Month: May 2021

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.

Adding 2, 6-lupetazin (11.4g, 100mmol, 1eq) and di-tert-butyl dicarbonate (21.8g, 100mmol, 1eq) into a 250mlflask; and then adding 100ml tetrahydrofuran, reacting under room temperature for 4 hours; and condensing up tetrahydrofuran(i.e., condensing tetrahydrofuran until used up), 21.4g orange-colored oily substance ZTH-1 is obtained, whereinthe yield is 100%., 21655-48-1

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

Reference：
Patent; Suzhou Maidixian Pharmaceutical Inc.; Zhang, Nan; Zhong, Rong; ZHANG, Nan; ZHONG, Rong; EP2589601; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a sealed tube, 2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)-7-fluoro-pyrido[1,2-a]pyrimidin-4-one (Intermediate 2; 50 mg, 0.162 mmol), and cis-2,6-dimethylpiperazine (74 mg, 0.647 mmol, 4.0 eq.) were stirred in DMSO (1.5 mL) at 110 C. overnight. The solvent was removed under high vacuum. The residue was taken up in CH2Cl2 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2SO4 and concentrated in vacuo. The crude was purified by column chromatography (SiO2, CH2Cl2/MeOH=95/5 to 90/10) to afford the title product (32 mg, 49%) as a light yellow solid. MS m/z 404.4 [M+H+].

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Hoffmann-La Roche Inc.; PTC Therapeutics, Inc.; Ratni, Hasane; Green, Luke; Weetall, Maria L.; Naryshkin, Nikolai A.; (33 pag.)US2019/315773; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1-chloro-4-methoxy-5-nitro-2-vinylbenzene (0.42 g,1.95 mmol), 4-(4- methyl-piperazin-1-yl)-benzylamine (1.2 g, 5.85 mmol) and quinol (0.043 g, 0.39 mmol) in n-butanol (8 mL) was heated to reflux for 12 hours under a N2 atmosphere. Water (100 mL) was added and the reaction mixture extracted with EtOAc (3 X 100 mL). The combined organic extracts were washed with brine (50 mL), dried (Na2S04) and concentrated under reduced pressure. The residue was purified by columnchromatography on neutral silica gel using 3-5% methanol in DC to give the title compound (0.35 g, 43%) as a solid.

216144-45-5, As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference：
Patent; SENTINEL ONCOLOGY LIMITED; BOYLE, Robert George; WALKER, David Winter; BOYCE, Richard Justin; WO2011/141716; (2011); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

General Procedure 3-1 : Synthesis of (4-((4-methylpiperazin-l-yl)methyl)aniline)[00187] The synthesis of the title compound was conducted as described in U.S. Pat. Appl. Publ.No. 2006058341 (March 16, 2006). Specifically, to a solution of 4-nitrobenzyl chloride in THF at the room temperature was added 1 -methyl piperazine. The solution was stirred for 3 hours after which time the crude reaction was diluted with ethyl acetate and washed repeatedly with water. The dried organics were concentrated to give directly the 4-nitrobenzylamine adduct.This was subsequently treated with Rainey Nickel in THF at 75PSI for 12 hours to give the title compound., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BIOGEN IDEC MA INC.; WO2008/94575; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4318-42-7

Step B/lntermediate B108: 1-(3-chloro-2-methyl-4-nitrophenyl)-4-(1- methylethyl)piperazine; To the solution of 2-chloro-4-fluoro-3-methyl-1 -nitrobenzene (12.5 g, 64.8 mmol, 1.2 equiv.) and isopropylpiperazine (10.8 g, 53.98 mmol, 1 equiv.) in 90 mL of anhydrous DMSO was added powdered K2CO3 (37 g, 269 mmol, 5 equiv.). The mixture was stirred at 40~50°C overnight before it was poured into 200 ml. of ice-water. The precipitates were collected and purified via chromatography on SiO2 to afford 1-(3- chloro-2-methyl-4-nitrophenyl)-4-(1-methylethyl)piperazine as a yellow solid (12.7g, 79percent Yield). 1 H NMR (400 MHz, CDCI3) delta ppm 0.95-1.05 (d, J=6.53Hz, 6H), 2.31 (s, 3H), 2.60-2.72 (m, 5H), 2.89-2.95 (m, 4H), 6.87 (d, J=8Hz, 1 H), 7.62 (d, J=8Hz, 1 H).

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/20990; (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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of 1-(2-hydroxyethyl)piperazine (51.7 g, 398 mmol) in DCM (500 mL) was added NEt3 (70.0 mL, 526 mmol) and di-tert-butyl dicarbonate (80.0 g, 367 mmol). The reaction mixture was stirred overnight at room temperature and then washed with 1M aq Na2CO3 solution (2×300 mL), dried (MgSO4) and concentrated in vacuo to give tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate (66.0 g, 72%) as a colourless oil.Analytical LCMS: (System B, RT=1.54 min), ES+: 231.4 [MH]+.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Biovitrum AB; US2009/203695; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-methoxy-4-(4-methylpiperazin-l-yl)aniline (331 mg, 1.5 mmol, 1 eq.) and 8-bromo-2-chloroquinazoline (363 mg, 1.5 mmol, 1 eq.) in n-BuOH (10 mL) was added TFA (0.14 mL, 1.8 mmol, 1.2 eq.). The mixture was stirred at 110 C for 12 h. The solution was then cooled to r.t. and concentrated. The resulting residue was dissolved in EA (20 mL), washed with aqueous Na2C03 solution, dried over anhydrous Na2S04and concentrated. The resulting residue was purified via column chromatography (EA/MeOH=5 : 1 , v/v) to afford 8-bromo-N-(2-methoxy-4-(4-methylpiperazin-l-yl)phenyl)quinazolin-2-amine (140 mg, 22% yield)., 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NEUPHARMA, INC.; QIAN, Xiangping; ZHU, Yong-Liang; WO2015/27222; (2015); 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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

5464-12-0, Intermediate H63: ethyl 3-{6-[2-(4-methylpiperazin-1-yl)ethoxy]pyridazin-3-yl}indolizine-2-carboxylate 2-(4-Methylpiperazin-1-yl)ethan-1-ol (0.2676 g, 1.85 mmol) was dissolved in 5.5 ml of THF, potassium tert-butoxide (0.309 g, 2.76 mmol) was added and the mixture was stirred at room temperature for 30 min. Ethyl 3-(6-chloropyridazin-3-yl)indolizine-2-carboxylate 1157 (0.280 g 0.92 mmol) was added and the mixture was stirred at RT for 5 min. The mixture was diluted with ethyl acetate and washed with brine, the phases were separated and the organic layer was dried over sodium sulphate. The solvent was removed and the residue was purified by flash chromatography on Biotage silica-NH cartridge (DCM to DCM_MeOH=98:2) to afford title compound (0.187 g, 0.45 mmol, 49percent yield). MS/ESI+ 410.4 [MH]+, Rt=0.57 min (Method A).

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHIESI FARMACEUTICI S.P.A.; BIAGETTI, Matteo; ACCETTA, Alessandro; CAPELLI, Anna Maria; GUALA, Matilde; RETINI, Michele; US2015/361100; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of N-(4-bromobutyl)phthalimide (5 g, 17.73 mmol) and 1- (2,4-difluoro-phenyl)-piperazine (17.73 mmol) in 2-butanone (100 mL), potassium carbonate (26.6 mmol) and potassium iodide (13.3 mmol) were added. The resulting mixture was heated at 900C overnight. After cooling the solution was filtered and evaporated to dryness. The residue was dissolved in dichloromethane (100 mL) and washed with water. The organic phase was dried over sodium sulphate and evaporated. This material was dissolved in ethanol (100 mL) and hydrazine (2 eq) was added. The solution was refluxed for 4 hours when a thick precipitate formed. Cone. HCl (5 mL) was then added and the mixture heated for a further hour. After cooling the solvent was evaporated and the residue dissolved in 2M HCl (100 mL). This solution was filtered and the aqueous filtrate evaporated again to dryness. The resulting residue was taken in isopropanol (30 mL) and filtered to give the hydrochloride salt of the required product. The salt was converted in the free amine by dissolution in NaOH (15% w/w) and extraction with dichloromethane. (2.6 g, 54%). 1H-NMR (CDCl3) S 1.3 (br s, 2H), 1.46-1.58 (m, 4H), 2.41 (t, 2H), 2.62 (s, 4H), 2.73 (t, 2H), 3.05 (br s, 4H), 6.77-6.83 (m, 2H), 6.87-6.94 (m, IH) (M+l) e/z 270, 115761-79-0

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SIENA BIOTECH S.P.A.; WO2006/8133; (2006); 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.2815-34-1,trans-2,5-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of 2, 2′-Bis [(DIPHENYLPHOSPHINO)-1,’-BINAPHTHYL] (0.068g, 0. 109mmol) and palladium acetate (0.016g, 0. [072MOL)] in toluene (5ml) were heated to [80C.] To this was added the product from example 316, step 1 [(1- [3- (4-IODO-PHENOXY)-PROPYL]-] piperidine) (0.5g, 1. 45mmol) pre-dissolved in toluene (5ml), (2S, 5R)-2, 5-dimethyl- piperazine (0.20g 1. [74MMOL)] predissolved in toluene (5ml), followed by sodium [TERT-] butoxide (0.20g, 2. [02MOL).] The mixture was heated at [100C] for 6 hours. After cooling to room temperature the reaction mixture was diluted with ethyl acetate, washed with water (x3), brine [(X1),] dried over magnesium sulphate and concentrated in vacuo. The residue was purified on silica gel eluting with a mixture of 0.88 ammonia solution : methanol : [DICHLOROMETHANE] (0.5 : 4.5 : 95) to furnish the title compound (0.98g, 20%); MS (ES+) m/e 332 [M+H] [+.]

2815-34-1, The synthetic route of 2815-34-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/35556; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics