Month: October 2022

On February 28, 2007, He, Qiuqin; Liu, Chaomei; Li, Ke; Cao, Yongbing published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-y1)-2-(2,4-difluorophenyl)-3-[(4-substituted)-piperazin-1-y1]-2-propanol. And the article contained the following:

According to the structure of fluconazole, eleven target compounds were designed and synthesized. All of them were confirmed by H-NMR or IR spectra, resp. The MIC80 of all the target compounds were determined by the method recommended by the national committee for clin. laboratory standards (NCCLS) using the RPMI 1640 test medium. Eleven target compounds were firstly reported. The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activities to a certain extent. Most of the target compounds showed higher antifungal activities than that of fluconazole. Especially, compound I showed strong antifungal activity with broad antifungal spectrum and was chosen for further study. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to triazolyl difluorophenyl piperazineyl propanol fluconazole analog synthesis antifungal agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On April 15, 2022, Pawara, Rahul; Ahmad, Iqrar; Nayak, Deepika; Belamkar, Sateesh; Surana, Sanjay; Kundu, Chanakya Nath; Patil, Chandragauda; Patel, Harun published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Design and synthesis of the novel, selective WZ4002 analogue as EGFR-L858R/T790M tyrosine kinase inhibitors for targeted drug therapy in non-small-cell lung cancer (NSCLC). And the article contained the following:

To conquer the drug-resistance of first-generation EGFR (epidermal growth factor receptor) kinase inhibitors and second-generation inhibitors’ non-selective toxicities in Non-Small Cell Lung Cancer (NSCLC) patients, a series of WZ4002 derivatives I [R1 = 4-fluorophenyl, 3,4-dichlorophenyl, 4-bromophenyl, etc.; R2 = 3-CH2=CHC(O)NHC6H4, 4-MeC(O)-N(CH2)2N-C6H4, 3-ClCH2C(O)NHC6H4, etc.] were discovered as novel double mutant EGFR-L858R/T790M TK inhibitors. This objective was attained by employing structure-based drug design and traditional optimization strategies based on the WZ4002 scaffold. Among the synthesized compounds I, representative compounds I [R1 = 4-chloro-3-fluorophenyl, 4-bromophenyl; R2 = 3-CH2=CHC(O)-N(CH2)2N-C6H4] displayed significant anti-proliferative activity on the Gefitinib-resistant cell line NCI-H1975, with an IC50 value of 0.179μM and 0.173μM, resp. Also, these compounds exhibited moderate anti-proliferative activity against the A549 cell, with an IC50 of 0.550μM and 0.528μM resp., suggesting their improved selectivity over the mutant EGFR-L858R/T790M. Excitingly, both these compounds showed significant inhibition of the double mutant EGFR-L858R/T790M TK with an IC50 value of 0.0063μM and 0.0060μM, resp. The IC50 values of both the promising compounds against the HepG2 cell line were more than 1μM, indicating safety for normal cells. Covalent docking and MD simulation further confirm their irreversible binding mode with the target protein. These results demonstrate that compounds I [R1 = 4-chloro-3-fluorophenyl, 4-bromophenyl; R2 = 3-CH2=CHC(O)-N(CH2)2N-C6H4] would be promising lead compound-targeting double mutant EGFR-L858R/T790M TK. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to phenyl amino pyrimidinyl oxy alkenone preparation antitumor sar, tyrosine kinase inhibition mol docking, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On January 1, 2014, Cremonesi, Giuseppe; Dalla Croce, Piero; La Rosa, Concetta published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Lewis acid-catalyzed formylation reaction of 4-(piperazin-1-yl)phenols. And the article contained the following:

The Lewis acid-catalyzed reaction of 4-(piperazin-1-yl)phenols I (R1 = Ac, CHO, Boc, PhCH2; R2 = H) with paraformaldehyde in aprotic solvents afforded salicylaldehydes I (R2 = CHO) in good yields. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to salicylaldehyde piperazinyl preparation, phenol piperazinyl paraformaldehyde formylation lewis acid catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On June 20, 2005, Li, Xianjie; Li, Haibo; Tian, Wanli; Xu, Zheng published an article.Synthetic Route of 67914-60-7 The title of the article was Synthetic technology of 1-acetyl-4-(4-hydroxyphenyl)piperazine. And the article contained the following:

An important intermediate of antifungal drug ketoconazole, 1-acetyl-4-(4-hydroxyphenyl)piperazine [i.e., 1-[4-(4-hydroxyphenyl)-1-piperazinyl]ethanone], was synthesized from piperazine-6H2O and p-chloronitrobenzene by substitution, N- acetylation with acetic anhydride, reduction with Ni/hydrazine, diazotization, and hydrolysis in the presence of Cu/Cu(NO3)2, and its possibility of com. use was studied. The compound was obtained with yield excelled present route. The route may be used in com. production (no data). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Synthetic Route of 67914-60-7

The Article related to acetyl hydroxyphenyl piperazine synthesis, ketoconazole intermediate hydroxyphenyl piperazinyl ethanone preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Synthetic Route of 67914-60-7

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

On April 11, 2013, Letavic, Michael A.; Lord, Brian; Bischoff, Francois; Hawryluk, Natalie A.; Pieters, Serge; Rech, Jason C.; Sales, Zachary; Velter, Adriana I.; Ao, Hong; Bonaventure, Pascal; Contreras, Victor; Jiang, Xiaohui; Morton, Kirsten L.; Scott, Brian; Wang, Qi; Wickenden, Alan D.; Carruthers, Nicholas I.; Bhattacharya, Anindya published an article.Related Products of 1428327-31-4 The title of the article was Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists. And the article contained the following:

The synthesis and preclin. characterization of two novel, brain penetrating P2X7 compounds will be described. Both compounds are shown to be high potency P2X7 antagonists in human, rat, and mouse cell lines and both were shown to have high brain concentrations and robust receptor occupancy in rat. Compound I is of particular interest as a probe compound for the preclin. assessment of P2X7 blockade in animal models of neuro-inflammation. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Related Products of 1428327-31-4

The Article related to brain penetrating p2x7 antagonist nicotinamide isoquinolinecarboxamide derivative, p2x7, depression, neuro-inflammation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1428327-31-4

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

On April 30, 2009, Barlaam, Bernard Christophe; Bower, Justin Fairfield; Delouvrie, Benedicte; Fairley, Gary; Harris, Craig Steven; Lambert, Christine; Ouvry, Gilles; Winter, Jon James Gordon published a patent.Related Products of 1211568-27-2 The title of the patent was Pyridine and pyrazine derivatives as Axl and/or c-Met receptor enzyme inhibitors and their preparation, pharmaceutical compositions and use in the treatment of tumors. And the patent contained the following:

The invention concerns pyridine a nd pyrazine derivatives of formula I or a pharmaceutically-acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of tumors. Compounds of formula I wherein W is CH and N; J is O and S; each G1, G2, G3 and G4 is CH and N, proved that no more than two of G1,G2, G3 and R4 is N; A is (un)substituted Ph, (un)substituted 5- to 6-membered monocyclic heteroaryl; and (un)substituted 8- to 10-membered bicyclic ring; each R3 is independently H, halo, CN, amino, sulfamoyl, CF3, C1-8 alkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 2-aminophenol with 2-amino-5-bromopyridine-3-carboxylic acid; the resulting 3-(benzoxazol-2-yl)-5-bromopyridin-2-amine underwent cross-coupling with 4-(dimethylaminomethyl)phenylboronic acid to give compound II. All the invention compounds were evaluated for their Axl and c-Met receptor tyrosine kinase inhibitory activity. From the Axl tyrosine kinase assay, it was determined that compound II exhibited 99.8 % inhibition at 1 μM concentration The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to pyridine preparation axl cmet tyrosine kinase inhibitor treatment tumor, pyrazine preparation axl cmet tyrosine kinase inhibitor treatment tumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

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

On June 30, 2007, He, Qiu Qin; Li, Ke; Cao, Yong Bing; Dong, Huan Wen; Zhao, Li Hua; Liu, Chao Mei; Sheng, Chun Quan published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Design, synthesis and molecular docking studies of novel triazole antifungal compounds. And the article contained the following:

Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized. In vitro antifungal activities showed that compounds I (R = R1 = Me; R = CMe3, CN, NO2, R1 = H) exhibited strong activities. In addition, the first three also displayed certain activities against fluconazole-resistant fungi. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to triazolylpropanol benzylpiperazinylphenoxy derivative preparation antifungal activity, mol docking triazolylpropanol derivative lanosterol demethylase, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On September 17, 1998, Tanoury, Gerald J.; Senanayake, Chris H.; Hett, Robert; Kuhn, Amy M.; Kessler, Donald W.; Wald, Stephen A. published an article.Electric Literature of 67914-60-7 The title of the article was Pd-catalyzed aminations of aryltriazolones: effective synthesis of hydroxyitraconazole enantiomers. And the article contained the following:

A palladium-catalyzed amination of triazolone I by piperazine II was used as the key step in an efficient synthesis of highly enantiomerically pure hydroxyitraconazole (III). II (>99% ee) was prepared by reaction of an achiral phenol precursor with the corresponding dioxolyl tosylate (>99% ee). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Electric Literature of 67914-60-7

The Article related to hydroxyitraconazole asym preparation, amination aryltriazolone palladium, triazolone aryl amination palladium, heck coupling vs palladium catalyzed amination, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 67914-60-7

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

On December 31, 1990, Chapman, David R.; Bauer, Ludwig; Waller, Donald P.; Zaneveld, Lourens J. D. published an article.Recommanded Product: 67914-60-7 The title of the article was Synthesis of diastereomeric ketoconazole analogs. And the article contained the following:

Syntheses of trans-isomers of ketoconazole (I) and the corresponding des-acetyl, 1-Me, 1-formyl and 1-methanesulfonyl analogs were investigated. These isomers, along with the corresponding cis-diastereomers were characterized by their carbon-13 NMR spectra. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 67914-60-7

The Article related to ketoconazole diastereomer, imidazolylmethyldioxolanylmethoxyphenylpiperazine, piperazinophenol imidazolylmethyldioxolanylmethanesulfonate reaction, nmr ketoconazole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 67914-60-7

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

On June 30, 2005, Liu, Yong; Wang, Jingkang; Yin, Qiuxiang published an article.Electric Literature of 86393-32-0 The title of the article was Determination of the space group for ciprofloxacin hydrochloride monohydrate crystals. And the article contained the following:

Ciprofloxacin hydrochloride monohydrate (CPFX) crystals were obtained exptl. The deaquation, melting, decomposing apex temperatures and water content of ciprofloxacin hydrochloride monohydrate crystals were measured by DSC and TG techniques resp. The data of X-ray powder diffraction (XRPD) of these crystals were collected exptl. The indexing results by the software Cerius2 were obtained. The results showed that the crystal of ciprofloxacin hydrochloride monohydrate belonged to monoclinic, and the unit cell parameters a, b, c and β were 12.93×10-10 m, 19.56×10-10 m, 7.07×10-10 m, and 91.10° resp. Based on the indexing results and the extinction principle, the space group for ciprofloxacin hydrochloride monohydrate crystals produced in crystallization experiment was P21/c. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Electric Literature of 86393-32-0

The Article related to ciprofloxacin hydrochloride monohydrate x ray powder diffraction space group, unit cell parameter, Crystallography and Liquid Crystals: Crystallographic Methods and Apparatus For Structure Determination and other aspects.Electric Literature of 86393-32-0

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