Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of carboxylic acid (50 mmol) in DMF (0.25 mL) in a 48 position Mettler Toledo XT reaction block was added PyBOP (50 mmol, 0.2 mL of 0.3 M solution in DMF) and TEA (75 mmol, 0.05 mL of 1.5 M solution in DMF) followed by the appropriate amine build blocks (55 mmol, 0.55 ml of 1 M solution in DMF). The reactions were stirred at rt 24 h and concentrated by GeneVac HT-4 to remove all reaction mixture including excess amine and DMF. The crude mixtures were dissolved in EtOAc (1 mL) and filtered through silica-packed short-column and washed with EtOAc (3 mL). The collected organic solution was concentrated in GeneVac HT-4 and dissolved in DMSO (1 mL). DMSO solution was subjected to HTAC for pre-purification analysis, purification, and final QC., 30459-17-7

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

Reference£º
Article; Hwang, Jong Yeon; Attia, Ramy R.; Carrillo, Angela K.; Connelly, Michele C.; Guy, R. Kiplin; Bioorganic and Medicinal Chemistry Letters; vol. 23; 6; (2013); p. 1891 – 1895;,
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.106261-48-7,4-((4-Methylpiperazin-1-yl)methyl)benzoic acid,as a common compound, the synthetic route is as follows.

Example 3: Preparation of 4-[(4-methylpiperazin-1-yl)methyl]-N-{6-methyl-5-[(4-(pyrid-3-yl)pyrimid-2-yl)amino]pyrid-3-yl}benzamide Method D; To a flask was added 4-((4-methylpiperazin-1-yl)methyl)benzoic acid (3.2 g) and SOCl2 (100 mL) and the solution was refluxed for 4 hours. The reaction mixture was concentrated under reduced pressure to give a solid, which was used for the next step directly. To the above carboxylic acid chloride was dropped a clear solution of N-(5-amino-2-methylpyridin-3-yl)-4-(3-pyridyl)pyrimidin-2-amine (3.0 g) in pyridine (80 mL) and the solution was stirred at room temperature overnight. The solvent was removed under reduced pressure, and then the residue was added with chloroform (100 mL) and water (100 mL) for extraction. The organic phase was dried, filtrated, concentrated, and purified through column chromatography to give 4-[(4-methylpiperazin-1-yl)methyl]-N-{6-methyl-5-[(4-(pyrid-3-yl)pyrimid-2-yl)amino]pyrid-3-yl}benzamide (4.2 g)., 106261-48-7

The synthetic route of 106261-48-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sun, Piaoyang; EP1840122; (2007); 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.928025-56-3,(S)-tert-Butyl 3-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Intermediate 16 (80% purity, 2.67 g, 9.95 mmol) was dissolved in THF (50 mL) and DIPEA (17.5 mL, 100.47 mmol) was added. tert-Butyl (3S)-3-ethyl- piperazine-1 -carboxylate (2.22 g, 10.36 mmol) was added and the reaction mixture was stirred at r.t. for approximately 60 h. The reaction mixture was concentrated in vacuo and the residue was partitioned between EtOAc (100 mL) and water (50 mL). The organic phase was washed with brine (50 mL), dried with anhydrous sodium sulfate and concentrated in vacuo. The residue was purified by flash column chromatography on silica (gradient elution with 0-20% EtO Ac/heptane) to afford the title compound (3.2 g, 77.9%) as a yellow gum. deltaEta (CDC13, 400 MHz) 7.71 (s, 1H), 5.58 (br s, 2H), 4.30-4.00 (m, 2H), 3.36 (t, J 11.9 Hz, 1H), 3.15 (br s, 1H), 2.98 (br s, 1H), 2.55 (s, 3H), 2.20 (s, 3H), 1.82-1.70 (m, 2H), 1.49 (s, 9H), 0.92 (t, J 6.7 Hz, 3H)., 928025-56-3

As the paragraph descriping shows that 928025-56-3 is playing an increasingly important role.

Reference£º
Patent; HORSLEY Helen Tracey; HUANG Qiuya; NEUSS Judi Charlotte; REUBERSON James Thomas; VANDERHOYDONCK Bart; WO2015/193169; A1; (2015);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

928025-56-3, (S)-tert-Butyl 3-ethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 111a (S)-tert-Butyl 3-Ethyl-4-(6-nitropyridin-3-yl)piperazine-1-carboxylate 111a A 250-mL single-neck round-bottomed flask equipped with a magnetic stirrer and a reflux condenser was charged with 1,4-dioxane (50 mL), 5-bromo-2-nitropyridine (2.02 g, 10 mmol), (S)-tert-butyl 3-ethylpiperazine-1-carboxylate (2.14 g, 10.0 mmol), Pd2(dba)3 (458 mg, 0.50 mmol), XantPhos (576 mg, 1.0 mmol), and cesium carbonate (6.52 g, 20 mmol). After three cycles of vacuum/argon flush, the mixture was heated at 100 C. overnight. After this time the reaction was cooled to room temperature. It was then filtered and the filtrate was evaporated under reduced pressure. The residue was purified by silica-gel column chromatography eluting with 3:1 petroleum ether/ethyl acetate to afford 111a (700 mg, 22%) as a yellow solid. MS: [M+H]+ 336, 928025-56-3

928025-56-3 (S)-tert-Butyl 3-ethylpiperazine-1-carboxylate 24820542, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GENENTECH, INC.; Crawford, James John; Ortwine, Daniel Fred; Wei, BinQing; Young, Wendy B.; US2013/116246; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1214196-85-6, 1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A suspension of 1-Boc-piperazine-2-carboxylic acid (9, 2.0 g, 8.69 mmol), EDCI (1.99 g, 10.42 mmol) and DMAP (0.32 g,2.61 mmol) in MeOH/CH2Cl2 (1:1) was stirred at 40 C for 1.5 hr, then the resulting solution was cooled down to room temperature and stirred for another 4 hrs. After removing the solvent, the residue was dissolved in CH2Cl2. The solution was washed with H2O (50 mL x 3). The combined aqueous was re-extracted with CH2Cl2 (40 mL x 3). All of the organics were combined, washed with 1 N NaHCO3 (50 mL x 3) and brine, and finally dried over Na2SO4. The product, a colorless liquid, was purified via flash chromatography, eluted with CH2Cl2 then 10% MeOH/CH2Cl2. Rf= 0.7 (10% MeOH/CH2Cl2, stained by phosphomolybdic acid (PMA)); yield – 84%

1214196-85-6, As the paragraph descriping shows that 1214196-85-6 is playing an increasingly important role.

Reference£º
Article; Zhao, Huanyu; Prosser, Anthony R.; Liotta, Dennis C.; Wilson, Lawrence J.; Bioorganic and Medicinal Chemistry Letters; vol. 25; 21; (2015); p. 4950 – 4955;,
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.

To a 0.342 g of 4-(4-ethyl-piperazin-1-yl)phenylamine (4d;0.00167 mol) in a dry round bottom flask was added 10 mL of 98%ethanol. Then 0.314 g of methyl 2,4-dioxo-6-phenylcyclohexanecarboxylate(E201; previously synthesized in our lab)22 was added.The reaction was refluxed for about 6 h and a total of 3 mL of additionalethanol was added. The reaction was monitored by thin layer chromatography(dichloromethane: methanol 85/15). After 6 h, the heatwas turned off and reaction continued to stir overnight. After reactionwas completed, the reaction was adsorbed on a silica gel and purifiedby automated flash chromatography (dichloromethane: methanol 75/25) to yield a dark orange solid (0.189 g, 33%). 1H NMR (300 MHz, d-CDCl3): delta (ppm)1.133-1.258 (t, 3H), 2.523-2.571 (q, 2H), 2.617-2.684(t, 4H), 3.219-3.469 (t, 4H), 3.252-3.550 (s, 3H), 5.476 (s, 1H),6.872-6.902 (d, 2H), 7.050-7.080 (2d, H), 7.263-7.328 (m, 5H). HRMS(ESI): m/z, Calcd. for C26H31N3O3 [M+H]+: 434.2433, found434.2435.

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

Reference£º
Article; Ghoneim, Ola M.; Bill, Ashley; Dhuguru, Jyothi; Szollosi, Doreen E.; Edafiogho, Ivan O.; Bioorganic and Medicinal Chemistry; vol. 26; 14; (2018); p. 3890 – 3898;,
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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

To a degassed solution of N-(4-(2-chloro-4-(2-methoxyethoxy)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)phenyl)-2,5-difluorobenzene sulfonamide (140 mg, 0.224 mmol in l,4-dioxane) was added 4-((4-methylpiperazin-l- yl)methyl)aniline (51 mg, 0.246 mmol), palladium(II) acetate (1 mg, 0.004 mmol), SPhos (3 mg, 0.008 mmol) and cesium carbonate (146 mg, 0.448 mmol). The mixture was heated under microwave irradiation at 150W for 20 min. The organic solvent was removed under vacuum and the aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with brine, dried over anhydrous sodium sulfate, and filtered. The filtrate was evaporated under reduced pressure. The product was purified by silica gel column chromatography using dichloro methane and methanol gradient eluents to give 2,5-difluoro- N-(4-(4-(2-methoxyethoxy)-2-((4-((4-methylpiperazin-l-yl)methyl)phenyl)amino)-7-((2- (trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)phenyl)benzenesulfonamide in 41% yield as a pale yellow solid. NMR (500 MHz, CDCh): d 7.63 (d, J = 8.5 Hz, 2H), 7.61 (d, J = 8.3 Hz, 2H), 7.53-7.57 (m, 1H), 7.25 (d, J = 8.3 Hz, 2H), 7.14-7.21 (m, 2H), 7.11 (d, J = 8.5 Hz, 2H), 6.96 (s, 2H), 5.51 (s, 2H), 4.55 (t, J = 4.6 Hz, 2H), 3.69 (t, J = 4.6 Hz, 2H), 3.56 (t, J = 8.3 Hz, 2H), 3.47 (s, 2H), 3.37(s, 3H), 2.48 (br, 8H), 2.29 (s, 3H), 0.92 (t, J = 8.3 Hz, 2H), -0.09 (s, 9H); Mass (ESI) m/z 794.58, 397.79 [M+H+], 70261-82-4

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DEVELOPMENT CENTER FOR BIOTECHNOLOGY; DCB-USA LLC; YEN, Shih-Chieh; LIAO, Chu-Bin; WANG, Hui-Chen; CHEN, Po-Ting; PAN, Yu-Chih; LI, Tsung-Hui; CHEN, Bo-Rong; CHIOU, Shian-Yi; (64 pag.)WO2019/133629; (2019); 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.639068-43-2,tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

639068-43-2, Step 3 Synthesis of 3,5-Dimethyl-4-(2-trifluoromethyl-benzoyl)-piperazine-1-carboxylic acid tert-butyl ester Triethyl amine (55.6 mg, 0.07 mL, 0.55 mmol) was added to a stirred solution of 2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (98.6 mg, 0.45 mmol) followed by 2-trifluoromethyl-benzoyl chloride (95.6 mg, 0.45 mmol) and the resulting mixture was stirred at room temperature for 30 minutes. The reaction mixture was concentrated under reduced pressure to get the residue. The residue thus obtained was purified by column chromatography using 60-120 silica gel and 50percent ethyl acetate in hexane to afford 74 mg (41.71percent yield) of 3,5-dimethyl-4-(2-trifluoromethyl-benzoyl)-piperazine-1-carboxylic acid tert-butyl ester. LCMS Purity: 96.7percent.

As the paragraph descriping shows that 639068-43-2 is playing an increasingly important role.

Reference£º
Patent; Bischoff, Alexander; Subramanya, Hosahalli; Sundaresan, Kumar; Sammeta, Srinivasa Raju; Vaka, Anil Kumar; US2010/160323; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

393781-71-0, 1-Boc-2-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1 ,1-dimethylethyl 2-ethyl-1-piperazinecarboxylate (100mg, 0.467 mmol) in DCM (5ml_) was added di-isopropylethylamine (0.253mL, 1.447 mmol), followed by gradual addition of 4-cyanobenzenesulfonyl chloride (103mg, 0.513 mmol). The reaction mixture was allowed to stir for 1 hour. The reaction mixture was diluted with DCM (1 OmL) and the solution was washed with saturated aqueous sodium bicarbonate solution (1OmL, twice), then with distilled water (1OmL). The organic layer was dried (MgSO4), filtered and reduced in vacuo to yield 1 ,1-dimethylethyl 4-[(4-cyanophenyl)sulfonyl]-2-ethyl-1-piperazinecarboxylate as a crude transparent oil (173mg), MS ES+ve m/z 280 (M+H-100). To 1 ,1-dimethylethyl 4-[(4-cyanophenyl)sulfonyl]-2-ethyl-1-piperazinecarboxylate (173mg, 0.456 mmol) was added hydrogen chloride 1 M solution in 1 ,4 dioxane (1OmL) solution, followed by the addition of 3 drops of water. The reaction mixture was allowed to stir for 14hours. After this time, 5M aqueous HCI (1 ml) was added and the mixture was stirred for 12hours. The reaction mixture was concentrated in vacuo to yield colourless oil. The colourless oil was dissolved in methanol (1 OmL) and passed down a SCX-2 column washing with two column volumes of methanol and eluting the product with 2N ammonia solution in methanol (three column volumes). The fraction containing eluted product was reduced in vacuo to yield 4-[(3-ethyl-1- piperazinyl)sulfonyl]benzonitrile (99mg) as a transparent oil, MS ES+ve m/z 280 (M+H).To a solution of 4-[(3-ethyl-1-piperazinyl)sulfonyl]benzonitrile (99mg, 0.354mol) in tetrahydrofuran (1OmL) was added triethylamine (0.074mL, 0.532mmol) followed by drop wise addition of benzoyl chloride (0.045mL, 0.390mmol). The reaction mixture was allowed to stir for 30minut.es. The reaction mixture was diluted with DCM (1 OmL) and the solution was washed with saturated aqueous sodium bicarbonate solution (1OmL, twice), then 0.1 M hydrochloric acid (1OmL). The organic layer was dried with (MgSO4), filtered and concentrated in vacuo to yield 144mg colourless oil. The oil was dissolved in minimum volume of hot ethyl acetate (~2ml), hot iso-hexane (10ml) was then added and allowed to cool to room temperature. The supernatant was decanted off, and residual solid triturated with diethyl ether (50ml), to yield a white solid (67mg, 37%).1H-NMR (CDCI3) delta 0.65-1.19 (3H, br m), 1.78-1.98 (2H, m), 2.20-2.40 (1 H, m), 2.40- 2.57 (1 H, m), 2.96-3.48 (1 H, m), 3.48-3.96 (3H, m), 4.21-5.01 (1 H, m), 7.28-7.31 (2H, m), 7.36-7.45 (3H, m), 7.81-7.89 (4H, m).MS ES+ve m/z 384 (M+H).The single enantiomers were isolated from the racemic 4-{[3-ethyl-4-(phenylcarbonyl)-1-piperazinyl]sulfonyl}benzonitrile (53mg) via chiral preparative chromatography using the following conditions:- Column: Chiralpak IC (20mm x 250mm, 5mum)- Eluent: Heptane: Ethanol 50:50 v/v pump-mixed – Flow rate =17. Omls/min- U.V. Absorbance (S) 215nm- Autosampler injection (250mul of sample in 20%Heptane/30%EtOH/50%DMF on column)- lsocratic Run time = 30 minutesIsolated enantiomers were analysed via chiral analytical chromatography using the following conditions:- Chiralpak IC (4.6mm x 250mm, 5mum)- Heptane: Ethanol 50:50 v/v pump-mixed – Flow rate =1. Omls/min- U.V. Absorbance (at) 215nm- Autosampler injection (1 Omul of sample in mobile phase on column)- lsocratic Run time = 30 minutesIsolated compounds: Example 5a: Faster running enantiomer (4-{[(3S)-3-ethyl-4-(phenylcarbonyl)-1- piperazinyl]sulfonyl}benzonitrile or 4-{[(3R)-3-ethyl-4-(phenylcarbonyl)-1- piperazinyl]sulfonyl}benzonitrile, 16mg)Retention time 19.37min, 393781-71-0

393781-71-0 1-Boc-2-Ethylpiperazine 18004789, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXO GROUP LIMITED; BESWICK, Paul, John; CAMPBELL, Alister; CRIDLAND, Andrew; GLEAVE, Robert, James; PAGE, Lee, William; WO2010/102663; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

9.1: 2,2-Dimethyl-piperazine-1,4-dicarboxylic acid 1-benzyl ester 4-tert-butyl ester To a solution of 18.5 g (82.0 mmol) 3,3-dimethyl-piperazine-1-carboxylic acid tert-butyl ester in 150 mL DCM at RT was added 30.0 mL (174 mmol) DIPEA. The mixture was cooled with ice and a solution of 14.0 mL (93.2 mmol) benzyl chloroformate in 60 mL DCM was added dropwise. The reaction mixture was stirred at RT over night and quenched with saturated aqueous sodium bicarbonate solution. The product was extracted with DCM. The organic layers were combined, dried over sodium sulfate and concentrated in vacuo. Yield: 23.0 g (81%) ESI-MS: m/z=249 (M-BOC+H)+

259808-67-8, The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; US2013/158042; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics