Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-fhioroquinoline-8-carbonitrile (compound lc, 1.4 g, 8.1 mmol) in DMSO (20 mL) was added (3/^,5.S’)-3,5-dimethylpiperazine- 1 -carboxylate (compound Id) (1.7 g, 1.7 mmol) and DIEA (878 mg, 6.8 mmol). The reaction mixture was stirred at 120 C for 3 hrs, then cooled to room temperature, diluted with water (100 mL), and extracted with EA (150 mL) twice. The combined organic layer was washed with brine, dried over Na2S04, filtered and concentrated in vacuo. The residue was purified by flash chromatography (silica gel, 80 g, 10% to 50% EtOAc in PE). The purified intermediate was dissolved in DCM (20 mL) and TFA (5 mL) was added. The reaction mixture was stirred at room temperature for 3 hrs, then concentrated to afford a crude compound 3b (1.6 g, 75% yield). MS: calc?d 266 [(M+H)+], measured 266 [(M+H)+], 129779-30-2

As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; DEY, Fabian; QIU, Zongxing; ZHU, Wei; ZOU, Ge; (55 pag.)WO2020/20800; (2020); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55112-42-0,4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride,as a common compound, the synthetic route is as follows.

To a suspension of tert-butyl 5-(2-(3-aminophenyl)quinazolin-4-ylamino)-lH- indazole-1 -carboxylate (100 mg, 0.22 mmol) and 4-methylpiperazine-l-carbonyl chloride hydrochloride (88 mg, 0.44 mmol,) in CH2Cl2 (2 mL)was added Et3N (92 muL, 0.66 mmol) and catalytic amount of DMAP. The reaction mixture was stirred at RT for 2 h after which 2 equivalents each of 4-methylpiperazine-l-carbonyl chloride hydrochloride and 3 equivalents OfEt3N were added. Continued to stir at ambient temperature for 16 hours. The reaction was concentrated in vacuo and the residue was purified by flash chromatography on silica (8:1 CH2Cl2:Me0H). The product tert-butyl 5-(2-(3-(l- methylpiperazine-4-carboxamido)phenyl)-quinazolin-4-ylamino)- 1 H-indazole- 1 – carboxylate was isolated. (160 mg, 100%)

55112-42-0, 55112-42-0 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride 3016934, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SURFACE LOGIX, INC.; WO2008/54599; (2008); A2;,
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259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[Referential Example 283] 4-(tert-Butoxycarbonyl)-2,2-dimethyl-1-[4-(pyridin-4-yl)benzoyl]piperazine To a solution of 1-(tert-butoxycarbonyl)-3,3-dimethylpiperazine (173 mg) in a mixture of N,N-dimethylformamide (2.5 ml) and triethylamine (1.0 ml) was added (4-nirophenyl) 4-(4-pyridyl)benzoate (330 mg). The resulting mixture was stirred at 60C for 5 days. The reaction mixture was diluted with methylene chloride and then added with a saturated aqueous solution of sodium chloride to form two layers. The organic layer obtained by separation was washed with a saturated aqueous solution of sodium bicarbonate and an aqueous solution of sodium chloride, dried over anhydrous sodium sulfate andconcentrated under reduced pressure. The crudely purified product was purified by chromatography on a silica gel column (methylene chloride: methanol = 50:1), whereby the title compound (199 mg) was obtained as colorless amorphous. 1H-NMR (CDCl3) delta: 1.49(9H,s), 1.61(6H,s), 3.45-3.56(6H,m), 7.50(2H,d,J=5.9Hz), 7.51(2H,d,J=7.8Hz), 7.67(2H,d,J=7.8Hz), 8.69(1H,d,J=5.9Hz). MS (FAB) m/z: 369 (M+H)+.

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1104754; (2001); A1;,
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77279-24-4, tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,77279-24-4

Carbon tetrabromide (1.681 g, 5.07 mmol) was dissolved in dichloromethane (17 ml), cooled with ice.thereTertiary butyl 4- (2-hydroxyMethyl) piperazine-1-carboxylate (1.062 g, 4.61 mmol), triphenylphosphine (1.329 g, 5.07 mmol), and stirred overnight at room temperature was added dichloromethane (11 ml). After the reaction, the solvent was evaporated. The residue was purified by silica gel column chromatography (SNAP ULTRA 25 g, hexane / ethyl acetate) to give the title compound (1.131 g, 83.7percent) as a yellow solid.

As the paragraph descriping shows that 77279-24-4 is playing an increasingly important role.

Reference£º
Patent; Yakult Honsha Co., Ltd.; University of Occupational and Environmental Health; Ono, Masahiro; Kobayashi, Tsuneyuki; Yamazaki, Ryuta; Haibara, Hirotake; Nishiyama, Yukiko; Hokkyo, Atsuko; Nishiyama, Hiroyuki; Kurita, Akinobu; Matsuzaki, Ken; Kono, Kimitoshi; Izumi, Hiroto; (215 pag.)JP2016/124812; (2016); A;,
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162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The 10 mmol of acid (6-8, 11a,b or 14) was dissolved in anhydrous acetonitryle (25 ml). The solution was cooled to -5 C, and triethylamine (1.4 ml, 10 mmol), and then HBTU (3.79 g, 10 mmol) or HATU (3.8 g, 10 mmol), were added. The mixture was stirred for 1 h at -5 C and then 10 mmol of amine 5 was added. The reaction mixture was allowed to stand overnight at room temperature. The residual amount of the activated ether (Bt- or At-ether of starting acid) was destroyed by addition of few drops of N,N-dimethylpropane-1,3-diamine, and the solvent was evaporated in vacuo to dryness. The residue was dissolved in 100 ml of chloroform. The solution was washed with water (40 mL), aqueous solution of 1 M HCl (40 ml) and 5% aqueous solution of NaHCO3 (40 ml). The organic layer was dried over Na2SO4, filtered off, and the solvent was evaporated in vacuo to dryness. The resulting residue was triturated with warm hexane (20 ml), and the precipitate was collected by filtration and dried.

162046-66-4, As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference£º
Article; Krysko, Andrei A.; Samoylenko, Georgiy V.; Polishchuk, Pavel G.; Fonari, Marina S.; Kravtsov, Victor Ch.; Andronati, Sergei A.; Kabanova, Tatyana A.; Lipkowski, Janusz; Khristova, Tetiana M.; Kuz’Min, Victor E.; Kabanov, Vladimir M.; Krysko, Olga L.; Varnek, Alexandre A.; Bioorganic and Medicinal Chemistry; vol. 21; 15; (2013); p. 4646 – 4661;,
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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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Methanesulphonyl chloride (467mu, 5.99 mmol) was added to a stirred solution of (S)-ferf-butyl 2- methylpiperazine-1-carboxylate (1 .0 g, 4.99 mmol) in dichloromethane (20 mL) and pyridine (2 mL). The reaction mixture was stirred at room temperature overnight. The solvent was evaporated. The residue was dissolved in diethyl ether (50 mL) and washed with 1 M hydrochloric acid (25 mL) followed by water (25 mL) and brine (25 mL). The organic phase was dried and evaporated. The product was dissolved in diethyl ether (20 mL) and treated with 4M hydrogen chloride in 1 ,4-dioxane (4 mL) and allowed to stand at room temperature overnight. The solvent was evaporated. The residue was triturated with diethyl ether, was filtered off, washed with diethyl ether and dried to give (S)-3-methyl-1-(methylsulphonyl)piperazine hydrochloride (457 mg, 2.128 mmol, 42.6% yield) as a colourless solid. 1H NMR (400MHz, CDCI3) delta-ppm 3.78-3.60 (m, 2H); 3.08 (dt, J = 12 Hz and J = 4 Hz, 1 H); 2.95 (J = 12 Hz and J = 4 Hz, 1 H); 2.95-2.86 (m, 2H); 2.77 (s, 3H); 2.70 (td, J = 8 Hz and J = 4Hz, 1 H); 2.31 (dd, J = 12 Hz and J = 12 Hz, 1 H); 1.09 (d, J = 8 Hz, 3H)., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE LLC; AMANS, Dominique; BAMBOROUGH, Paul; BIT, Rino, Antonio; BROWN, John, Alexander; CAMPBELL, Matthew; LINDON, Matthew, John; SHIPLEY, Tracy, Jane; THEODOULOU, Natalie, Hope; WELLAWAY, Christopher, Roland; WESTAWAY, Susan, Marie; WO2014/78257; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

To a solution of piperazine-2-carboxylic acid dihydrochloride (25.0 g, 123 mmol), dioxane (180 ml) and 5N aqueous sodium hydroxide solution (90 ml) was added dropwise di-tert-butyl dicarbonate (62.7 g, 288 mmol) under ice-cooling. The mixture was stirred at room temperature for 4 hr, and the solvent was evaporated under reduced pressure. The residue was washed with ether, and acidified to pH=2-3 with concentrated hydrochloric acid under ice-cooling, and the mixture was extracted with ethyl acetate. The extract was dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure to give the object product (31.5 g, 77.6%) as a solid. 1H-NMR (CDCl3) delta; 1.44 (18H, s), 2.87 (1H, br s), 3.08-3.23 (2H, m), 3.76-4.10 (2H, m), 4.51-4.75 (2H, m), 5.07 (1H, br s)., 3022-15-9

The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Matsumoto, Takahiro; Kamo, Izumi; Nomura, Izumi; US2009/318412; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Triethylamine (190mul, 1.37mmol) was added to a solution of commercially available (S)-(+)-2-methylpiperazine (125mg, 1.25mmol) in CH2Cl2 (7mL) at 0C and stirred for 5min. p-Toluenesulfonyl chloride (238mg, 1.25mmol) was then added and the mixture was stirred for 1h at 0C before being allowed to warm to room temperature and stirred for a further 4h. Water was then added and the aqueous layer was separated and extracted with CH2Cl2, before being washed sequentially with 1M HCl (50mL), water (50mL), saturated aqueous NaHCO3 solution (50mL) and saturated aqueous sodium chloride solution (50mL). The organic layer was separated, dried (Na2SO4), filtered and concentrated in vacuo to afford tosyl piperazine, (3S)-3-methyl-1-[(4-methylbenzene)sulfonyl]piperazine (310mg, 97%) as a white solid. The product could be used without further purification; mp 138.5-141C (acetone); [alpha]23D=+38.9[alpha]D23=+38.9 (c 0.93, CHCl3); numax (ATR)/cm-1 3352, 2971, 2922, 2863, 2821, 1605, 1452, 1325, 1165, 1133, 1121, 997, 914, 861, 811, 754s, 655; deltaH (500MHz, DMSO-d6) 7.61-7.59 (2H, m, 2¡ÁArH), 7.47-7.44 (2H, m, 2¡ÁArH), 3.41-3.37 (2H, m, CH2NTs), 2.85 (1H, dt, J 12.1 and 2.8, CH2NTs), 2.68-2.60 (2H, m, 3-H and CHHN(H)), 2.41 (3H, s, ArCH3), 2.06 (1H, td, J 11.3 and 3.1, CHHN(H)), 1.70 (1H, t, J 10.8, CHHN(H)), 0.90 (3H, d, J 6.4, 3-(CH3)); deltaC (126MHz, DMSO-d6) 143.4, 131.9, 129.7, 127.5, 52.3, 49.5, 45.9, 44.3, 20.9, 18.8; m/z (CI+) 255 (MH+, 100%), 99 (M+ -Ts, 10); HRMS (CI+) MH+ calculated for C12H19N2O2S 255.1167, observed 255.1164.

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Article; Armstrong, Alan; Pullin, Robert D. C.; Jenner, Chloe R.; Foo, Klement; White, Andrew J. P.; Scutt, James N.; Tetrahedron Asymmetry; vol. 25; 1; (2014); p. 74 – 86;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of compound 7, 8, or 9 (1 equiv) in 1-butanol was added compounds 12(1.1 equiv) and p-toluenesulfonic acid (1 equiv). The mixture was placed in a pressure flask, and heated to 100C for 15h. The reaction mixture was quenched by saturated Na2CO3 aqueous solution, and then was extracted with DCM and the organic phase was washed with water, dried over anhydrous Na2SO4. The combined organic layer was concentrated under reduced pressure and was further purified by flash column chromatography using dichloromethane/methanol as eluent to afford product H1-H14, Y1-Y14, or L1-L14 as a pale yellow solid., 115619-01-7

As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

Reference£º
Article; Hou, Yunlei; Zhu, Liangyu; Li, Zhiwei; Shen, Qi; Xu, Qiaoling; Li, Wei; Liu, Yajing; Gong, Ping; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 690 – 709;,
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.1403898-64-5,(2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation 46: (2R,5R) -4-(2,4-Di methoxy-benzyl)-5-hydroxymethyl-2-methyl-pi perazi ne1-carboxylic acid tert-butyl ester To an ice-cooled solution of (2R ,5R)-5-hydroxymethyl-2-methyl-piperazine- 1 -carboxylic acid tert-butyl ester (10.0 g, 43.5 mmol) in DOE (70 mL) were added 2,4-dimethoxy-benzaldehyde (11.1 g, 66.6 mmol) and sodium triacetoxyborohydride(11.1 g, 52.2 mmol) in small portions. Thereaction mixture was stirred at room temperature overnight. Saturated aqueous NaHCO3 was added and the product was extracted with DCM. The organic phase was dried and evaporated. Chromatography on silica gel, eluting with petrol – EtOAc 0-50% gave the title compound (16.3 g, 99%). 1297-012-1 MS: [M+H] = 381., 1403898-64-5

The synthetic route of 1403898-64-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; BUCK, Ildiko Maria; DAY, James Edward Harvey; HOWARD, Steven; SAXTY, Gordon; MURRAY, Christopher William; HOPKINS, Anna; WO2014/60767; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics