Month: December 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.

5308-25-8, General procedure: To a solution of N-methylpiperazine (0.9819mmol) in dry DMF (4mL), triethylamine (0.27mL, 1.9638mmol) and potassium iodide (16.29mg, 0.0981mmol) were added at rt under N2 atmosphere. To the resultant mixture, compound 2 (0.4g, 0.9819mmol) was added and heated at 125C. After the reaction was complete, as indicated by TLC, DMF was evaporated in vacuo. The obtained residue was diluted with 20mL of water. The compound was extracted with CH2Cl2 (3¡Á5mL). The organic layers were collected, washed with saturated brine solution, dried over anhydrous MgSO4 and concentrated in vacuo. The resultant crude was purified by column chromatography [CH2Cl2/MeOH (1-10%)] to get the title compound.

5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Suresh, Narva; Nagesh, Hunsur Nagendra; Chandra Sekhar, Kondapalli Venkata Gowri; Kumar, Anil; Shirazi, Amir N.; Parang, Keykavous; Bioorganic and Medicinal Chemistry Letters; vol. 23; 23; (2013); p. 6292 – 6295;,
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.

The 5 – ((2,4-dioxo -3,4-dihydrochinazolines having antiviral properties -1 (2H)-yl) methyl) – 2-fluoro-benzoic acid (100 mg, 0 . 16mmol), EDCI (124 mg, 0 . 64mmol), HOBt (88 mg, 0 . 64mmol) and TEA (66 mg, 0 . 64mmol) into the reaction bottle in, addition of about 2 ml of the dissolution of water-free DMF, r.t. The lower stirring 60 min, then dropwise (3S, 5R) – 3,5-dimethyl piperazine-1-carboxylic acid T-butyl ester (104 mg, 0 . 48mmol) in the DMF solution to the reaction solution, r.t. The lower stirring overnight, the reaction solution is poured into 100 ml water, using 100mLDCM extraction, an organic layer for sequentially 1MHCl (100 ml), saturated NaCl (100 ml) and water (100 ml) washing, vacuum concentration, silica gel column chromatography, to obtain 59 mg solid, yield 36.3%.

129779-30-2, 129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Institute Of Materia Medica Chinese Academy Of Medical Sciences; Xu, Bailing; Chen, Xiaoguang; Yao, Haiping; Ji, Ming; Jin, Jing; Zhou, Jie; Wang, Ke; Zhao, Dalong; (55 pag.)CN105461697; (2016); A;,
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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The 3 – ((2,4-dioxo -3,4-dihydrochinazolines having antiviral properties -1 (2H)-yl) methyl) benzoic acid (150 mg, 0 . 51mmol), HATU (388 mg, 1 . 02mmol), HOBt (138 mg, 1 . 02mmol) and TEA (104 mg, 1 . 02mmol) into the reaction bottle in, addition of about 5 ml of the dissolution of water-free DMF, r.t. The lower stirring 15 min, then dropwise (S)-N-Boc-2-ethyl piperazine (153 mg, 0 . 76mmol) in the DMF solution to the reaction solution, r.t. The lower stirring sleepovers, reducing pressure and evaporating solvent, addition of about 20mLDCM, saturated NaHCO3washing (25 ml ¡Á 2), dried anhydrous sodium sulfate, silica gel column chromatography to obtain 150 mg of solid, yield 65.8percent.

325145-35-5, As the paragraph descriping shows that 325145-35-5 is playing an increasingly important role.

Reference£º
Patent; Institute Of Materia Medica Chinese Academy Of Medical Sciences; Xu, Bailing; Chen, Xiaoguang; Yao, Haiping; Ji, Ming; Jin, Jing; Zhou, Jie; Wang, Ke; Zhao, Dalong; (55 pag.)CN105461697; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-70-5, tert-Butyl 4-benzylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,57260-70-5

General procedure: These compounds were prepared by means of the previously reported methods [44]. To a solution of tert-butyl piperazine-1-carboxylate (0.559g, 3.0mmol) and triethylamine (0.63mL, 3.3mmol) in CH2Cl2 (15mL) appropriate substituted benzyl chlorides or benzyl bromides 2a-g (3.6mmol) were added. After stirring the mixture at room temperature overnight, it was then diluted with H2O and the organics extracted with CH2Cl2 (2¡Á20mL), dried over MgSO4, and concentrated under reduced pressure. Purification of the crude material by flash column chromatography (SiO2, PE/AcOEt, 60/40) gave the corresponding intermediates. These intermediates (2.49mmol) were then treated with TFA (5.75mL, 76.8mmol) in toluene (15mL) and stirred for 80min at room temperature. After the removal of the solvent under reduced pressure, the residue was diluted with aqueous NaOH (1N) and the organics extracted with CH2Cl2 (2¡Á20mL), dried over MgSO4, and concentrated under reduced pressure to give the desired compounds 4a-g (72-89%).

57260-70-5 tert-Butyl 4-benzylpiperazine-1-carboxylate 584330, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Sadeghzadeh, Masoud; Sheibani, Shahab; Ghandi, Mehdi; Daha, Fariba Johari; Amanlou, Massoud; Arjmand, Mohammad; Hasani Bozcheloie, Abolfazl; European Journal of Medicinal Chemistry; vol. 64; (2013); p. 488 – 497;,
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Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Take 1.86g of 4-hydroxybenzaldehyde and 3.72g of intermediate A22 in a 50ml round bottom flask was added 15mlN, N- dimethylformamide, another additional 4.2g of potassium carbonate, the reaction solution in a 85 C oil bath Stirred for 3 hours, cooled to room temperature. The reaction mixture was diluted with ethyl acetate and washed with water four times. The ethyl acetate layer was separated and dried over anhydrous sodium sulfate and evaporated to dryness under reduced pressure. The residue was chromatographed on silica gel with petroleum ether-ethyl acetate = 4: 1, petroleum ether-ethyl acetate = 1: 1, then with petroleum ether-ethyl acetate = 1: 1 and 1% by volume of triethylamine Column chromatographyTo give 3.35 g of intermediate A23 in a yield of 66%, 208167-83-3

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Tsinghua University; Rao Yu; Wu Wei; Lan Tianlong; Hu Jiantao; Fan Zhongyun; Huang Binlu; (31 pag.)CN107286098; (2017); A;,
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.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

655225-01-7, The compound obtained in Example 102-1 (45 mg, 0.27 mmol) in DMF (1 ml) solution of, tertiary butyl 4- (2-bromoethyl) piperazine-1-carboxylate (88 mg, 0.30 mmol) , it was added cesium carbonate (107 mg, 0.33 mmol). And stirred overnight at 70 , was solidified after the completion of the reaction was concentrated under reduced pressure to dryness. The residue was purified by silica gel column chromatography (chloroform / methanol) to give the title compound (95 mg, 92percent).

As the paragraph descriping shows that 655225-01-7 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
Piperazines – an overview | ScienceDirect Topics

31321-68-3, (R)-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (R)-piperazine-2-carboxylic acid (70 g, 344.71 mmol, 1.0 equiv, 2HCl) in dioxane (1120 mL) and H2O (700 mL) was added 50% aq. NaOH until the solution was pH=11. Benzyl chloroformate (156.82 mL, 1.10 mol, 3.2 equiv) was added and the reaction mixture was stirred at room temperature for 12 h. To the solution was then added H2O (1200 mL) and the aqueous layer was washed with MTBE (3 x 800 mL). The aqueous layer was adjusted to pH=2 with concentrated HCl (12N) and extracted with EtOAc (2 x 1000 mL). The combined organic extracts were dried, filtered and the filtrate was (1187) concentrated under reduced pressure to afford the desired product (137 g, 99.8% yield) as a yellow solid. LCMS (ESI) m/z: [M + H] calcd for C21H22N2O6: 399.16; found 399.2.

31321-68-3, The synthetic route of 31321-68-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; REVOLUTION MEDICINES, INC.; SEMKO, Christopher Michael; WANG, Gang; BURNETT, G. Leslie; AGGEN, James Bradley; KISS, Gert; CREGG, James Joseph; GLIEDT, Micah James Evans; PITZEN, Jennifer; LEE, Julie Chu-Li; WON, Walter; THOTTUMKARA, Arun P.; GILL, Adrian Liam; (356 pag.)WO2019/212991; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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