Category: piperazines

In 2019,Organic Chemistry Frontiers included an article by Zhang, Fei-Yi; Lan, Xiao-Bing; Xu, Chang; Yao, Hua-Gang; Li, Tian; Liu, Feng-Shou. Formula: C5H12N2. The article was titled 《Rigid hindered N-heterocyclic carbene palladium precatalysts: synthesis, characterization and catalytic amination》. The information in the text is summarized as follows:

To explore the high efficiency of the Buchwald-Hartwig amination with a wide substrate scope, easily prepared and air stable palladium precatalysts bearing rigid hindered N-heterocyclic carbenes (NHCs) were synthesized and characterized. A simple and efficient protocol for the amination of (hetero)aryl chlorides with amines is described, which revealed that sterically encumbered NHC ligands are crucial to promote the transformation. It is highlighted that the most challenging reactions could be performed between less reactive five-membered heteroaryl chlorides and heteroanilines. This methodol. provides a rapid and straightforward access to a wide range of arylated amines with excellent functional group tolerance. Remarkably, the powerful synthetic utility of palladium precatalysts was further extended to the synthesis of pharmaceuticals. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Formula: C5H12N2)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Formula: C5H12N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

《Microwave-Assisted Cu(I)-Catalyzed Synthesis of Unsymmetrical 1,4-Diamino-2-butynes via Cross-A3-Coupling/Decarboxylative A3-Coupling》 was written by Xu, Xianjun; Feng, Huangdi; Van der Eycken, Erik V.. Safety of 1-MethylpiperazineThis research focused onunsym diamino butyne preparation chemoselective microwave irradiation; amine formaldehyde propiolic acid decarboxylative cross coupling copper. The article conveys some information:

1,4-Diamino-2-butynes display both chem. and physiol. properties. Here a highly efficient synthesis avenue to generate unsym. 1,4-diamino-2-butynes has been developed by microwave-assisted Cu(I)-catalyzed cross-A3-coupling/decarboxylative coupling of two different amines, formaldehyde, and propiolic acid through a domino process. This multicomponent reaction provides a series of target products in moderate to good yields with high chemoselectivity. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Safety of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Safety of 1-Methylpiperazine

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Quality Control of 4-Methyl-1-piperazinesulfonyl ChlorideOn November 1, 2019 ,《Photoredox-Catalyzed Generation of Sulfamyl Radicals: Sulfonamidation of Enol Silyl Ether with Chlorosulfonamide》 appeared in Journal of Organic Chemistry. The author of the article were Luo, Qiyu; Mao, Runyu; Zhu, Yan; Wang, Yonghui. The article conveys some information:

A novel and practical photoredox-catalyzed generation of sulfamyl radicals followed by radical sulfonamidation of enol silyl ether has been described. Diverse functionalized β-ketosulfonamides ArCOCH2SO2NRR1 (Ar = 4-MeC6H4, 4-BrC6H4, 2-FC6H4, etc.; R = H, Me, Et, etc.; R1 = H, Me, Et, etc.) were prepared in modest to excellent yields under mild and economic reaction conditions through the present catalytic protocol. Furthermore, the methodol. developed provides an efficient and convenient approach to the synthesis of the antiseizure drug Zonisamide. In the experiment, the researchers used 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Quality Control of 4-Methyl-1-piperazinesulfonyl Chloride)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Quality Control of 4-Methyl-1-piperazinesulfonyl Chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

HPLC of Formula: 109-01-3In 2020 ,《Metal-Free Synthesis of Thermally Stable Fluorescent p-Terphenyls by Ring Transformation of 2H-Pyran-2-ones》 was published in ChemistrySelect. The article was written by Chandrasekar, Subashini; Singh, Fateh V.. The article contains the following contents:

A metal-free approach for the synthesis of p-terphenyls I (Y = piperidin-1-yl, N,N-dimethylamin-1-yl, 4-methylpiperidin-1-yl, etc.) and cyclic p-terphenyls II and III is described via carbanion induced ring transformation reaction of 6-biphenyl-2H-pyran-2-ones IV with malononitrile, cyclohexanone and 1,4-dioxaspiro[4.5]decan-8-one resp. Addnl., the base-mediated ring transformation reactions were working smoothly under mild reaction conditions and ring transformation products I, II and III were isolated in good to excellent yields. The synthetic approach provides the flexibility of introducing of both electron-withdrawing and -donating functionalities in p-terphenyl architecture. Moreover, the photo phys. properties of compounds I, II and III were analyzed using UV-visible and Fluorescence Spectroscopy. The p-Terphenyls I (Y = 4-phenylpiperazin-1-yl) showed cyan fluorescence in chloroform (λmax (em): 508 nm) and acetonitrile (λmax (em): 420 nm) while cyclic p-terphenyl II (Y = 4-phenylpiperazin-1-yl) showed blue fluorescence in chloroform and 1,4-dioxane (λmax (em): 470 nm). Similarly, compound III (Y = 4-phenylpiperazin-1-yl) showed blue fluorescence in chloroform (λmax (em): 468 nm) and 1,4-dioxane (λmax (em): 473 nm). Addnl., the thermal stability of synthesized cyclic p-terphenyls III (Y = 4-methylpiperidin-1-yl, N,N-dipropylamin-1-yl, piperidin-1-yl) were also studied using TG and DTA techniques. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..HPLC of Formula: 109-01-3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The author of 《Novel practical deprotection of N-Boc compounds using fluorinated alcohols》 were Choy, Jason; Jaime-Figueroa, Saul; Jiang, Laurence; Wagner, Paul. And the article was published in Synthetic Communications in 2008. Recommanded Product: 4-(Piperazin-1-yl)-1H-indole The author mentioned the following in the article:

The thermolytic deprotection of N-Boc compounds was accomplished using F3CCH2OH or (F3C)2CHOH as solvents. Even though the cleavage of the tert-butylcarbamate (Boc) group can be achieved at solvent reflux temperature, the deprotection process was significantly accelerated under microwave-assisted conditions. The practicality of this methodol. was demonstrated on alkyl, aryl, and heteroaromatic N-Boc-amines. In the experiment, the researchers used many compounds, for example, 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Recommanded Product: 4-(Piperazin-1-yl)-1H-indole)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 4-(Piperazin-1-yl)-1H-indole

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Application In Synthesis of 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acidOn May 9, 2008 ,《Spectral correlation of high-performance liquid chromatography-diode array detection data from two independent chromatographic runs》 appeared in Journal of Chromatography A. The author of the article were Li, Wei; Hu, Chang-qin. The article conveys some information:

A novel qual. anal. method for peak tracking in impurity profiling control by the correlation of spectra was established. Two-dimensional (2D) standard spectrochromatog. data produced by HPLC with diode array detection (HPLC-DAD) were compared with sample data to develop two-dimensional chromatog. spectral correlative maps. Taking full advantage of separation efficiency of HPLC and spectral specificity of the analytes, the method was successfully used to recognize impurities in quinolone antibacterials, when in combination with relative retention times (RRTs). For the comparison of spectra was expanded to three-dimensional space, simultaneous identification of the chromatog. peaks can be obtained rapidly without preparation and injection of a reference solution, even when the mobile phase changed or the peaks of multi-component samples overlapped. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid(cas: 182868-72-0Application In Synthesis of 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid)

1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid(cas: 182868-72-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Application In Synthesis of 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The author of 《A novel water-soluble perylenetetracarboxylic diimide as a fluorescent pH probe: Chemosensing, biocompatibility and cell imaging》 were Georgiev, Nikolai I.; Said, Awad I.; Toshkova, Reneta A.; Tzoneva, Rumiana D.; Bojinov, Vladimir B.. And the article was published in Dyes and Pigments in 2019. Quality Control of 1-Methylpiperazine The author mentioned the following in the article:

Herein the authors pay attention to the design, synthesis and sensor activity of a novel biocompatible perylene-3,4,9,10-tetracarboxylic diimide (PDI) pH-probe in water. The synthesized compound shows selective fluorescence signaling properties as a function of pH (pKa value of 6.35±0.02) which makes the probe suitable for pH determination in the physiol. range. Thus prepared water soluble fluorescent system demonstrate low cytotoxicity to L929 cell lines from 330 μM to 1.3 μM and cell permeability in the lower concentration range. That findings show the high potential of the newly prepared PDI probe for monitoring of pH variations in bio-samples. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Quality Control of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Quality Control of 1-Methylpiperazine

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

SDS of cas: 84807-09-0On October 1, 2005 ,《Automated Microflow NMR: Routine Analysis of Five-Microliter Samples》 was published in Analytical Chemistry. The article was written by Jansma, Ariane; Chuan, Tiffany; Albrecht, Robert W.; Olson, Dean L.; Peck, Timothy L.; Geierstanger, Bernhard H.. The article contains the following contents:

A microflow CapNMR probe double-tuned for 1H and 13C was installed on a 400-MHz NMR spectrometer and interfaced to an automated liquid handler. Individual samples dissolved in DMSO-d6 are submitted for NMR anal. in vials containing as little as 10 μL of sample. Sets of samples are submitted in a low-volume 384-well plate. Of the 10 μL of sample per well, as with vials, 5 μL is injected into the microflow NMR probe for anal. For quality control of chem. libraries, 1D NMR spectra are acquired under full automation from 384-well plates on as many as 130 compounds within 24 h using 128 scans per spectrum and a sample-to-sample cycle time of ∼11 min. Because of the low volume requirements and high mass sensitivity of the microflow NMR system, 30 nmol of a typical small mol. is sufficient to obtain high-quality, well-resolved, 1D proton or 2D COSY NMR spectra in ∼6 or 20 min of data acquisition time per experiment, resp. Implementation of pulse programs with automated solvent peak identification and suppression allow for reliable data collection, even for samples submitted in fully protonated DMSO. The automated microflow NMR system is controlled and monitored using web-based software. The experimental process involved the reaction of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0SDS of cas: 84807-09-0)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.SDS of cas: 84807-09-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

《Identification of Aminoimidazole and Aminothiazole Derivatives as Src Family Kinase Inhibitors》 was written by Francini, Cinzia Maria; Fallacara, Anna Lucia; Artusi, Roberto; Mennuni, Laura; Calgani, Alessia; Angelucci, Adriano; Schenone, Silvia; Botta, Maurizio. Recommanded Product: 127116-19-2 And the article was included in ChemMedChem in 2015. The article conveys some information:

Src family kinases (SFKs) are a family of non-receptor tyrosine kinases (TKs) implicated in the regulation of many cellular processes. The aberrant activity of these TKs has been associated with the growth and progression of cancer. In particular, c-Src is overexpressed or hyperactivated in a variety of solid tumors and is most likely a strong promoting factor for the development of metastasis. Herein, the synthesis of new 4-aminoimidazole and 2-aminothiazole derivatives and their in vitro biol. evaluation are described for their potential use as SFK inhibitors. Initially, 2-aminothiazole analogs of dasatinib and 4-aminoimidazole derivatives were synthesized and tested against the SFKs Src, Fyn, Lyn, and Yes. Five hits were identified as the most promising compounds, with Ki values in the range of 90-480 nM. A combination of mol. docking, homol. modeling, and mol. dynamics were then used to investigate the possible binding mode of such compounds within the ATP binding site of the SFKs. Finally, the antiproliferative activities of the best candidates were evaluated against SH-SY5Y and K562 cell lines. Compound 3 b [2-(4-{2-methyl-6-[(5-phenylthiazol-2-yl)amino]pyrimidin-4-yl}piperazin-1-yl)ethanol] was found to be the most active inhibitor. After reading the article, we found that the author used 2-(4-(6-Chloro-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol(cas: 127116-19-2Recommanded Product: 127116-19-2)

2-(4-(6-Chloro-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol(cas: 127116-19-2) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Recommanded Product: 127116-19-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

《Anticancer potential of new 3-nitroaryl-6-(N-methyl)piperazin-1,2,4-triazolo[3,4-a]phthalazines targeting voltage-gated K+ channel: Copper-catalyzed one-pot synthesis from 4-chloro-1-phthalazinyl-arylhydrazones》 was written by Romero, Angel H.; Sojo, Felipe; Arvelo, Francisco; Calderon, Christian; Morales, Alvaro; Lopez, Simon E.. Recommanded Product: 1-MethylpiperazineThis research focused ontriazolophthalazine preparation anticancer mol docking potassium channel; 1,2,4-triazolo-phthalazine; Anticancer activity; CH oxidative cyclization; Molecular docking; Nitro-substitution; Potassium-channel. The article conveys some information:

A series of six 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines were prepared through a facile and efficient one-pot copper-catalyzed procedure from 4-chloro-1-phthalazinyl-arylhydrazones with relatively good yields (62-83%). The one-pot copper-catalytic procedure consists of two simultaneous reactions: (i) a direct intramol. dehydrogenative cyclization between ylidenic carbon and adjacent pyrazine nitrogen to form 1,2,4-triazolo ring and, (ii) a direct N-amination on carbon-chlorine bond. Then, an in vitro anticancer evaluation was performed for the synthesized compounds against five selected human cancer cells (A549, MCF-7, SKBr3, PC-3 and HeLa). The nitro-derivatives were significantly more active against cancer strains than against the rest of tested compounds Specifically, compound I was identified as the most promising anticancer agent with significant biol. responses and low relative toxicities on human dermis fibroblast. The cytotoxic effect of compound I was more significant on PC3, MCF-7 and SKBr3 cancer cells with low-micromolar IC50 value ranging from 0.11 to 0.59μM, superior to Adriamycin drug. Mechanistic exptl. and theor. studies demonstrated that compounds I act as a K+ channel inhibitor in cancer models. Further mol. docking studies suggest that the EGFR Tyrosine Kinase enzyme may be a potential target for the most active 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics