Month: March 2021

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.

To a mixture of 4-(4-carboxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (918 mg, 3 mmol) and 5-aminoindan (399 mg, 3 mmol) in methylene chloride (30 mL) was added EDCI (580 mg, 3 mmol) and DMAP (20 mg, 0.16 mmol). The mixture was stirred at room temperature overnight and then extracted with methylene chloride (50 mL) and aqueous hydrochloric acid (1 N, 20 mL). The organic layer was washed with water, then sodium hydroxide solution and finally with water and brine. The solution was dried over sodium sulfate and filtered. Solvents were evaporated and the residue was crystallized from ethyl acetate (40 mL) to give 4-[4-(indan-5-ylcarbamoyl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester. This intermediate was dissolved in methylene chloride (5 mL) and trifluoroacetic acid (3 mL). The mixture was stirred at room temperature for 1 hr and solvents were evaporated. The residue was extracted with methylene chloride and 1 N sodium hydroxide solution. The organic layer was washed with brine and dried over sodium sulfate. The product, N-indan-5-yl-4-piperazin-1-yl-benzamide was obtained after solvent evaporation (450 mg, Yield: 47%). LCMS calc for C20H23N3O (m/e) 321.42, obsd 322.5 (M+H).

162046-66-4, As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference£º
Patent; Bolin, David Robert; Cheung, Adrian Wai-Hing; Hamilton, Matthew Michael; Marcopulos, Nicholas; McDermott, Lee Apostle; Qian, Yimin; US2010/113782; (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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

STEP A: 4-(4-Bromo-2-cvano-phenyl)-piperazine-1-carboxylic acid tert-butyl ester. A mixture of 5-bromo-2-fluoro-benzonitrile (1.05g), piperazine-1 -carboxylic acid tert-butyl ester (1.08g) and Na2CO3 (1.03g) in DMF was heated to 1000C for 24h. The resulting mixture was cooled, diluted with water (50 ml_) and extracted with diethyl ether. The resulting mixture was dried over MgSO4, the solvent was removed and the resulting residue purified on SiO2 (hexanes/ EtOAc 0 to 25%) to yield the title compound., 57260-71-6

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; Janssen Pharmaceutica N.V.; WO2009/79593; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8,694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

to a solution of HSD1251 (50 mg, 0.18 mmol) in DMF (2.5 mL) was added 4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (0.19 mmol), HATU (0.18 mmol), and DIPEA (0.39 mmol). Reaction was continued for 12 h at room temperature and monitored by TLC. After completion, reaction mixture was extracted with ethyl acetate and washed with brine solution and dried over Na2S04. Crude was purified with flash chromatography to get the desired product as Off-white solid (50% yield, 47 mg1H NMR (500 MHz, DMSO-6) delta 10.93 (s, 1H), 8.63 (s, 1H), 8.29 (d, = 2.2 Hz, 1H), 8.05 (dd, = 8.5, 2.3 Hz, 1H), 7.98 – 7.89 (m, 2H), 7.71 (d, = 8.5 Hz, 1H), 3.56 (s, 2H), 3.34 – 3.30 (m, 2H), 3.13 (t, = 6.2 Hz, 2H), 2.37 (s, 8H), 2.14 (s, 3H), 1.99 (ddt, = 8.9, 6.3, 2.9 Hz, 2H), 1.87 – 1.79 (m, 2H);13C NMR (126 MHz, DMSO) delta 166.54, 149.19, 143.71, 142.60, 138.52, 132.53, 131.81, 129.74, 129.42, 128.11 (q, = 28.9 Hz), 125.91(q, = 274.6 Hz), 123.78, 123.53, 117.19, 117.14, 116.03, 57.94, 55.22, 53.19, 46.22, 29.73, 26.89, 22.37, 22.07; HRMS (ESI) m/z calcd for C28H30F3N6O [M + H]+523.2433, found 523.2433.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Patent; PURDUE RESEARCH FOUNDATION; SINTIM, Herman O.; DAYAL, Neetu; OPOKU-TEMENG, Clement; (195 pag.)WO2018/183586; (2018); 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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

Example 0723 Triethylamine was added to a solution of hydrochloride (23 mg) of 1-methylpiperazin-2-one in dichloromethane (1 mL), followed by adjusting to pH 8. 3-(4-(6-((5-Isopropylpyridazin-3-yl)amino)-1,5-naphthyridin-3-yl)-1H-pyrazol-1-yl)propanal (19 mg), acetic acid (0.01 mL), and sodium triacetoxyborohydride (42 mg) were added thereto, followed by stirring at room temperature for 1 hour. The solvent was distilled off under reduced pressure, and the obtained residue was purified by silica gel column chromatography (ethyl acetate-methanol, NH silica), thereby obtaining 4-(3-(4-(6-((5-isopropylpyridazin-3-yl)amino)-1,5-naphthyridin-3-yl)-1H-pyrazol-1-yl)propyl)-1-methylpiperazin-2-one (4.4 mg) as a white solid. 1H-NMR (DMSO-d6) delta: 10.70 (1H, s), 9.05 (1H, d, J=1.8 Hz), 8.86 (1H, d, J=2.1 Hz), 8.72 (1H, s), 8.52 (1H, s), 8.24- 8.18 (3H, m), 7.70 (1H, d, J=9.3 Hz), 4.24-4.17 (2H, m), 3.30-3.25 (2H, m), 3.09-2.98 (1H, m), 2.87-2.83 (2H, m), 2.80 (3H, s), 2.66-2.60 (2H, m), 2.40-2.32 (2H, m), 2.07-1.98 (2H, m), 1.34 (6H, d, J=7.2 Hz). MS m/z (M+H): 486., 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference£º
Patent; FUJIFILM Corporation; FURUYAMA, Hidetomo; KURIHARA, Hideki; TERAO, Takahiro; NAKAGAWA, Daisuke; TANABE, Shintaro; KATO, Takayuki; YAMAMOTO, Masahiko; SEKINE, Shinichiro; MASHIKO, Tomoyuki; INUKI, Shinsuke; UEDA, Satoshi; US2015/322063; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

0.36 g of N-[4-tert-butyl-5-(4-methoxybenzyl)thiazol-2-yl]-2-chloroacetamide and 5 mL of tetrahydrofuran, Stir at room temperature, 0.24 g of pyridine and 0.23 g of N-ethylpiperazine are added; Reaction overnight, Desolvent, Add dichloromethane, Saturated salt water wash, Drying with anhydrous sodium sulfate, Desolvent, Add petroleum ether to precipitate solids, Suction filtration Wash with petroleum ether, Dry to obtain light yellow solid N-[4-tert-butyl-5-(4-methoxybenzyl)thiazol-2-yl]-2-(4-ethylpiperazinyl)acetamide, yield 65.1%

5308-25-8, As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference£º
Patent; Hunan University; Hu Aixi; Wu Zhilin; Ding Na; Ye Jiao; (20 pag.)CN107365280; (2017); A;,
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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

7-Bromo-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridine-2-carbaldehyde (69-1) (1 g, 3.90 mmol) and (R)-tert-butyl 3-methylpiperazine-1-carboxylate (70-1) (0.935 g, 4.67 mmol) were dissolved in DCE (26 mL) and acetic acid (0.266 mL, 4.67 mmol) was added. The reaction was stirred for 30 min and sodium triacetoxyborohydride (4.13 g, 19.5 mmol) was added portionwise. After stirring for 16 hours the reaction was quenched by the slow addition of sat. sodium bicarbonate (100 mL) and extracted with DCM (2 x 100 mL). The combined organics were washed with brine, dried over sodium sulfate and concentrated. The residue was purified by column chromotagraphy (silica, 0-10 % MeOH in DCM) to give (R)-tert-butyl 4-((7-bromo-5- methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-2-yl)methyl)-3-methylpiperazine-1-carboxylate (70.2) (1.3 g, 76 %) as a white solid. LC/MS (ES+): m/z 440.8 [M + H]+, 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; C4 THERAPEUTICS, INC.; PHILLIPS, Andrew, J.; NASVESCHUK, Chris, G.; HENDERSON, James, A.; LIANG, Yanke; FITZGERALD, Mark, E.; MICHAEL, Ryan, E.; (790 pag.)WO2017/197056; (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.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.

182618-86-6, A mixture of 4-(4-nitro-phenyl)-piperazine-l-carboxylic acid tert-butyl ester (3 g, 9.76 mmol) and 10% palladium on carbon (300 mg) in 50 mL ethanol and 20 mL ethyl acetate was hydrogenated at room temperature under a 50 psi hydrogen atmosphere for 2 hrs.The reaction mixture was filtered through a plug of Celite and evaporated under reduced pressure to give 4-(4-amino-phenyl)-piperazine-l-carboxylic acid tert-butyl ester that was used in the in the next step without further purification.

The synthetic route of 182618-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2008/141976; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-(Thiophen-2-yl) hexanoic acid (77 mg, 0.39 mmol), HOBt (58 mg, 0.43 mmol), TBTU (138 mg, 0.43 mmol), anhydrous triethylamine (87 ??, 0.63 mmol) and dry 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 (100 mg, 0.43 mmol and dry 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 for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (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 evaporated under reduced pressure. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 75 % yield. H NMR (300 MHz, CDCI3) ? 7.48 (d, 2H), 7.08 (dd, 1 H), 6.88-6.93 (m, 3H), 6.76-6.77 (m, 1 H), 3.75 (t, 2H), 3.59 (t, 2H), 3.22-3.28 (m, 4H), 2.81 (t, 2H), 2.34 (t, 2H), 1.65-1.77 (m, 4H), 1.44-1.48 (m, 4H). MS (+ESI) calcd for C18 H21 F3 N4 O m/z: [M + Na]+ , 410.1621 ; found 433.1532 [Diff(ppm) = -1.15]., 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
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

5271-27-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

(0667) A mixture of 4-iodobenzonitrile (300 mg, 1.31 mmol), 1-methyl-3-phenylpiperazine (346 mg, 1.96 mmol), cesium carbonate (1.28 g, 3.93 mmol) and chloro(2-dicyclohexylphosphino- 2′,6′-dimethoxy-1,1′-biphenyl)[2-(2-aminoethylphenyl)]palladium(II) dichloromethane adduct (176 mg, 0.262 mmol) in tert-amyl alcohol (5 mL) was stirred at 100 ¡ãC for 16 h under N2. After cooling to ambient temperature, the mixture was concentrated under reduced pressure to give a residue, which was diluted with H2O (10 mL). The water layer was extracted with EtOAc (20 mL x 2). The collected organic layers were washed with brine (10 mL) and dried over anhydrous Na2SO4. The mixture was filtered and the filtrate was concentrated under reduced pressure. The residue was purified by flash silica gel chromatography (ISCO?; 4 g SepaFlash? Silica Flash Column, Eluent of 065percent EA/PE gradient (at) 40 mL/min) to give 4-(4-methyl-2- phenylpiperazin-1-yl)benzonitrile as an oil. ESI-MS m/z [M+H]+: 277.9.

5271-27-2 1-Methyl-3-phenylpiperazine 2760009, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; WALJI, Abbas; BERGER, Richard; STUMP, Craig, A.; SCHLEGEL, Kelly Ann, S.; MULHEARN, James, J.; GRESHOCK, Thomas, J.; WANG, Deping; FRALEY, Mark, E.; JONES, Kristen, G.; (273 pag.)WO2017/222951; (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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

129799-08-2, To 1-(1,1-dimethylethyl) 3-methyl piperazine-1,3-dicarboxylate (1.00g, 4.09 mmol) in dry toluene (15 mL) was added 3-bromo-chlorobenzene (653 mg, 3.41 mmol), Pd2(dba)3 (93.0 mg, 0.102 mmol), BINAP (191 mg, 0.307 mmol), and cesium carbonate (1.11 g, 4.77 mmol). The reaction mixture was stirred at 100 C for 42 h, then cooled to room temperature and filtered through celite. The filter cake was washed with ethanol, and the filtrate was concentrated. Column chromatography on silica (hexanes:ethyl acetate 3: 1) provided 1-(1,1-dimethylethyl) 3-methyl 4-(3-chlorophenyl)piperazine-1,3- dicarboxylate (310 mg, 21% yield) as a colorless oil. ?H NMR (400 MHz, CDC13) 8 7.20- 7.13 (t, 1H), 6.84-6.79 (m, 2H), 6.73-6.78 (d, 1H), 4.63-4.50 (br s, 1H), 4.41-4.32 (br s, 1H), 4.24-4.02 (br s, 2H), 3.71-3.65 (s, 3H), 3.55-3.46 (br s, 1H), 3.42-3.26 (br s, 1H), 3.16-2.97 (br s, 1H), 1.49-1.42 (s, 9H); MS (ESI) for C17H23ClN204: 355 (MH(at)).

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EXELIXIS, INC.; WO2005/117909; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics