Month: April 2021

148546-99-0, 3-(4-Methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of intermediate 6 (prepared according to A2. c-1) (0.0005 mol) and 3-(4-methyl-1-piperazinyl)-benzenamine (0.0005 mol) in 2-methoxyethanol (4 ml) was stirred for 1 hour at 100C and the solvent was evaporated. The residue was stirred in DIPE and then the DIPE was decanted off. The residue was dissolved in CH3OH, warmed and acidified with HCl/2-propanol. The resulting precipitate was filtered off and dried. Yield: 0.123 g of final compound 36 (51.5 %; M. p.: > 250C).

148546-99-0, 148546-99-0 3-(4-Methylpiperazin-1-yl)aniline 11564613, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2005/12304; (2005); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.,3022-15-9

Piperazine-2-carboxylic acid dihydrochloride (10.0 g, 49.2 mmol) was dissolved in H2O (125 mL) and 1,4-dioxane (200 mL), and the solution was brought to pH 11 with 50% NaOH in H2O. Benzyl chloroformate (14 mL, 98 mmol) was added while maintaining the pH at 11 with 50% NaOH in H2O. After 1 h, an additional portion of benzyl chloroformate (2 mL, 14 mmol) was added. After 30 min, the solution was extracted with Et2O (3 x 100 mL). The aqueous layer was brought to pH 2 with concentrated HCl and extracted with EtOAc (3 x 200 mL). The combined EtOAc extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure to give 18.9 g (96%) of the desired product as a thick oil. The material was used without further purification. LC-MS: RT = 9.250 min; [M+H]+ = 421.1.

As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

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

50606-32-1, Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50606-32-1, 56.2. 4-[2-Benzyloxycarbonylamino-2-(dimethoxy-phosphoryl)-acetyl]-piperazine-l- carboxylic acid butyl ester: To a solution of intermediate 56.1 (1.5 g) in DCM (5 mL) was added DIPEA (3.4 mL) and HATU (2.2 g). After stirring at RT for 10 min, intermediate 2.2 (1.1 g) was added. The reaction mixture was stirred overnight at RT and H2O was added. The phases were separated, the org. phase was washed with sat NaCl solution, dried (MgStheta4) and evaporated off. The crude was purified by CC (Hept/EA 2/8) to afford the desired compound (1.1 g). LC-MS (A): tR = 0.95 min; [M+H]+: 486.01.

The synthetic route of 50606-32-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; WO2009/69100; (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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

5317-33-9, EXAMPLE 104; 4-{7-[3-(4-Methyl-piperazin-1-yl)-propoxy]-quinazolin-4-yl}-piperidine-1-carboxylic acid (6-pyrrolidin-1-yl-pyridin-3-yl)-amide; To a solution of 3-(4-methylpiperazin-1-yl)-propan-1-ol (0.22 mmol) in anhydrous THF (2 mL) was added NaH (0.4 mmol) and the mixture was stirred at rt for 5 min. Then, 4-(7-fluoro-quinazolin-4-yl)-piperidine-1-carboxylic acid tert-butyl ester (0.2 mmol), prepared as described in Example 65, was added to it and the mixture was stirred at 60 C. for 2 h. It was then concentrated in vacuo and partitioned between water and DCM. The DCM layer was drawn off, washed with water, brine, dried (anhydrous MgSO4), filtered and concentrated in vacuo. This crude product was then treated with 3M HCl/MeOH (2 mL) and stirred at rt for 2 h and then concentrated in vacuo. A portion of the crude residue (0.05 mmol) was dissolved in a mixture of DCM:MeOH (1:1; 2 mL) and neutralized with excess Et3N (0.3 mmol) and treated with (6-pyrrolidin-1-yl-pyridin-3-yl)-carbamic acid 4-nitrophenyl ester hydrochloride (0.075 mmol), which was prepared from 6-Pyrrolidin-1-yl-pyridin-3-ylamine (WO 2002048152 A2) essentially as described in Example 74a, at rt for 1 h. It was then concentrated in vacuo and the crude product was dissolved in DCM and washed with water thrice, then washed with brine, dried over anhydrous MgSO4, filtered and concentrated in vacuo. The crude product was then purified by Preparative TLC (silica gel; DCM:MeOH:NH4OH, 90:9:1) to obtain 10 mg (35%) of the title compound. 1H-NMR (300 MHz, CDCl3): 9.13 (s, 1H), 8.08-7.96 (m, 2H), 7.66-7.60 (m, 1H), 7.34-7.22 (m, 2H), 6.39-6.27 (m, 2H), 4.32-4.14 (m, 4H), 3.74-3.59 (m, 1H), 3.46-3.38 (m, 4H), 3.13 (t, 2H), 2.65-2.50 (m, 10H), 2.37 (s, 3H), 2.22-1.86 (m, 10H). LC/MS (ESI): 559.1 (MH)+.

5317-33-9 3-(4-Methylpiperazin-1-yl)propan-1-ol 79208, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Baindur, Nand; Gaul, Michael David; Kreutter, Kevin Douglas; Baumann, Christian Andrew; Kim, Alexander J.; Xu, Guozhang; Tuman, Robert W.; Johnson, Dana L.; US2006/281772; (2006); 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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, To a stirred solution of triphosgene (0.373 mg, 1.258 lmol) in anhydr. THF (20 ml) was added 7d (S)-4-(4-morpholino-6-(tetrahydrofuran-3-yloxy)-1,3,5-triazin-2-yl)aniline (1.200 mg, 2.097 lmol) at 25 C. The reaction mixture wasstirred for 5 min and NEt3 (45 mL, 0.33 mmol) were added and the reaction mixture was stirred for additional 1 h. Then 9a 4-amino-N-(2-(dimethylamino)ethyl)-N-methylbenzamide (1.392 mg, 6.29 lmol) was added and stirred for another 0.5 h and NEt3 (406 mL, 2.91 mmol) was added and the mixture was stirred over night. The solvents were removed in a N2 stream and the crude mixture was purified by semi-prep-HPLC to obtain 3 as an off white solid (665 mg, 53%).

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Dehnhardt, Christoph M.; Venkatesan, Aranapakam M.; Chen, Zecheng; Delos-Santos, Efren; Ayral-Kaloustian, Semiramis; Brooijmans, Natasja; Yu, Ker; Hollander, Irwin; Feldberg, Larry; Lucas, Judy; Mallon, Robert; Bioorganic and Medicinal Chemistry Letters; vol. 21; 16; (2011); p. 4773 – 4778;,
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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

(a) Step 1 cis-2,6-Dimethylpiperazine (0.114 g, 1.00 mmol) and potassium carbonate (0.0691 g, 0.500 mmol) were added to 4 mL of methylene chloride, and stirred at room temperature. Four milliliters of a methylene chloride solution of the 7-(bromomethyl)-6-methoxybenzofuran-3(2H)-one (0.129 g, 0.500 mmol) described in [WO2011/136319] was added dropwise, and stirring was continued for 12 hours at room temperature. The reaction solution was filtered, and the residue obtained by concentrating the filtrate was purified by silica gel chromatography (methanol/chloroform), and 7-[(cis-3,5-dimethylpiperazin-1-yl)methyl]-6-methoxybenzofuran-3(2H)-one (0.131 g, 90percent) was obtained. 1H NMR (300 MHz, CDCl3) delta 1.03 (d, J=6.6 Hz, 6H), 1.73 (t, J=11.1 Hz, 2H), 2.82 (dd, J=2.1, 11.1 Hz, 2H), 2.87-2.98 (m, 2H), 3.67 (s, 2H), 3.93 (s, 3H), 4.64 (s, 2H), 6.70 (d, J=9.0 Hz, 1H), 7.62 (d, J=9.0 Hz, 1H).

21655-48-1, As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
Patent; THE UNIVERSITY OF TOKYO; NAGANO, Tetsuo; NAKANO, Hirofumi; HASEGAWA, Tsukasa; SAITO, Nae; KOJIMA, Hirotatsu; OKABE, Takayoshi; MUKAIDA, Naofumi; (42 pag.)US2017/145005; (2017); 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.67455-41-8,4-(Piperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.,67455-41-8

General procedure: To a solution of arylamine (0.5 mmol, 1.0 equiv) in MeOH(1.0 mL) was added HCl (0.5 mL, 1.5 mmol, 3.0 equiv) followed by H2O (0.5 ml). This mixture was stirred 2 min, and the NaNO2 solution (0.25 mL) was then added. The NaNO2 solution was prepared by dissolving 35 mg of NaNO2 in H2O (0.25 mL). This mixture was stirred 30 minat 0-5 C followed by B2pin2 (2, 381 mg, 1.5 mmol, 3.0equiv) in MeOH (1.0 mL). This mixture was stirred 60 min.H2O (10 mL) was added to the reaction mixture, then extracted with CH2Cl2 (50 mL, 3¡Á). The combined organic layers were washed with sat. NaHCO3, dried over Na2SO4, followed by evaporation, and the crude residue was purified by flash chromatography.

As the paragraph descriping shows that 67455-41-8 is playing an increasingly important role.

Reference£º
Article; Zhao, Cong-Jun; Xue, Dong; Jia, Zhi-Hui; Wang, Chao; Xiao, Jianliang; Synlett; vol. 25; 11; (2014); p. 1577 – 1584;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

150407-69-5, (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

150407-69-5, To a solution of piperazine carboxylic acid (10 g, 27 mmol) in DCM (50 mL) was added TEA (2.39 mL, 54 mmol) and HATU (11.4 g, 30 mmol) with stirring. The reaction mixture was stirred at room temperature for 30 mins then treated with piperidine (2.57 g, 30 mmol). The reaction solution was stirred for 48 hrs then concentrated. The residue was purified by columnchromatography on silica gel eluted with petroleum ether / EtOAc (3 : 1) to afford compound Tnt48-1 as yellow oil (10.7g). MS-ESI (mlz): 432 (M+1) Rf: 0.6 (PE : EtOAc= 1: 1) ?H NMR(CDC13) oe: 7.307.24 (m, 5H), 5.25 (s, 1H), 5.14 (d, J=12.3 Hz, 1H), 5.064.98 (m, 1H),4.183.80 (m, 5H), 3.41 (s, 2H), 3.21 (d, J13 Hz, 3H), 1.61 (s, 2H), 1.52 (t, J1=16.6 Hz,J214.7 Hz, 3H), 1.39 (s, 1OH).

The synthetic route of 150407-69-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; COBURN, Craig; MALETIC, Milana; LUO, Yunfu; QI, Zhiqi; YU, Tingting; SOLL, Richard; WO2015/70367; (2015); 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

Reference Example 50: 3 -Oxo-4-(2-trimethylsilanyl-ethoxymethyl)-piperazine-l -carboxylic acid benzyl ester.; Piperazin-2-one (2.00 g, 20.0 mmol) was dissolved in H2O (10 ml) – 1,4-dioxane (10 ml); and NaHCO3 (1.85 g, 22.0 mmol) and benzylchloroformate (3.42 g, 20.0 mmol) was added thereto. After stirring at room temperature for 13 h, the reaction mixture was diluted with H2O and EtOAc. The aqueous layer was extracted with EtOAc and the combined organic layer was washed with brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure to obtain crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester as pale brown oil. This oil was used for the next step without further purification. The crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester was dissolved in DMF (40 ml) and NaH (55% in oil, 1.05 g, 24.0 mmol) and SEMCl (5.01 g, 30.0 mmol) was added thereto at room temperature. After stirring at 500C for 18 h, the reaction mixture was diluted with EtOAc. The mixture was washed with H2O and brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure. The EPO residue was purified by silica gel column chromatography (hexane / EtOAc = 8 / 2 to 5 / 5, to obtain the intended compound as a colorless oil.

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK & CO., INC.; BANYU PHARMACEUTICAL CO., LTD.; WO2007/11809; (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

2-[(4-Bromo-2-fluoro-phenyl)methyl]-6-phenyl-thiazinane 1,1-dioxide (208 mg, 0.52 mmol), Pd(OAc)2 (5.8 mg, 0.026 mmol), 2-dicyclohexylphosphine-2′,6′-di-iso-propoxy-1,1′-biphenyl (24.8 mg, 0.052 mmol) and cesium carbonate (254 mg, 0.78 mmol) were weighed out in a vial and the vial was purged with nitrogen. 1,4-Dioxane (2.5 mL) and 1-piperazin-1-ylethanone (100 mg, 0.78 mmol) were then added and the reaction was stirred at 80 C. for 2 hours. The reaction was then filtered through diatomaceous earth, concentrated and purified by reverse-phase HPLC to give 1-(4-(4-((1,1-dioxido-6-phenyl-1,2-thiazinan-2-yl)methyl)-3-fluorophenyl)piperazin-1-yl)ethanone (210 mg, 89% yield).

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference£º
Patent; Genentech, Inc.; Fauber, Benjamin; Gobbi, Alberto; Rene, Olivier; Bodil van Niel, Monique; Gancia, Emanuela; Gaines, Simon; Laddywahetty, Tammy; Vesey, David; Ward, Stuart; Winship, Paul; US2015/197529; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics