Month: November 2020

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.

1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.05 mmol), (4-fluorophenyl)boronic acid (575 mg, 4.11 mmol), copper(II) acetate (372 mg, 2.05 mmol) and pyridine (0.33 ml, 4.09 mmol) were suspended in anhydrous DCM (10 ml) with 4A molecular sieves (500 mg). The mixture was stirred for 16 hours at ambient temperature, then for 5 hours at 35 C. Air was bubbled through the mixture for 10 min, then it was stirred for 18 hours at ambient temperature. Air was bubbled through the mixture for 10 min, then it was stirred at 35 C. for 6 hours and at ambient temperature for 72 hours. Additional (4-fluorophenyl)boronic acid (286 mg, 2.05 mmol) was added and the reaction was stirred for 4 hours at 35 C. The reaction was cooled to ambient temperature and filtered through celite. The filtrate was partitioned with sat. aq. NaHCO3 (20 ml). The organic layer was separated and the aqueous extracted with DCM (2¡Á20 ml). The organics were combined and concentrated in vacuo to give a green oil. The oil was purified via flash column chromatography using a gradient of 0-50% EtOAc in heptane. The product containing fractions were combined and concentrated in vacuo to afford the title compound as a yellow oil (213 mg, 26%). 1H NMR (250 MHz, Chloroform-d) delta 7.01-6.90 (m, 2H), 6.87-6.78 (m, 2H), 4.47 (d, J=13.4 Hz, 1H), 4.32-4.22 (m, 1H), 4.09 (s, 1H), 3.63 (s, 3H), 3.59-3.46 (m, 1H), 3.37 (dd, J=13.3, 4.2 Hz, 1H), 3.28-3.00 (m, 2H), 1.46 (s, 9H). LCMS Method 3-Tr=1.90 min, (ES+) (M+H+) 339.2.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (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.154590-34-8,tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation 10 :; 4- (4-Amino-2-fluoro-phenyl)-piperazine-l-carboxylic acid tert-butyl ester:; To a solution of 4-(2-fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert- butyl ester (9.00 grams, 27.7 mmol), obtained in preparation 7, in methanol and THF (4: 1,140 mL) was added ammonium formate (6.98 grams, 111 mmol) followed by the addition of 10% Pd-C (1.47 grams, 13.8 mmol) and stirred at 25-35 C for 5 hours. The reaction mixture was filtered through a pad of celite and washed thoroughly with methanol. Removal of volatiles left a pasty mass, which was diluted with water and extracted with ethyl acetate (150 mL x 3). The combined organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of solvent produced the title amine (7.75 grams, 95%). ‘H NMR (CDC13) : 8 6.78 (t, J= 9.1 Hz, 1H), 6.47-6. 38 (m, 2H), 3.57 (t, J= 4.8 Hz, 4H), 2.90 (t, J= 4.8 Hz, 4H), 1. 48 (s, 9H), IR (KBr, cm-1) : 3451,3347, 1681. CI-MS (m/z) : 296 (M++1), 282,240, 196.153, 106,96.

154590-34-8, The synthetic route of 154590-34-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DR. REDDY’S LABORATORIES LTD.; WO2005/82892; (2005); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.,122833-04-9

10208] Step 1. To a mixture of 2-methoxy-4-(4-methylpip- erazin-1-yl)aniline (Combi-l3locks mc, Cat: SS-3744; 342 mg, 1.55 mmol) and tert-butyl (3-(2-(methylsulfinyl)-7-ox- opyrido[2,3-d]pyrimidin-8(7H)-yl)phenyl)carbamate (52) (521 mg, 1.30 mmol)intert-butanol(lOmL, 105 mmol) was added DIEA (0.57 mE, 3.25 mmol). The reactionmixture was heated at 800 C. in an oil bath for 21 h. The resulting brown suspension was concentrated under reduced pressure and the crude solid was suspended in Et20 (ca. 20 mE) and filtered affording the crude material of tert-butyl (3-(2-((2-methoxy- 4-(4-methylpiperazin-1 -yl)phenyl)amino)-7-oxopyrido[2,3- d]pyrimidin-8(7H)-yl)phenyl)carbamate (la) as a green solid. mlz (ESI, +ve ion) 558.0 (M+H). ?H NMR (400 MHz, DMSO-d5) oe ppm 9.57 (1H, s), 8.73 (1H, s), 8.14 (1H, s), 7.89 (1H, d, J9.4 Hz), 7.57 (1H, d, J8.4 Hz), 7.42 (3H, t, J8.0Hz), 7.28 (1H, d, J8.8 Hz), 6.87 (1H, d, J8.6 Hz), 6.53 (1H, d, J2.3 Hz), 6.43 (1H, d, J9.4 Hz), 6.05 (1H, br. s.), 3.73- 3.82 (3H, m), 3.06 (4H, br. s.), 2.36-2.47 (4H, 2.15-2.26 (3H, s), 1.45 (9H, s).

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TASKER, Andrew; WURZ, Ryan; PETTUS, Liping H.; HERBERICH, Bradley J.; US2014/249131; (2014); 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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

3 mmol of piperazine dihydrochloride hydrate was added of 10 mL of CH3CN, TEA (6 mmol) and 2-chloro-3-nitropyridine (1 mmol). After 2 h, at reflux, the mixture was evaporated under reduced pressure and the residue was treated with H2O (5mL) and ethylacetate (5 mL). The aqueous phase was separated and extracted twice with ethylacetate (2¡Á5 mL). The combined organic phases were dried on Na2SO4, filtered and evaporated under reduced pressure. The crude residue was purified by silica gel column chromatography, using dichloromethane/methanol (9:1) as eluent. Yield 62%, as yellow solid. 1H NMR (DMSO-d6): 8.44 (dd, 1H, J=4.5 Hz, J=1.6 Hz), 8.29 (dd, 1H, J=8.1 Hz, J=1.6 Hz), 6.94 (dd, 1H, J=8.1 Hz, J=4.5 Hz), 3.56 (m, 4H), 2.80 (m, 4H)., 142-64-3

The synthetic route of 142-64-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Moraca, Francesca; De Vita, Daniela; Pandolfi, Fabiana; Di Santo, Roberto; Costi, Roberta; Cirilli, Roberto; D’Auria, Felicia Diodata; Panella, Simona; Palamara, Anna Teresa; Simonetti, Giovanna; Botta, Maurizio; Scipione, Luigi; European Journal of Medicinal Chemistry; vol. 83; (2014); p. 665 – 673;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of 3-(4-methylpiperazin-1-yl)-propan-1-ol: 1-Methylpiperazine (6.99 mL, 63 mol) was dissolved in toluene (30 mL). 3-Bromopropanol (2.62 mL, 30 mmol) was added slowly and the mixture was stirred overnight at r.t. After heating to 80 C. for 2 h and cooling to r.t., the mixture was filtered and the filter cake was thoroughly washed with toluene. After removal of the solvent, the residue was subjected to Kugelrohr distillation (b.p., 180 C./2 mbar) to obtain a colourless oil (4.08 g, 25.8 mmol, 86%). LC/ESI-MS: m/z=159 [M+H]., 109-01-3

As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Patent; 4SC AG; US2007/21446; (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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of l-fluoro-4-nitrobenzene (4.23 g, 30 mmol, 1.0 eq.) in DMSO (40 mL) was added TEA (9.1 g, 90 mmol, 3.0 eq.) followed by 2-(piperazin-l-yl)ethanol (3.9 g, 30 mmol, 1.0 eq.) and the mixture was stirred at 90 C overnight. The mixture was poured into ice-water (400 mL), filtered and dried in vacum to afford 2-(4-(4-nitrophenyl)piperazin- l-yl)ethanol as a yellow solid (7.2 g, 95.6%)., 103-76-4

As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference£º
Patent; NEUPHARMA, INC.; QIAN, Xiangping; ZHU, Yong-Liang; WO2015/27222; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 5 (0.16g, 0.77mmol), H2O (0.4ml) and AcOH (1.6ml) was mixed with the 84 (0.22g, 1.00mmol) and then refluxed for overnight. The reaction was quenched by saturated NaHCO3 (aq.) and the mixture was extracted by ethyl acetate (30ml x 3). The residue was purified by flash column over silica gel (dichloromethane: methanol = 9: 1, Rf = 0.35) to afford 88 (0.22g, 73.54%) as a pale yellow solid. 1H-NMR (500MHz, CDCl3): 5 1.16 (t, J= 7.5 Hz, 3H), 2.52 (q, J= 7.5 Hz, 2H), 2.66 (t, J= 5.0 Hz, 4H), 2.88 (d, J= 5.0 Hz, 3H), 3.25 (t, J= 5.0 Hz, 4H), 4.84 (s, 1H), 5.51 (s, 1H), 6.51 (s, 1H), 6.95 (d, J= 8.5 Hz, 2H), 7.23 (d, J= 8.5 Hz, 2H), 7.42-7.43 (m, 3H), 8.31-8.33 (m, 2H).

115619-01-7, As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

Reference£º
Patent; TAIPEI MEDICAL UNIVERSITY; YEN, Yun; LIOU, Jing-Ping; CHEN, Chun-Han; (70 pag.)WO2017/15400; (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.300543-56-0,(R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

Example 2a) [2- [4- [ (4-chlorophenyl)phenylmethyl] -1-piperazinil] ethoxy] – acetonitrile dihydrochlorideCharge 2400 mL of acetonitrile to the reaction vessel, add 400 g of (-) -1- [ (4-chlorophenyl) phenylmethyl ] -4-piperazine, 300 g Na2CO3, 20 g KI and 300 g of 2- (2-chloroethoxy) acetonitrile in turn under stirring.Stir and gradually raise the temperature to 110-115 0C. Keep the temperature for 20 hours, after the reaction is completed, cool the mixture to 80-90 0C and add 25 g of activated carbon and stir for 20 minutes. Filter off carbon and wash cake with appropriate amount of acetonitrile. Into combined filtrate in? troduce dry HCl gas until pH value reaches 0.5-1. Continue to stir the slurry for 20 minutes and filter. Wash the cake with appropriate amount of ethanol and dry at 50-550C for 10 hours to obtain 520 g of the title product.The yield 95%, HPLC (area) 95 %. The obtained [2- [4- [(4- chlorophenyl) phenylmethyl] -1-piperazinyl] ethoxy] -acetonitrile dihydrochloride has in the X-ray powder diffractogram the peaks at about: 8.5; 18.5; 19.1; 22.7; 24.9; 25.7; 25.9 in 28.7 +/- 0.2 2Theta.b) Maceration of a crude [2- [4- [ (4-chlorophenyl)phenylmethyl] – 1-piperazinyl] ethoxy] -acetonitrile dihydrochloride10 g of [2- [4- [ (4-chlorophenyl) phenylmethyl] -1-piperazinyl] ethoxy] -acetonitrile dihydrochloride were suspended in 30 mL of methanol. The suspension was heated to the boiling tempera? ture and stirred at this temperature for at least 20 minutes. Thereafter the suspension was cooled to 0 0C and stirred at this temperature for one hour. The precipitate was filtered, washed with cold methanol and dried. HPLC (area) 98 %., 300543-56-0

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

Reference£º
Patent; KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO; WO2008/110586; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55112-42-0, 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55112-42-0, Step 1: Preparation of racemic Zopiclone (I) Example- 1To a mixture of 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine (100 g), DBU (173.9 g), pyridine (90.25 g) and dichloromethane (1000 ml), 1- chlorocarbonyl-4-methylpiperazine hydrochloride (151.56 g) was added and stirred for 5 hours at 20-25 C. On completion of the reaction, chilled water (1000 ml) was added to it to form a biphasic mixture and the organic phase was extracted. The aqueous phase was further extracted with dichloromethane (1000 ml). The organic phases were combined, washed with water (5 x 1000 ml) and evaporated under vacuum. The resultant solid residue was dissolved in acetonitrile (500 ml), charcoalized with activated carbon (5 gms), filtered on celite bed and washed with acetonitrile (2 x 50 ml). The filtrate and the acetonitrile washings were combined, cooled, stirred for 2 hours at 5 – 10C, filtered and dried to obtain zopiclone. (Yield: 81%; Purity: 99.65% by HPLC).

55112-42-0 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride 3016934, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; LUPIN LIMITED; WO2009/101634; (2009); 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.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: 2,5-Dihydroxybenzaldehyde (1.0 eq.) and cesium carbonate (1.0 eq.) were suspended in DMF and the suspension, warmed to 60 ¡ãC for 15 min. After cooling down to rt, the corresponding bromide (1.1 eq.) was added in DMF (0.5 M concentration of 2,5-dihydroxybenzaldehyde) and the reaction was stirred at rt for 2h for benzylic haloalkanes or at 60 ¡ãC overnight for aliphatic haloalkanes. The solvents were evaporated and the crude dissolved in water and ethyl acetate. The aqueous phase was extracted with ethyl acetate (3x) and the combined organic layers were dried over magnesium sulfate, filtered and the solvent evaporated. The crude product was purified by flash chromatography., 655225-01-7

655225-01-7 tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate 15946441, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Hernandez-Olmos, Victor; Knape, Tilo; Heering, Jan; von Knethen, Andreas; Kilu, Whitney; Kaiser, Astrid; Wurglics, Mario; Helmstaedter, Moritz; Merk, Daniel; Schubert-Zsilavecz, Manfred; Parnham, Michael J.; Steinhilber, Dieter; Proschak, Ewgenij; Bioorganic and Medicinal Chemistry; vol. 27; 21; (2019);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics