and n-hexane was added to the residue. The solid was collected by filtration and dried to give 14.11 g of the title compound.

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Mitsui Chemicals, Inc.; US5969138; (1999); A;,
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