Tag: M.W:200-300

611225-86-6, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

611225-86-6, 104 mg (0.35 mMol) triphosgene are ^j-n’ ^ dissolved in13 ml ice-cooled CH2CI2. ^-/ ~~” Then a solution of 230 mg (1.05mMol) 4-(4-ethylpiperazin-1-O Hylmethyl)~aniline and 209 i (1.50 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 3 additional minutes, the mixture is warmed up to rt by a water bath and then a solution of 1.0 mMol 5-(6-chloro-pyrimidin-4-yioxy)-2,3-dihydro-1H-indole (Step 14.1) and 139 jll. (1.00 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 2 h at rt, the mixture is diluted with sat. Na2C03 solution / water 1:1 and EtOAc, the aqueous phase separated off and extracted twice with EtOAc. The organic layers are washed with water and brine, dried (Na2S04) and concentrated. Crystallization from DIPE gives the title compound: MS: [M+1]+= 493 / 495; TLC(CH2CI2/MeOH/NH3conc- 90:10:1): Rf = 0.24; HPLC: et_ = 10.5.

The synthetic route of 611225-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2006/34833; (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.

General procedure: To a solution of9(0.16g,0.58mmol) ini-PrOH(5mL),substituted phenylamine(0.64mmol)wasadded. The reaction mixture was stirred at reflux for4h under N2atmosphere. After the reaction was completed, the mixture wasnaturally cooled to room temperature.Themixture was filtered and the solid was collectedto giveintermediate12or15. 1.2.1 (4-((6-Bromoquinazolin-4-yl)amino)phenyl)(4-methylpiperazin-1-yl)methanone (12a)Yellow solid; yield:73 %.MS (ESI)m/z: [M+H]+=426.1/428.1.

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

Reference：
Article; Xin, Minhang; Hei, Yuan-Yuan; Zhang, Hao; Shen, Ying; Zhang, San-Qi; Bioorganic and Medicinal Chemistry Letters; vol. 27; 9; (2017); p. 1972 – 1977;,
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.

To compound 4 (183mg , 0.8 mmol) in DCM (3 ml), was added DIPEA ( 0.278 ml, 2 eq) and then propionyl chloride (130mg, 1 mmol) . The reaction was stirred at room temperature for lhr. The mixture was concentrated and partitioned between ethyl acetate and water, ethyl acetate layer was separated and dried, concentrated, then HC1 in dioxane ( 4N, 2 ml) was added. The mixture was stirred at room temperature for lhr, concentrated to afford crude 5a. It was then diluted with dry DMF ( 5 ml), was added, followed by addition of DIPEA (0.278ml, 1.6 mmol) and then (Biotin-LC-LC-NHS ( 454mg, O.Smmol). The mixture was stirred at room temperature for 12 hrs. The mixture was diluted with water, extracted with ethyl acetate. The organics were concentrated and then purified by HPLC to yield the desired product 6a ( 390 mg). NMR: pass, 192130-34-0

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

Reference：
Patent; NESTEC S.A.; SELVARAJ, Fabiyola; PRINCEN, Fred; SINGH, Sharat; WO2014/188377; (2014); 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.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

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

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