Tag: M.W:200-300

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：
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

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.

Acetic acid (33 ??_, 0.59 mmol), HOBt (87 mg, 0.65 mmol), TBTU (208 mg, 0.65 mmol), anhydrous triethylamine (131 ??_, 0.94 mmol) and anhydrous DMF (2 mL) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-(trifluoromethyl)phenyl)piperazine (150 mg, 0.65 mmol) and anhydrous DMF (1 mL) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred under nitrogen and monitored by TLC. After 24 hours, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M HCI solution. The aqueous mixture was extracted with DCM (20 mL, followed by 4 x 10 mL) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 mL) and brine (3 x 20 mL). The organic layer was dried over magnesium sulphate and the solvent removed in vacuo. The residue was purified using flash chromatography (4:1 , EtOAc:n-hexane) to obtain the desired product in a 57% yield. H NMR (300 MHz, CDCI3) ? 7.49 (d, J = 8.7 Hz, 2H), 6.91 (d, J = 8.7 Hz, 2H), 3.79-3.76 (m, 2H), 3.65-3.61 (m, 2H), 3.31-3.24 (m, 4H), 2.14 (s, 3H). 3C NMR (75 MHz, CDCI3) 168.0, 151.9, 125.4 (q, J = 3.75 Hz), 1 19.6 (q, J = 33 Hz), 1 18.2 (q, J = 268.5 Hz), 1 15.0, 48.3, 48.0, 45.8, 41.0, 21.3. MS (+ESI) calcd for C13 H15 F3 N2 O m/z: [M + H]+, 273.1209; found 273.1222 [Diff(ppm) = 4.8].

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

Reference：
Patent; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (2013); A1;,
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, In reference to the process disclosed in WO2012/031004, 2-nitro-5-bromopyridine (1.01 g, 5.0 mmol), tert-butyl 2-oxo-4-piperazinecarboxylate (1.00 g, 5.0 mmol, and cesium carbonate (3.26 g, 10.0 mmol) were suspended in 1,4-dioxane, and the suspension was bubbled with nitrogen gas for 30 minutes. To the suspension was added Xantphos (246 mg, 0.43 mmol) and tris(dibenzylideneacetone)dipalladium (229 mg, 0.25 mmol), and the mixture was stirred under reflux for two hours. The resultant reaction mixture was cooled to room temperature, and water and ethyl acetate were then added to the mixture, followed by filtration with Celite. The organic phase was separated from the filtrate, and the aqueous phase was extracted with ethyl acetate. The resultant organic phases were combined together and dried over anhydrous sodium sulfate, and the resultant solid was separated by filtration. The filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography to yield the title compound (1.08 g, 67%). 1H-NMR (CDCl3) delta: 8.67 (1H, d, J=2.4 Hz), 8.32 (1H, d, J=8.8 Hz), 8.15 (1H, dd, J=8.8, 2.4 Hz), 4.33 (2H, s), 3.93-3.83 (4H, m), 1.51 (9H, s)

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

Reference：
Patent; Teijin Pharma Limited; MIZUNO, Tsuyoshi; SHIMADA, Tomohiro; UNOKI, Gen; EBISAWA, Masaru; TAKEUCHI, Susumu; MINAMIZONO, Kunio; SASAKI, Kosuke; YOKOSAKA, Takuya; IGARASHI, Junji; MARUYAMA, Akinobu; TAKAHASHI, Hiroshi; HORIE, Kyohei; SAKAI, Yuri; (447 pag.)EP3305785; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIPEA (5.24 ml, 30.06 mmol) was added to a stirred mixture of ferf-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1.73 g, 7.51 mmol) and 7-bromo-4-chloro-5,8-difluoroquinazoline (2.1 g, 7.51 mmol) in MeCN (100 ml) at room temperature. The resulting solution was stirred at room temperature for 3 hours, a suspension developed after ~30 minutes. The precipitate was collected by filtration, washed with MeCN (3 x 20 ml) and dried under vacuum to afford desired product, 2.64 g. On standing overnight a second crop of desired product, 300 mgs was isolated to afford ferf-butyl 4-(7-bromo-5,8-difluoroquinazolin-4-yl)-3-(2-hydroxyethyl)piperazine-l-carboxylate (2.94 g, 83%), as a white solid, which was used without further purification. 1H NM R (400 MHz, DMSO, 30C) 1.43 (9H, s), 1.71 – 1.82 (2H, m), 2.86 (1H, s), 3.18 (1H, s), 3.37 – 3.51 (2H, m), 3.72 (1H, d), 3.97 (2H, d), 4.36 (1H, s), 4.70 (1H, s), 7.75 (1H, dd), 8.62 (1H, s) OH not observed, m/z (ES+), [M+H]+ 473, 475., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

6.4 g (26.09 mmol) tert-butyl-4-(aminocarbothioyl)piperazine 1-carboxylate and 3.8 mL CH3I in 80 mL dichloromethane were stirred for 4 days at room temperature. Evaporation of the mixture yielded the corresponding methyl compound as the hydroiodide which was reacted further without further purification., 196811-66-2

196811-66-2 tert-Butyl 4-carbamothioylpiperazine-1-carboxylate 12093220, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Amberg, Wilhelm; Netz, Astrid; Kling, Andreas; Ochse, Michael; Lange, Udo; Hutchins, Charles W.; Garcia-Ladona, Francisco Javier; Wernet, Wolfgang; Hahn, Alfred; US2010/41698; (2010); 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

Step 3: l-(4-Bromo-phenyl)-3-[4-(4-methyl-piperazine-l-carbonyl)-phenyl]-urea rTo a solution of (4-amino-phenyl)-(4-methyl-piperazine-l-yl)-methanone (10.0 g, 0.0456 mol) and TEA (4.7 g, 0.0456 mol) in DCM (150 mL) was added 4-bromophenyl isocyanate (10.9 g, 0.0547 mol). The reaction mixture was stirred at room temperature for 12 h. The white solid was obtained and was filtered and dried to afford the title compound [15.0 g, 79%]; LC-MS (ESI): Calculated mass: 416.1; Observed mass: 417.1 [M+H]+ (RT: 0.23 min).

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

Reference：
Patent; ENDO PHARMACEUTICALS INC.; SMITH, Roger, Astbury; THOMPSON, Scott, Kevin; HOSAHALLI, Subramanya; BEJUGAM, Mallesham; NANDURI, Srinivas; PANIGRAHI, Sunil, Kumar; MAHALINGAM, Natarajan; WO2012/58671; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

197638-83-8, 1-Boc-4-(4-Formylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,197638-83-8

Compound 23 was synthesized as show n Scheme 4.

The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; COMBS, Colin; MULLER, Gerhard; DAMEN, Eddy; NAGAMOTO-COMBS, Kumi; (73 pag.)WO2017/100703; (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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.,694499-26-8

Methyl 3-azido-4-methylbenzoate (9.6 g, 0.5 mol) and 4-((4-methylpiperazine-1-substituted) methyl) -3- (Trifluoromethyl) aniline (13.7 g, 0.5 mol) was dissolved in re-distilled tetrahydrofuran (50.0 mL), and a solution of potassium tert-butoxide (16.8 g, 0.15 mol) in re-distilled tetrahydrofuran (50.0 mL) was slowly dropped. After 1 hour of reaction, the temperature was naturally raised to room temperature and the reaction was continued for 8 hours. After the reaction was completed, the solvent was spin-dried, extracted with EtOAc and water, and the organic phase was washed with saturated brine,Anhydrous Na2SO4 was dried, and the red solid obtained by silica gel column chromatography was the target product (13.5 g, yield: 61%).

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chinese Academy Of Sciences Guangzhou Bio-pharmaceutical And Health Institute; Ding Ke; Li Yupeng; Shen Mengjie; Long Huoyou; Zhang Zhang; Leng Fang; Lu Xiaoyun; (51 pag.)CN103539784; (2016); B;,
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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A mixture of acetoxymethyl 4-nitrophenyl carbonate (1 mmol) and PDBTZ (1 mmol) in hexamethylphosphoramide (1.3 mL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide title compound., 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-METHYLPIPERAZINE-1-CARBOXYLIC acid test-butyl ester (160 mg; 0.80 MMOL ; 2 eq.) (prepared as reported in J. Med. Chem. 1993,36, 690-698), cesium carbonate (195 mg; 0.6 MMOL ; 1.5 eq. ), palladium acetate (9 mg; 0.04 MMOL ; 0.10 eq. ) and 2,2′- bis (diphenylphosphino)-1, 1′-binaphthyl (38 mg; 0.06 MMOL ; 0.15 eq. ) were added to a solution of 2-METHYLQUINOLIN-5-YL-TRIFLUOROMETHANESULFONATE (D1) (117 mg, 0.4 MMOL ; 1 eq) in dry toluene (2.5 mL) under nitrogen. The reaction mixture was stirred at reflux under nitrogen for 10 h. The reaction was cooled and filtered through a pad of celite which was then washed with DCM (50 mL). The filtrates was concentrated in vacuo and the crude product was purified by SPE cartridge (Si, 2g), eluting with 5percent ethylacetate in cyclohexane to afford 3-methyl-4-(2-methylquinolin-5-yl)piperazin-1- carboxylic acid tert-butyl ester as a yellow oil (84 mg; yield 62percent). MS; (ES) m/z: 341.45 [MH] +. C2OH27N302 requires 342. 4.APOS;H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.8-3. 6, m/m, 2H), 3. 4- 3. 3 (m, 1 H), 3. 2- 3. 1 (m, 1 H), 3.1-2. 9 (m, 2H), 2.74 (s, 3 H), 1.45 (s, 9H), 1.36 (d, 3H). This compound (84 mg) was dissolved in a mixture 3: 1 of trifluoroacetic acid: DCM (4 mL) and stirred at r. T. for 6h. The solvent was evaporated in vacuo and the residue purified on SCX cartridge (1G) to afford the title compound (D14) (44 mg; yield 76percent) MS; (ES) m/z: 241.45 [MH] +. C15H19N3 requires 242.4. 1H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.3 (m, 4H), 3.15 (m, 4 H), 2.74 (s, 3 H), 1.9 (m, 2H)., 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/46124; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics