Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Method 1 1-(t-Butoxycarbonyl)-3-methylpiperazine To a cold (-5 C.) solution of 2-methylpiperazine (5.00 g, 0.05 mole) in 200 mL of CH2 Cl2 under Ar was added a solution of di-t-butyl dicarbonate (10.9 g, 0.05 mole) in 100 mL of CH2 Cl2 over 1 h. The resulting mixture was stirred at -5 C. for 1 h and then at r.t. for 2 h. The solution was then washed (H2 O), dried (Na2 SO4) and evaporated to give an oil which was chromatographed (SiO2 /ethyl acetate then ethyl acetate-MeOH-NH4 OH 10:1:0.1) to give the product (4.30 g, 43%) as an oil. This material was used without further purification: 1 H nmr (200 MHz, CDCl3) delta4.15-3.75 (br s, 2H), 3.0-2.6 (m, 4H), 2.47-2.35 (m, 1H), 1.48 (s, 9H), 1.08 (d, J=6.7 Hz, 3H)., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; Bristol-Myers Squibb Company; US5300506; (1994); A;,
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

A reaction mixture of 8 (0.235 g, 1.0 mmol), l-(2,4-difluorophenyl)piperazine (0.208 g, 1.1 mmol), Pd(OAc)2 (28.8 mg, 0.13 mmol), BINAP (0.135 g, 0.22 mmol), and CS2CO3 (0.427 g, 1.3 mol) in dry toluene (5 mL) was stirred at 50 C for 48 h. After cooling, the palladium catalyst was removed by filtration through Celite pad. The product mixture was diluted with ethyl acetate (50 mL) and washed with aqueous NaHCCte (10 mL x 2) and brine (10 mL x 2). The organic layer was dried over magnesium sulfate, filtered, and concentrated in vacuo. The resulting product was purified by flash chromatography to yield 9 as a white solid (0.252 g, 0.72 mmol, 72%); Rf = 0.36 (20% ethyl acetate in hexane). NMR (400 MHz, CDCb) delta 7.83 (t, J = 8.8 Hz, 1H), 6.95 – 6.87 (m, 1H), 6.86 – 6.76 (m, 2H), 6.65 (dd, J = 9.0, 2.5 Hz, 1H), 6.54 (dd, J = 14.6, 2.5 Hz, 1H), 3.86 (s, 3H), 3.49 – 3.41 (m, 4H), 3.13 (dd, J = 6.2, 4.0 Hz, 4H). 13C NMR (101 MHz, CDCb) delta 165.09, 164.93, 164.89, 162.53, 159.53, 159.42, 157.1 1, 157.06, 157.00, 156.95, 155.53, 155.42, 154.59, 154.47, 136.30, 136.26, 136.21, 136.17, 133.44, 133.41, 119.80, 1 19.76, 1 19.71, 119.67, 1 1 1.02, 1 10.99, 1 10.81, 1 10.78, 109.50, 109.48, 107.70, 107.60, 105.16, 104.92, 104.90, 104.66, 101.75, 101.48, 77.16, 51.84, 50.60, 50.57, 47.43. MS (ESI) m/z 351 [M+H]+., 115761-79-0

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

Reference£º
Patent; THE SCRIPPS RESEARCH INSTITUTE; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; ROUSH, William R.; CHOI, Jun Yong; PODUST, Larissa; WO2015/48306; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7-Cyclopentyl-2-(5-formyl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide (1 mol. eq.) and amine (1-2 mol. eq.) are dissolved in either dichloroethane/THF (3:1) or MeOH/dichloromethane mixtures (40 vols.). The mixture is stirred at 20-40C for 16 hours, then cooled to 0C, NaCNBH3 or NaBH4(l .5 – 2 mol. eq.) are then added and the mixture stirred at rt for 5h. Where necessary, further MeOH and/or acetic acid is added to aid reaction progress. The mixture is then quenched with aqueous NaHCO3 solution (10ml) and the product extracted with either diethyl ether, dichloromethane or CHCl3/iPrOH (1 :1). The combined organics are dried (MgStheta4), filtered and the solvent evaporated. The crude product is purified by SiO2 chromatography

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVARTIS AG; ASTEX THERAPEUTICS LTD.; BESONG, Gilbert; BRAIN, Christopher Thomas; BROOKS, Clinton A.; CONGREVE, Miles Stuart; DAGOSTIN, Claudio; HE, Guo; HOU, Ying; HOWARD, Steven; LI, Yue; LU, Yipin; MORTENSON, Paul; SMITH, Troy; SUNG, Moo; WOODHEAD, Steven; WRONA, Wojciech; WO2010/20675; (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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

To a cooled solution of imidazole at 000 (1.00 g, 14.7 mmol, 2equiv) in 0H2012 (18 mL),benzyl chloroformate (1.03 mL, 7.35 mmol, 1 equiv) was slowly added. After 1h45 ofstirring the white solid (imidazole hydrochloride) was filtered off. The obtained filtrate wasconcentrated, and then solubilised in ethanol (17.5 mL). In another flask the solution ofpiperazine dihydrochloride (1.75 g, 11.03 mmol, 1.5 equiv) in water (17.5 mL) wasprepared, then added dropwisely to ethanolic solution of Cbz-imidazole. The resultedmixture was stirred for 4h30 at room temperature and then concentrated to 1h of itsvolume. Obtained aqueous phase was extracted with chloroform (4x) to remove the diacylated product, then NaOHsat was added to the previous aqueous phase (pH 9-10).The resulted aqueous phase was extracted again with chloroform (4x) to recover the monoacylated product. The organic phase with monoacylated product was washed with water (4x), dried over MgSO4 and concentrated to give (1) (0.809 g, 50% in two steps) asa colorless oil

142-64-3, As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference£º
Patent; CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE; UNIVERSITE D’ORLEANS; AGROFOGLIO, Luigi; ROY, Vincent; PLEBANEK, Elzbieta; BESSIERES, Maxime; (105 pag.)WO2018/50771; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Racemic ulifloxacin (105 g) was dissolved in DMSO (1500 mL). L-tartrate (27 g) solution in DMSO (405 mL) was added to the racemic ulifoxacin solution with agitation. Cloudiness and precipitation appear. After 20 hours of agitation at an ambient temperature, the mixture was filtered and dried under vacuum to yield 82 g of solid. The solid was recrystallized in DMSO to yield 34 g of (R)- 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a] quinoline-3-carboxylic acid-L-tartrate salt. The salt was dispersed in water and the dispersion was neutralized with 2% NaOH aqueous solution to a pH value of 7 to 8. The precipitate was filtered and dried to yield 22 g of (R) -6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid. It has specific rotation [Show Image] (c=0.15, 0.1mol/L NaOH), optical purity e.e>95%., 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Guangzhou Baiyunshan Pharmaceutical Co. Ltd. Guangzhou Baiyunshan Pharmaceutica Factory; Guangzhou Pharmaceutical Industry Academe; EP2258705; (2010); 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 n-butanol (2 mL) was added compound 4A-3 (30 mg, 0.135 mmol) and compound 5A-3 (48 mg, 0.135mmol), and then p-toluenesulfonic acid (23 mg, 0.132 mmol) was added under stirring. The mixture was heated to 100C and stirred for 5 hours. After TLC indicated the reaction was completed, the reaction mixture was concentrated under reduced pressure to give a crude product, which was further purified and isolated by column chromatography to obtain an off-white solid product, compound I-2 (25 mg, yield 34.3%). 1H NMR (400 MHz, cd3od) delta 8.11 (s, 1H), 8.05 (s, 1H), 7.81 (d, J=5.5 Hz, 1H), 7.57 (d, J=8.6 Hz, 1H), 6.68 (d, J=2.3 Hz, 1H), 6.57 (dd, J=8.7, 2.4 Hz, 1H), 3.83 (s, 3H), 3.42-3.34 (m, 1H), 3.29 (s, 4H), 2.89 (s, 4H), 2.55 (s, 3H), 1.30 (d, J=6.7 Hz, 6H). LCMS: t=0.690 min, 537.2 (M), 538.2 (M+1).

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

Reference£º
Patent; Humanwell Healthcare (Group) Co., Ltd.; WANG, Xuehai; XU, Yong; SHENG, Xijun; ZHANG, Xiaolin; XIA, Hangui; YANG, Zhongwen; YUE, Yang; HUANG, Lu; XIAO, Qiang; (80 pag.)EP3372594; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-82-4, A suspension of 23 (0.10 g, 0.33 mmol), 4-(4-methyl-piperazin- 1-ylmethyl)- phenylamine (0.10 g, 0.49 mmol), Pd2(dba)3 (25 mg, 0.027 mmol), Xantphos (32 mg, 0.055 mmol) and cesium carbonate (0.22 g, 0.68 mmol) in dioxane (4 mL) was sealed in a microwave reaction tube and irradiated with microwave at 160 0C for 20 min. After cooling to room temperature, the resulting mixture was filtered and the filtered solid washed with DCM. The filtrate was concentrated and the residue purified by HPLC. The fractions were combined and poured into saturated NaHCO3 solution (25 mL). The combined aqueous layers were extracted with EtOAc (2 x 25 mL) and the combined organic layers washed with brine, dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated and the residue re- dissolved in minimum amount of EtOAc and hexanes added until solid precipitated. After filtration, the title compound was obtained as a yellow solid (10 g, 6%).[0204] 1H NMR (500 MHz, DMSO-d6): delta 2.18 (s, 3H), 2.25-2.45 (m, 8H), 2.46 (s, 3H), 3.41 (s, 2H), 7.00 (dd, J = 3.6, 1.7 Hz, IH), 7.21 (d, J = 8.5 Hz, 2H), 7.29 (dd, J= 8.4, 1.3 Hz, IH), 7.38 (dd, J = 3.6, 2.3 Hz, IH), 7.81 (s, IH), 7.87 (d, J= 8.5 Hz, 2H), 7.94 (d, J= 8.3 Hz, IH), 8.39 (s, IH), 9.27 (s, IH), 11.7 (s, IH) MS (ES+): m/z 469 (M+H)+

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference£º
Patent; TARGEGEN INC.; WO2009/49028; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Chloro derivative (1 mol), amine (1 mol) and K2CO3 (2mol) were taken in DMF (10 v). The reaction mixture washeated to 100 C, stirred for 16 h. Then the reaction mixturewas cooled to room temperature, diluted with water (50 v) extracted with EtOAC (2 x 50 v). Combined organic layerswere dried over anhydrous sodium sulphate, evaporated thesolvent in vacuo. Crude products were purified by columnchromatography., 118753-66-5

118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Kasturi, Sivaprasad; Surarapu, Sujatha; Uppalanchi, Srinivas; Anantaraju, Hasitha Shilpa; Dwivedi, Shubham; Yogeeswari, Perumal; Ethiraj, Krishna S.; Anireddy, Jaya Shree; Letters in drug design and discovery; vol. 15; 2; (2018); p. 181 – 192;,
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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

EXAMPLE-6 2-Cyano-1-(4-isopropyl-2-piperazinyl)-carbonyl Pyrrolidine Trifluoroacetate (Compound No.2). Step-1 To an aqueous (100 ml) sodium hydroxide (4.0 g, 100 mmol) solution of piperazine-2-carboxylic acid dihydrochloride (5 g, 24.63 mmol) is added a solution of di-tert-butyl dicarbonate (11.0 g, 50.45 mmol) in dioxan (50 ml) at 0 C. over a period of half an hour. The reaction mixture is stirred at 0 C. for 1 hr. followed by stirring at room temperature (25 C.) for another 2 hrs. Neutralized (pH 6-7) with aqueous 2N HCl, extracted with ethyl acetate. Organic layer washed with brine solution, dried (Na2SO4) and evaporated in vacuo to yield an oil which solidifies on cooling. (Yield 8.02 g, 98.76%).

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TORRENT PHARMACEUTICALS LTD.; US2004/106802; (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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

Step-2: To a stirred solution of product from step-1 (0.18 g) in DMF (4 ml) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (0.180 g, 0.6861 mmol) at RT and the reaction mixture was heated at 110 C. for 1 h. The reaction mixture was cooled to RT and stirred with triethyl amine (1 ml) for half an hour. The reaction mixture was evaporated and the crude product was purified by column chromatography using 0 to 10% methanol in dichloromethane as eluent to afford (Z)-methyl 1-acetyl-3-((4-(N-methyl-2-(4-methylpiperazin-1-yl) acetamido)phenylamino)(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-6-carboxylate as yellow solid. MS (ES+): m/z 583.4 (MH+)., 262368-30-9

The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ANGION BIOMEDICA CORP.; PANICKER, Bijoy; MISHRA, Rama K.; LIM, Dong Sung; OEHLEN, Lambertus J.W.M.; JUNG, Dawoon; US2015/306078; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics