Month: October 2022

On November 9, 2021, Qin, Chong; Chen, Yiming; Zhong, Tengjiang; Zhang, Sai; Ge, Ling published a patent.Synthetic Route of 1211568-27-2 The title of the patent was High-efficiency androgen receptor modulator and its application. And the patent contained the following:

A high-efficiency androgen receptor modulator (e.g., I) having wide application in field of pharmaceuticals is provided. The androgen receptor (AR) modulator contains the E3 ubiquitin ligase ligand combined with an androgen receptor (AR) modulator. The androgen receptor (AR) modulators and their pharmaceutical composition are used in preparation of antiandrogen drugs. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Synthetic Route of 1211568-27-2

The Article related to heterocyclyl androgen receptor modulator antitumor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Synthetic Route of 1211568-27-2

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

On April 30, 2007, He, Qiu Qin; Liu, Chao Mei; Li, Ke; Cao, Yong Bing published an article.Category: piperazines The title of the article was Design, synthesis of novel antifungal triazole derivatives with high activities against Aspergillus fumigatus. And the article contained the following:

Based on the active site of Aspergillus fumigatus lanosterol 14α-demethylase (AF-CYP51), novel triazole compounds I (R = aryl) were designed. Their chem. synthesis and the antifungal activities were reported. The results showed that all the target compounds exhibited excellent activities with broad spectrum, in which I (R = 4-FC6H4, 4-H2NCOC6H4, pyridin-4-yl) showed comparable activities against A. fumigatus to the control drug Itraconazole. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Category: piperazines

The Article related to piperazinyl triazole preparation antifungal aspergillus fumigatus, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: piperazines

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

On July 29, 2022, Zhang, Chen; Wang, Jianmin; Qian, Guofei; Huang, Zhenggang; Tang, Pingming; Ye, Fei; Li, Yao; Ni, Jia; Yan, Pangke published a patent.Application of 1211568-27-2 The title of the patent was Preparation of a bifunctional molecule with EGFR degradation as antitumor agent. And the patent contained the following:

The present invention discloses a preparation of a bifunctional mol. with EGFR degradation as antitumor agent, which can be used to prepare drugs for treating diseases related to EGFR activity. The invention compound was prepared via the reaction of benzyl piperazine-1-carboxylate and tert-Bu 3-oxoazetidine-1-carboxylate, followed by deprotection, condensation, reduction reaction and substitution reaction. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Application of 1211568-27-2

The Article related to preparation egfr degradation antitumor agent condensation suzuki coupling, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 1211568-27-2

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

On October 22, 2020, Du, Wu; Wen, Kun; Fu, Yiwei; Lv, Haibin; He, Jinyun; Qin, Dekun; Li, Yu; Duan, Jingyi; Li, Yong; Ai, Chaowu; Tu, Zhilin; Chen, Yuanwei; Li, Xinghai published a patent.HPLC of Formula: 1211568-27-2 The title of the patent was A class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and application. And the patent contained the following:

The invention disclosed a class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and application. The claimed compound is shown in structure ARB-L-U (ARB = androgen receptor recognition/binding part; L = linker part; U = ubiquitin protease recognition/binding part). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The claimed compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).HPLC of Formula: 1211568-27-2

The Article related to bifunctional chimeric heterocycle preparation androgen receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 1211568-27-2

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

On February 29, 2008, Zhao, Lihua; Liu, Chaomei; Wu, Qiuye; Zhang, Lurong; Kim, Joanne published an article.SDS of cas: 67914-60-7 The title of the article was Design, synthesis and antitumor activity of thalidomide derivatives. And the article contained the following:

The antitumor activity of thalidomide derivatives [i.e., 2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione derivatives] was studied. A method for the synthesis of the title compounds is reported here. According to the structure of thalidomide, starting from β-D-glucosamine hydrochloride, twenty compounds were designed and synthesized. Product structures were determined by NMR, IR, MS. The target compounds were evaluated for their anticancer activity. The survival of 4T1 cells was determined Compounds substituted by a 3,4,6-tri-O-acetyl glucopyranoside have better antitumor activity than thalidomide dose. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).SDS of cas: 67914-60-7

The Article related to thalidomide analog glucopyranoside preparation antitumor agent breast cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 67914-60-7

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

Cao, Ling-feng; Zhang, Yong-tang; Zhang, Jing-zheng published an article in 2011, the title of the article was Improved process of the piperazine condensation for preparation of ciprofloxacin hydrochloride.Reference of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate And the article contains the following content:

Ciprofloxacin hydrochloride I complying with CP, EP and USP standard was prepared via substitution of cyclopropanecarboxylic acid with anhydrous piperazine. A novel reaction system was developed effectively to reduce the amount of two main byproducts and to increase product yield and quality. Based on the reaction system, other factors were investigated such as the equivalent of piperazine, the reaction temperature and reaction time to determine the optimal parameters of piperazine: the n-pentanol:2-Me pyrrolidone (v:v = 1:1) mixed solvent, 4 mol/L of anhydrous piperazine, 125°C∼130°C and reaction of 8 h, the total yield can reach 81.9%. 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).Reference of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to ciprofloxacin hydrochloride preparation cyclopropanecarboxylic acid piperazine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

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

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