Month: February 2021

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

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;,
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

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

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

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;,
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.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

[00236] To a 15 mL pressure tube was added 8-ethyl-4-methyl-2-(methylsulfonyl)pyrido[2,3-d]pyrimidin-7(8H)-one (70.0 mg, 0.202 mmol), 1 mL dimethylsulfoxide (dmso), and 4-morpholinoaniline (Aldrich, 72.9 mg, 0.409 mmol, 2 eq,) was added. The reaction mixture was heated to 1000C for 16 h. The reaction was diluted with EtOAc, washed with sat. aqueous NaHCO3, dried over Na2SO4, filtered, and concentrated. The crude material was purified by preparative hplc using 20 – 90% ACN in H2O with 0.05% THF. The desired product containing fractions were combined, diluted with EtOAc, and washed with saturated NaHCO3, H2O, and brine. The organic layer was dried over Na2SO4 and solvent was removed on a rotary evaporator to a colorless film. The film was dissolved in 2 mL ACN and 2 mL H2O, frozen and lyophilized overnight, yielding 8.7 mg (10% yield) of 6-Bromo-8-ethyl-4-methyl-2-[(4-morpholin-4-ylphenyl)amino]pyrido[2,3- EPO phiyrimidin-7(8H)-one as a colorless powder: 1H NMR (400 MHz, CDCl3): delta 8.13 (s, IH),7.56 (d, J= 8.8 Hz5 2H), 7.22 (s, IH)5 6.94 (d, J= 9.2 Hz5 2H), 4.50 (q, J= 7.2 Hz5 2H), 3.88(t, J= 4.4 Hz, 4H)5 3.15 (t, J= 5.2 Hz5 4H)5 1.58 (s, 3H)5 1.35 (t, J= 6.8 Hz, 3H)5 MS (EI) forC20H22BrN5O2: 444.3 (MH+)

115619-01-7, The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EXELIXIS, INC.; WO2007/44698; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of ethyl 2-(4-acetylpiperazin-l-yl)-2-phenylacetate (154). Ethyl 2-bromo-2-phenylacetate (0.22 ml, 1.23 mmol) was dissolved in acetonitrile (4 ml) and DIPEA (0.28 ml, 1.60 mmol) and 1- (piperazin- l-yl)ethanone (0.21 g, 1.60 mmol) were sequentially added. The reaction was stirred at room temperature overnight. The solvent was evaporated and the residue was purified by flash chromatography (DCM/Acetone = 9/1) to obtain ethyl 2-(4-acetylpiperazin-l-yl)-2- phenylacetate (341 mg, 95 % yield) as a pale yellow oil. 1H NMR (300 MHz, DMSO-d6) ppm 6.80 – 7.63 (m, 5 H), 4.18 (s, 1 H), 4.00 – 4.16 (m, 2 H), 3.33 – 3.49 (m, 4 H), 2.26 – 2.45 (m, 4 H), 1.95 (s, 3 H), 1.13 (t, 3 H)., 13889-98-0

13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHIESI FARMACEUTICI S.P.A.; AMARI, Gabriele; PESENTI, Cristina; BOSSOLO, Stefano; WO2013/98145; (2013); 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.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

A mixture of compound 3 (306 mg, 1 mmol),tert-butyl 2-amino-4-(thran-3-yl)-phenylcarbamate (246 mg, 0.9 mmol) and 1 -(3-dimethylaminopropyl)-3-ethylcar- bodiimide hydrochloride (573 mg, 3 mmol) in pyridine (15 mE) was stirred at room temperature for overnight. The mixture was poured into water (100 mE), filtered to obtain compound 4 (420 mg, 83%) as a yellow solid.

162046-66-4, The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Regenacy Pharmaceuticals, LLC; van Duzer, John H.; Mazitschek, Ralph; (123 pag.)US2018/141923; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics