Category: piperazines

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of sodium hydride (13.4 mg, 0.3 mmol) in tetrahydrofuran (5.0 mL) was added 2-(4-methylpiperazin-1-yl)ethanol (43.9 mg, 0.3 mmol) at 0¡ã C. The reaction mixture was stirred at room temperature for 30 min. A solution of 4,6-dichloropyrimidin-2-amine (50 mg, 0.3 mmol) in dimethylformamide (0.5 mL) was added to the reaction mixture at 0¡ã C. The resulting reaction mixture was stirred at room temperature for 3 h. After completion, the reaction mixture was concentrated under reduced pressure. The residue obtained was washed with diethyl ether to afford compound 1 (20 mg, 24percent) as a brown solid. 1H NMR (400 MHz, DMSO-d6): delta 2.11 (s, 3H), 2.26 (br s, 4H), 2.41 (br s, 4H), 2.58-2.61 (t, J=5.8 Hz, 2H), 4.29-4.32 (t, J=5.9 Hz, 2H), 6.06 (d, J=3.1 Hz, 1H), 6.99 (br s, 2H). MS m/z (M+H): 272.1., 5464-12-0

Big data shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; Celgene Avilomics Research, Inc.; Alexander, Matthew David; Chuaqui, Claudio; Malona, John; McDonald, Joseph John; Ni, Yike; Niu, Deqiang; Petter, Russell C.; Singh, Juswinder; (164 pag.)US2016/75720; (2016); A1;,
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955400-16-5, (S)-tert-Butyl 3-(methoxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,955400-16-5

N,N-diisopropylethylamine (4.6 mL), and ethyl bromoacetate (2.1 mL) were added to a mixture of tert-butyl(3S)-3-(methoxymethyl)piperazine-1-carboxylate (2.0 g) and methylene chloride (45 mL), and the reaction mixture was stirred at room temperature for 23 hours. The reaction mixture was added water so as to separate the organic layer,and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane-ethylacetate) to obtain tert-butyl (3S)-4-(2-ethoxy-2-oxoethyl)-3-(methoxymethyl)piperazine-1-carboxylate (2.3 g) as an oil.

As the paragraph descriping shows that 955400-16-5 is playing an increasingly important role.

Reference£º
Patent; Astellas Pharma Inc.; TAKAHASHI, Taisuke; TANAKA, Hiroaki; AKAIWA, Michinori; NEGORO, Kenji; MIHARA, Hisashi; FUJI, Hideyoshi; TAKAMATSU, Hajime; (133 pag.)EP3196200; (2017); A1;,
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103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

l-Methoxy-2-nitro-5,7,8,9-tetrahydro-benzocyclohepten- 6-one (15.09 g, 64.15 mmol) in methylene chloride (870 ml)treated with 2-Piperazin-l-yl- ethanol (3 eq) followed by acetic acid (10 eq). The mixture was stirred at 50C for 2 hrs and cooled to 0C and sodium triacetoxyborohydride (4 eq) was added, then warmed to RT and stirred. After a few hours starting material was still present. Added 0.4 eq further of sodium triacetoxyborohydride, then again after 6 hours. Stirred overnight. Poured into a solution of sat. aq. Sodium bicarbonate and ice and made basic to pH 10 with IN sodium hydroxide, extracted 2X dichloromethane, dried MgS04, filtered and concentrated. This material was taken up into ethanol and HC1/ ethanol was added. The resulting precipitate was triturated for 2 hours then filtered. The solid was free-based using NaOH followed by sodium bicarbonate and extracted into dichloromethane to give the title compound (19g, 85% yield). 1H-NMR (400 MHz, CDCI3) 7.56 (d, J = 8.2 Hz, 1H), 7.00 (d, J = 8.2 Hz, 1H), 3.82 (s, 3H), 3.63-3.06 (m, 2H), 3.29-3.24 (m, 1H), 3.00-2.86 (m, 3H), 2.72-2.67 (m, 2H), 2.60-2.51 (m, 8H), 2.46-2.37 (m, 2H), 2.12-2.07 (m, 2H), 1.87-1.78 (m,lH), 1.37-1.29 (m, 1H). LC/MS (ESI+) m/z = 350 (M+H)+, 103-76-4

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

Reference£º
Patent; CEPHALON, INC.; COURVOISIER, Veronique; JACOBS, Martin J.; OTT, Gregory R.; WO2013/134353; (2013); A1;,
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70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-81-3, General procedure: These amines were required for the syntheses of 4 and 20 respectively. To a solution of 4-nitrobenzylchloride (1 mmol) in anhydrous THF (3 mL) was added 1-methylpiperazine or piperidine (1 mmol) and triethylamine (1.5 mmol, 0.21 mL). The solution was heated at 70 C overnight. The reaction mixture was then extracted with dichloromethane and water. The organic fractions were combined, dried over anhydrous Na2SO4, and concentrated under reduced pressure. The residue was purified by column chromatography (hexane/EA 1:4) and characterized by 1H NMR (Supplementary Information). It was dissolved in 10 mL ethanol, PtO2 (0.01 g) was added under nitrogen. Hydrogenation was carried out on a Parr hydrogenator at 50 psi for 16 h. The catalyst was then removed by filtration and the filtrate was concentrated in vacuo to give the amine in quantitative yield.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Article; Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2917 – 2929;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

REFERENCE SYNTHETIC EXAMPLE 9 Synthesis of AD23-04 1) Synthesis of AD23-01 5.0 g (17.5 mmol) of AD18-04 was heated with 50 mL of thionyl chloride for 1 hour with reflux, and the reaction solution was concentrated under reduced pressure. The resulting acid chloride was used directly in the subsequent reaction. 3.4 g (15 mmol) of tert-butyl 4-(2-aminoethyl)tetrahydro-1 (2H)-pyrazinecarboxylate in 100 mL of methylene chloride was stirred with 100 mL of water, 2 g of sodium hydrogen carbonate and the acid chloride at room temperature for 1 day. After addition of 100 mL of methylene chloride, the reaction solution was allowed to separate, and the organic layer was dried over anhydrous sodium sulfate and filtered. The filter cake was mixed with 10 g of silica gel, and from the silica gel mixture, 4.24 mg (8.5 mmol, yield 49percent) of AD23-01 was purified by column chromatography (silica gel 125 g, methylene chloride : methanol = 1:0 to 5:1)., 192130-34-0

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nissan Chemical Industries, Ltd.; EP2439204; (2012); A1;,
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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.

115619-01-7, A mixture of propylphosphonic anhydride (50% in DMF, 0.41 ml_, 0.70 mmol, 2 equiv), 5- (2,6-dichloro-3,5-dimethoxy-phenyl)-quinoline-8-carboxylic acid (Step 159.1 ) (132 mg, 0.35 mmol), 4-(4-ethylpiperazin-1-yl)-aniline (Step 1.9) (79 mg, 0.39 mmol, 1.1 equiv), DMAP (3 mg), and Et3N (0.49 ml_, 3.5 mmol, 10 equiv) in DMF (3 ml_), was stirred for 16 h at rt, under an argon atmosphere. The reaction mixture was diluted with EtOAc and H2O. The aqueous layer was separated and extracted with EtOAc. The combined organic phase was washed with brine, dried (Na2SO4), filtered and concentrated. The residue was purified by trituration in EtOAc to afford the title compound as a yellow solid: ES-MS: 564.9 / 566.9 [M+H]+; tR= 4.45 min (System 1 ).

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

Reference£º
Patent; NOVARTIS AG; WO2009/141386; (2009); A1;,
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655225-01-7, tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of tert-butyl 4-(2-bromoethyl)piperazine-l-carboxylate (130 mg, 0.44 mmol) in acetone (20 mL) was added l’-[(5-chloro-lH-indol-2-yl)methyl]spiro[cyclopropane-l,3′- pyrrolo[2,3-c]pyridin]-2′(l ‘H)-one (142 mg, 0.44 mmol) and potassium carbonate (182 mg, 1.32 mmol). The reaction was heated under reflux for 48 hours. The reaction mixture was filtered and the filtrate was concentrated in vacuo. The residue was purified by preparative TLC (10percent methanol in dichloromethane) to afford 130 mg of fert-butyl 4-(2-{5-chloro-2-[(2’- oxospiro [cyclopropane- 1 ,3 ‘-pyrrolo [2, 3 -c]pyridin] – 1 ‘(2’H)-yl)methyl] – 1 H-indol- 1 – yl} ethyl )piperazine-l -carboxylate.

655225-01-7, As the paragraph descriping shows that 655225-01-7 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; FENG, Song; GAO, Lu; GUO, Lei; HUANG, Mengwei; LIANG, Chungen; WANG, Baoxia; WANG, Lisha; WU, Guolong; YUN, Hongying; ZHANG, Weixing; ZHENG, Xiufang; ZHU, Wei; WO2014/184163; (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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

2-chloro-7-(3-nitrophenyl)thieno[3,2-d]pyrimidine (6, 0.5 g, 1.7 mmol) and 2-methoxy-4-(4- methylpiperazin- l -yl)aniline (7, 0.34 g, 1.5 mmol) were taken up in 2,2,2 trifluoroethanol (5 mL) along with p-toluenesulfonic acid (p-TSA) (0.980 g, 5.1 mmol) to form a mixture. The mixture was heated at 150 C for 45 min in a microwave. The production of product 8 in the reaction mixture was monitored using LCMS. The reaction mixture was then basified with 0.5M NaOH (in CH3OH) and concentrated. Water was added to the resultant concentrate and the mixture was extracted in ethyl acetate, dried over Na2S04 and concentrated. The resultant concentrate was purified by column chromatography (Silica gel 10%CH3OH in DCM) to obtain a yellow solid of N-(2-methoxy-4-(4- methylpiperazin- l -yl)phenyl)-7-(3-nitrophenyl)thieno[3,2-d]pyrimidin-2-amine (8, 0.265 g, 32%). ‘HNMR (CDC13): 8.58-8.55 (d, 2H), 8.43-8.35 (dd, 2H), 8.30-8.25 (d, I H), 8.10 (s, I H), 7.70-7.63 (m, 2H), 6.58 (s, I H), 6.58 (s, I H), 3.90 (s, 3H), 3.24-3.18 (m, 4H), 2.72-2.65 (m, 4H), 2.40 (s, 3H), 122833-04-9

As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; GATEKEEPER PHARMACEUTICAL, INC.; GRAY, Nathanael, S.; ZHOU, Wenjun; WO2011/79231; (2011); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of compound 4-6 (1 mmol) in 5 ml of dry DCM and piperazine derivative (1 mmol) was cooled in an ice bath. Then, 1.1 mmol of DCC in 5 ml of dry dichloromethane was added tothe mixture under nitrogen (N2) atmosphere. Reaction mixture was stirred for 0.5 hour in an ice bath, then 10-16 hours at room temperature. Reaction solvent was evaporated to the dryness. Residue was dissolved in hot acetonitrile then cooled in refrigerator to get the DCU precipitated. White crystalline DCU was removed by filtration. Liquid part was evaporated and crystallized from appropriate solvents to give compound 7-34, 13754-38-6

13754-38-6 1-Benzoylpiperazine 762654, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Akgun, Hulya; Yilmaz, Demet Us; Atalay, Rengul Cetin; Gozen, Damla; Letters in drug design and discovery; vol. 13; 1; (2016); p. 64 – 76;,
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192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-N-(2-aminoethyl)1-N-Boc-piperazine (2.06 g, 8.99 mmol) in CH2CI2 was added triethylamine (2.5 ml_, 17.9 mmol) and 2,4- dichlorobenzenesulfonyl chloride (2.65 g, 10.8 mmol). The reaction mixture was stirred at room temperature for 4 days. The reaction was then concentrated in vacuo and purified by column chromatography (10-70percent ethyl acetate:hexane) to produce 3.46 g (88percent) of the title compound as a white solid: LCMS (m/z): 438.0/440.0 I(M/M+2)+H].

192130-34-0, 192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2007/70865; (2007); A2;,
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