Heterocyclic Building Blocks-piperazine

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

After dissolving 1-(6-chloropyrimidin-4-yl)-N-(2, 6-dichloro-3,5-dimethoxyphenyl)- 1 H-benz[d]imidazol-2- amine (20 mg, 0.044 mmol) and 4-(4-ethylpiperazin-1-yl) aniline (13.6 mg, 0.066 mmol) in a mixture of 1,4-dioxane(0.1 mE) and dimethyl sulfoxide (0.1 mE) and cooling to 0 C., trifluoroacetic acid (10.2 pL, 0.133 mmol) was slowly added dropwise. Then, after heating to 120 C., the reaction mixture was stirred for 20 hours. Afier the reaction was terminated, the reaction mixture was cooled to room temperature. Afier extracting several times using ethyl acetate, the obtained organic layer was washed with water and a saturated sodium chloride solution, dried using sodium sulfate and then concentrated. The obtained residue was purified by colunm chromatography (dichloromethane/methanol, 20:1) to obtain a target compound (16 mg, 59% yield) as a yellow solid. ?H NMR (400 MHz, CDC13) oe 9.91 (brs, 1H), 8.62 (s, 1H), 7.49 (d, J=7.6 Hz, 1H), 7.28 H (m, 2H), 7.15 (t, J=7.6 Hz, 2H), 7.02 (t, J=8.0 Hz, 1H), 7.00 (d, J=8.8 Hz, 2H), 6.51 (s, 1H), 3.93 (s, 6H), 3.26 (t, J=4.6 Hz, 4H), 2.64 (t, J=4.4 Hz, 4H), 2.36 (q, J=7.2 Hz, 2H), 1.15 (t, J=7.2 Hz, 3H). ?3C NMR (400 MHz, CDC13) oe 163.49, 158.07, 156.36, 154.72, 150.63, 149.39, 142.67,135.44,131.39,129.12,124.81,123.28,120.86,117.78, 116.76, 112.85,110.17,95.25,92.88,56.47,52.64,52.30,49.03, 11.85. MSmIz: 620 [M+1].

115619-01-7, 115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY; SIM, Tae Bo; YOON, Ho Jong; YOON, Ji Hye; HUR, Woo Young; ROH, Eun Joo; KWAK, Yeon Ui; (19 pag.)US2016/145240; (2016); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

A solution of di-tert-butyldicarbonate (63 g, 290 mmol) in MeOH (100 mL) was added portionwise to a solution of piperazine-2-carboxyilic acid dihydrochloride (25.0 g, 123 mmol) and triethylamine (48 mL, 340 mmol) in MeOH (150 mL) over 30 minutes. Upon complete addition, the reaction mixture was heated to 50 0C for 2 h. Upon cooling to rt, the reaction mixture was concentrated under reduced pressure. The material was dissolved in water (300 mL) and the solution was brought to pH 2 with 1 M aqueous HCl. This was extracted with EtOAc (4 x 200 mL), and the combined extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure until -100 mL EtOAc remained. The solution was diluted with hexanes (150 mL) and cooled to 0 0C. The resulting solid was collected by filtration, washed with hexanes (2 x) and air- dried. This gave 38.9 g (96%) of the title compound as a white solid. Analytical data: 1H NMR (400 MHz, DMSO-J6) delta 13.02-12.80 (br, IH), 4.50-4.24 (m, 2H)5 3.94-3.72 (br, IH), 3.66 (d, J= 12.8 Hz, IH), 3.22-2.92 (m, 2H), 2.90-2.68 (brs IH), 1.42-1.34, (m, 18H)., 3022-15-9

3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,630125-91-6

To a solution of 2-chloro-4 6-dimethylpyrimidin-5-amine (50 mg 0.317 mmol) in THF (10 mL) was added triphosgene (33.0 mg 0.111 mmol) . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo to give 2-chloro-5-isocyanato-4 6-dimethylpyrimidine (50 mg 0.257 mmol 81yield) . To a solution of 4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) aniline (94 mg 0.327 mmol) and Et3N (0.114 mL 0.817 mmol) in THF (10 mL) was added a solution of 2-chloro-5-isocyanato-4 6-dimethylpyrimidine (50 mg 0.272 mmol) in THF (10 mL) . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo. The residue was dissolved in DCM (60 mL) and washed with H2O (20 mL) and brine (20 mL) . The organic layer was dried over Na2SO4 filtered and concentrated. The residue was purified by preparative HPLC (DCM/MeOH 10/1) to yield a white solid of 1- (2-chloro-4 6-dimethylpyrimidin-5-yl) -3- (4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) phenyl) urea (80 mg 0.167 mmol 61.2yield) 1HNMR(400 MHz CD3OD) delta 7.88 (s 1H) 7.39 (d J 8.0 Hz 1H) 6.99 (d J 2.8 Hz 1H) 3.75 (s 2H) 3.04 (m 8H) 2.49 (m 8H) 1.37 (m 3H) ES-LCMS m/z 471.0 (M+H)

630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R & D COMPANY LIMITED; CHEUNG, Mui; DEMARTINO, Michael P.; EIDAM, Hilary Schenck; GUAN, Huiping Amy; QIN, Donghui; WU, Chengde; GONG, Zhen; YANG, Haiying; YU, Haiyu; ZHANG, Zhiliu; (391 pag.)WO2016/37578; (2016); 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.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

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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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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
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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;,
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.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;,
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.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
Piperazines – an overview | ScienceDirect Topics