Month: September 2021

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5747-48-8, A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11- piperazinyldibenzo [b,f] [1,4] thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min at 25- 30C. Sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 mole)] and 2-(2-chloroethoxy)ethanol [32.0 gm (0.257 moles)] were added at room temperature. The reaction mixture was heated to reflux at 110-112C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check the absence of compound of Formula IV) and was cooled to 25C to 30C, and was added 150 cc DM water. The reaction mixture was then stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extract and the organic layer were combined, to which was added 250 cc water and was acidified with formic acid to obtain a pH of 2- 3. The reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH adjusted to 8-10 using sodium carbonate. The resulting reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 125 cc toluene. The organic layers were combined and washed with DM water 300 cc twice. The organic layer was distilled off under vacuum below 70C to afford 2-(2-(4-dibenzo[b,fJ-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy) ethanol. Purity of 2-(2-(4-dibenzo[b,f]-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy) ethanol was 99.0% (area % by HPLC).

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/121415; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-82-4, General procedure: Compound 5 (1.0 eq.) and amine derivative (1.0 eq.) were dissolvedin dioxane (5 mL) and then Pd2(dba)3 (0.2 eq.), BINAP(0.2eq), Cesium carbonate (1.0eq.) were added. The reactionmixture was stirred at 100 C until the reaction was done. Theresultant mixture was concentrated, and the residue was purifiedby silica gel column chromatography to give the correspondingproducts 6a-r.

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference：
Article; Chen, Yang; Cheng, Zhongyu; Huang, Xin; Jiang, Yaoxuan; Qiao, Hui; Xie, Jiahao; Yang, Linlin; Yu, Bin; Zhao, Wen; Zhou, Wenjuan; European Journal of Medicinal Chemistry; vol. 199; (2020);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78818-15-2,78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

-(t-Butyloxycarbonyl)-piperazin-2-one (0.6 g, 3.0 mmol), EXAMPLE 40, is dissolved in THF (80 mL), cooled in an ice bath and treated with tretrabutylammonium iodide (0.23 g, 0.62 mmol) and 60% sodium hydride (0.12 g, 3.0 mmol). The reaction mixture is stir

78818-15-2 Benzyl 3-oxopiperazine-1-carboxylate 736777, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AVENTIS PHARMACEUTICALS INC.; US2004/102450; (2004); A1;,
Piperazine – Wikipedia
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

A solution of methyl 3-bromo-2-phenylquinoxaline-6-carboxylate (150 mg, 0.44 mmol, 1.00 equiv) in DMF (8 rriL), l-(4-(trifluoromethyl)phenyl)piperazine (202 mg, 0.88 mmol, 2.00 equiv), DIEA (170.3 mg, 1.32 mmol, 3.00 equiv) were placed in a 20-mL sealed tube and stirred overnight at 100C in an oil bath. The reaction was then quenched by the addition of water. The resulting solution was extracted with 4×50 rriL of ethyl acetate and the organic layers combined and dried over anhydrous sodium sulfate followed by filtration to remove solids. The resulting mixture was concentrated under vacuum, resulting in 177.4 mg (78%) of methyl 2- phenyl-3-(4-(4-(trifluoromethyl)phenyl)piperazin-l-yl)quinoxaline-6-carboxylate as a yellow solid.LC-MS (ES, m/z): 492 [M+H]+

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BIOENERGENIX; MCCALL, John, M.; MCKEARN, John; ROMERO, Donnal, L.; CLAIR, Michael; WO2011/28947; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 6-(4-fluorobenzyl)-3,3,4-trimethyl-2,3-dihydro-lH-pyrrolo[3,2-b]pyridin-5(4H)-one (190 mg, 0.66 mmol) in DCM (3.00 mL) and was added triethylamine (0.277 mL, 1.99 mmol) and the reaction was stirred at room temperature under an atmosphere of nitrogen. Chloroacetyl chloride (0.058 mL, 0.730 mmol) was added and the reaction was stirred at room temperature for 30 minutes. The reaction was diluted in 25 mL DCM and washed with 10 mL saturated sodium bicarbonate solution, 10 mL water and 10 mL brine. The organic layer was passed through a biotage phase separator and concentrated under vacuum. The residue was dissolved in 3 mL THF and triethylamine (0.28 mL, 1.99 mmol) and (2R,5R)-tert-butyl 5-(hydroxymethyl)-2-methylpiperazine-l- carboxylate (199 mg, 0.86 mmol, obtained as described in WO 2012/143726) was added. The reaction was stirred at 60C for 18h, then was diluted in 25 mL EtOAc and washed with 2 x 10 mL water and 10 mL brine. The organic layer was passed a through biotage phase separator and concentrated under vacuum to afford the title compound (170 mg, 0.31 mmol, 46 % yield). LCMS Method A RT= 0.84 min, ES+ve 557.

1403898-64-5, 1403898-64-5 (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate 71003242, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CASILLAS, Linda N.; HARLING, John David; MIAH, Afjal Hussain; SMITH, Ian Edward David; RACKHAM, Mark David; (204 pag.)WO2017/182418; (2017); A1;,
Piperazine – Wikipedia
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

General procedure: To a stirred solution of oxirane (0.17mmol) in methanol (5 mL) was added the appropriate secondary amines (0.17mmol).Then the reaction mixture was refluxed for 24 h. After completion, the reaction mixture was allowed to room temperature the resulting crude was concentrated under reduced pressure and purified by column chromatography to yield the corresponding beta-amino alcohol derivatives., 30459-17-7

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

Reference：
Article; Vanguru, Sowmya; Jilla, Lavanya; Sajja, Yasodakrishna; Bantu, Rajashaker; Nagarapu, Lingaiah; Nanubolu, Jagadeesh Babu; Bhaskar, Bala; Jain, Nishant; Sivan, Sreekanth; Manga, Vijjulatha; Bioorganic and Medicinal Chemistry Letters; vol. 27; 4; (2017); p. 792 – 796;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,76003-29-7

To a solution of 50.0 mmol of 5 and 60.0 mmol of 7 in 50.0 mL of 1,4-dioxane was added 0.500 mmol of copper (I) iodide followed by the addition of 100 mmol of K3P04 and 5 mmol of trans-cyclohexanediamine, then the resulting mixture was stirred at 100C for 16 h. The reaction mixture was cooled to rt and diluted with 500 mL of H20. The resulting aqueous solution was extracted with CHC13. The organic phase was washed with saturated NaCl, dried over MgS04 and concentrated in vacuo. The crude product was purified by column chromatography to give 43.4 mmol of 8. 4.2 Results [0176] Analytical data for exemplary compounds of structure 8 are provided below. 4.2.a tert-Butvl 4-(6-aminop_vridin-3-vl)-3-oxopiperazine-I -carboxvlate [0177] ‘H NMR (400 MHz, CDC13) No. 7.97-8.00 (m, 1H), 7.35-7.40 (m, 1H), 6.50-6.54 (m, 1H), 4.54 (br s, 2H), 4.24 (s, 2H), 3.65-3.69 (m, 2H), 3.75-3.80 (m, 2H), 1.50 (s, 9H); MS m/z: 293 (M+1).

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference：
Patent; ICAGEN, INC.; ASTELLAS PHARMA INC.; WO2005/99711; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 4-Bromo-2-fluoro-1-nitrobenzene (0.50 g, 2.28 mmol), piperidin-4-ylmethanol, 2-(piperazin-1-yl)ethanol and 3,4,5-trimethoxyphenol (2.28 mmol), K2CO3 (0.32 g, 2.28 mol) were mixed in DMF(10 mL) and heated at 90 C under N2 for 5 h. After cooling, the reaction mixture was filtered toremove solid and the solvent was evaporated. The residue was dissolved in dichloromethane andwashed with water, dried over anhydrous MgSO4 and concentrated in vacuo. The residue solid wasapplied on column of silica gel and then eluted with the mixed solvent of ethyl acetate and hexanes(3:1, v/v) to give the pure product as a white solid., 103-76-4

103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Al-Sanea, Mohammad M.; Khan, Mohammed Safwan Ali; Abdelazem, Ahmed Z.; Lee, So Ha; Mok, Pooi Ling; Gamal, Mohammed; Shaker, Mohamed E.; Afzal, Muhammad; Youssif, Bahaa G. M.; Omar, Nesreen Nabil; Molecules; vol. 23; 2; (2018);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

An oven dried 1000 mL 3-necked flask was equipped with a mechanical stirrer, nitrogen in- and outlet and cooled to room temperature under a nitrogen flow. Amine 3 (38.1 g, 173 mmol) was put in the flask and dissolved in dry N-methylpyrollidin-2-one (NMP) (503 g). The solution was cooled for 20 minutes in an ice-water bath after which solid terephthaloyl dichloride flakes (17.53 g, 86.3 mmol, 0.50 eq) were added to the flask in a single portion while stirring at 500 rpm. The addition funnel was rinsed with NMP (40 g) and the suspension was stirred for 1 h at 0 C. followed and 0.5 h at room temperature. Concentrated aqueous ammonium hydroxide (94 g, 30 w %) was slowly added to the reaction mixture which was subsequently poored into demineralized water (3.5 L). The pH of the solution was adjusted to 10 by addition of more ammonium hydroxide solution (130 g, 30 w %). The fine, white precipitate was allowed to settle for about 0.5 hour after which the clear top layer was decanted. The precipitate was suspended, filtered over a Millipore filter (Durapore GV, 0.22 mum pore size) while applying vacuum and washed with demineralized water (3×250 mL). The crude product was further purified by repetitive (4×) suspension of the product in warm, high-purity MilliQ water (1.0 L, T=65 C.) for about 1 hour, cooling to approximately 36-38 C., filtration over a Millipore filter, washing with MilliQ water (2×250 mL) and drying to the air under suction for 5-15 minutes. The wet product was dried overnight under vacuum at 50 C. to give the desired compound as an off-white, fine powder (46.4 g, 95%).

55121-99-8, As the paragraph descriping shows that 55121-99-8 is playing an increasingly important role.

Reference：
Patent; TEIJIN ARAMID B.V.; VAN DEN HEUVEL, Christiaan J.M.; VELD, Martijn Arnoldus Johannes; QUAIJTAAL, Joannes H.M.; VERHOEF, Rene P.; DE JONG, Jorrit; NIJENHUIS, Wido; (12 pag.)US2018/223077; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl piperazine-1-carboxylate(0.6 g, 3.2 mmol) and triethylamine (4.6 mL, 32 mmol) in anhydrous THF (10 mL)was added trimethylsilyl isocyanate (4.2 mL, 32 mmol) dropwise atrt. The mixture was stirred at rt for 1.5 h and quenched with ice-water (10 mL), and then THF was removed. The aqueous layer was extracted with EtOAc (30 mL ×3) . The combined organic layers were dried over anhydrous Na2SO4and concentrated. The residue was washed with EtOAc (2 mL) by supersonicvibration for 1 min and vacuum filtered to give tert-butyl4-carbamoylpiperazine-1-carboxylate as a white solid (0.3 g, 40) . 1H NMR (400 MHz, CDCl3): delta ppm 3.42-3.49 (m, 4H) , 3.37-3.42 (m, 4H) , 1.49 (s, 9H) and MS-ESI: m/z252.05 [M+Na] + .

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics