Month: April 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of 10 (100 mg, 0.33 mmol) and 1-(4-trifluoromethylphenyl)piperazine (85 mg,0.37 mmol) in DMF (0.5 mL) was added solid K2CO3 (82 mg, 0.59 mmol). The resulting suspensionwas stirred at 90 C for 48 h. Water (5 mL) and DCM (5 mL) were added and the phases were separated.The aqueous phase was then extracted with further DCM (2 5 mL). The organics were dried over anh.Na2SO4, filtered and evaporated in vacuo to give a yellowish solid (161 mg). Column chromatography(hexane/EtOAc mixture) gave 15 as a white solid (52 mg, 32% yield). The analytical sample wasobtained by washing with cooled pentane (38 mg), m.p. 157-158 C. IR (ATR) : 667, 711, 721, 744,770, 806, 824, 909, 951, 971, 984, 1039, 1070, 1106, 1157, 1199, 1230, 1330, 1354, 1390, 1429, 1493, 1522,1594, 1615, 2847, 2919 cm1. 1H-NMR (400 MHz, CDCl3) : 0.10-0.18 (complex signal, 2H, 9-H2),0.84-0.98 (complex signal, 2H, 8-H and 10-H), 2.54-2.66 (complex signal, 2H, 2-H and 6-H), 2.75 (m, 1H,1-H or 7-H), 2.90 (m, 1H, 7-H or 1-H), 3.26 (m, 1H, 3-Ha or 5-Ha), 3.41 [t, J = 5.4 Hz, 4H, 2?(6?)-H2],3.48 (m, 1H, 5-Ha or 3-Ha), 3.56-3.82 [complex signal, 6H, 3-Hb, 5-Hb, 3?(5?)-H2], 5.69 (m, 1H, 11-Hor 12-H), 5.85 (m, 1H, 12-H or 11-H), 6.65 (d, J = 8.8 Hz, 1H, 50-H), 6.95 [d, J = 8.6 Hz, 2H, 2??(6??)-H],7.50 [d, J = 8.6 Hz, 2H, 3??(5??)-H], 7.66 (dd, J = 8.8 Hz, J? = 2.2 Hz, 1H, 40-H), 8.31 (d, J = 2.2 Hz, 1H,20-H). 13C-NMR (100.5 MHz, CDCl3) : 3.9 (CH2, C9), 10.2 (broad s, CH, C8 and C10), 35.6 (CH, C1and C7), 42.7 (CH, C2 or C6), 44.5 [CH2, C3?(5?)], 45.1 (CH, C6 or C2), 47.7 [CH2, C2?(6?)], 49.6 (CH2,C3 or C5), 53.6 (CH2, C5 or C3), 105.8 (CH, C50), 114.6 [CH, C2??(6??)], 120.8 (q, J = 32 Hz, C, C4??),122.1 (C, C30), 124.6 (q, J = 269 Hz, C, CF3), 126.4 [q, J = 4 Hz, CH, C3??(5??)], 128.1 (CH, C11 or C12),129.3 (CH, C12 or C11), 137.5 (CH, C40), 147.5 (CH, C20), 153.0 (C, C1??), 159.1 (C, C60), 167.0 (C, CO).HRMS-ESI + m/z [M + H]+ calcd. for [C28H29F3N4O + H]+: 495.2396, found: 495.23692.

30459-17-7, The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Leiva, Rosana; McBride, Andrew; Binnie, Margaret; Webster, Scott P.; Vazquez, Santiago; Molecules; vol. 23; 3; (2018);,
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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.

Preparation of 1-tert-butyl 3-methyl 4-(4′-chloro-2′-fluoro-4-nitrobiphenyl-3-carbonyl)piperazine-1,3-dicarboxylate (6)Starting material 5 (708 mg, 2.9 mmol) in 20 ml of dichloromethane is initially introduced in a 50 ml multinecked flask with dropping funnel, thermometer and N2 inlet lube, and 1.7 ml of DIPEA are added. The solution is cooled to 0 C., and a solution of 900 mg (3 mmol) of starting material 4 in 10 ml of dichloro-methane is added dropwise over the course of 15 min with stirring. The ice bath is then removed, and the mixture is stirred for a further one hour. Water is added to the reaction mixture, the organic phase is separated off, dried over sodium sulfate, and the solvent is removed. The residue is filtered absorptively through a silica-gel column with ethyl acetate, and the filtrate is evaporated to dryness. The desired product 6 is obtained in a yield of 80% (1.5 g, 2.3 mmol) as solid (mass: [M*-(tBu)]=266; RT 3.44 min. HPLC method 1-100-2_Speed).

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; Merck Patent Gesellschaft Mit Beschrankter Haftung; US2012/115852; (2012); A1;,
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163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1 ,1-dimethylethyl (3R)-3-methyl-1-piperazinecarboxylate (301 mg, 1.5 mmol) in anhydrous acetonitrile (1OmL) was added PS-DIEA (925mg) and the solution was stirred gently under an argon atmosphere at room temperature for 15mins. 4-chlorobenzenesulfonyl chloride (371 mg, 1.8 mmol) as a solution in acetonitrile (5ml_) was added and the reaction was stirred for 24hrs. After this time, the reaction was filtered and PS-isocyanate (3g) was added to the solution which was stirred at room temperature over a weekend (approx 64hrs). The reaction was again filtered and PS-trisamine (1.2g) was added to the solution mixture which was stirred for 2hrs at room temperature. Finally the reaction was filtered and reduced in- vacuo to yield the title compound (411 mg, 73%).1H-NMR (CDCI3) 51.02 (3H, d, J= 6.8Hz), 1.43 (9H, s), 2.79 (1 H, br m), 2.97 (1 H, br m), 3.11 (1 H, dt J=12.5, 3.29Hz), 3.60 (1 H, m), 3.80 (1 H, br m), 4.1 1 (2H, br m), 7.48 (2H, m), 7.75 (2H, m)

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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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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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Piperazines – an overview | ScienceDirect Topics

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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Piperazines – an overview | ScienceDirect Topics

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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Piperazines – an overview | ScienceDirect Topics