Tag: 200-300

On August 31, 2007, He, Qiuqin; Liu, Chaomei; Li, Ke; Cao, Yongbing; Zhao, Lihua; Tang, Wenya 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-yl)-2-(tert-butyl)-3-(O-substituted)-2-propanol derivatives. And the article contained the following:

A method for the synthesis of the title compounds [i.e., α-(1,1-dimethylethyl)-α-[[4-(1-piperazinyl)phenoxy]methyl]-1H-1,2,4-Triazole-1-ethanol derivatives] is reported here. The antifungal activity of triazole derivatives bearing a tert-Bu group was studied and their antifungal activity was compared with those of the control drugs (fluconazole and itraconazole). Twelve target compounds were designed by the replacement of a 2,4-difluorophenyl group with a tert-Bu group. The target compounds were determined by NMR, IR. The MICs80 of these title compounds were determined by a method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using an RPMI 1640 test medium. The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activity. Other hydrophobic moieties besides a 2,4-difluorophenyl group can be introduced to design triazole compounds 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 triazoleethanol dimethylethyl piperazinyl phenoxy preparation antifungal agent, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On April 30, 1997, Huang, Liang-Fu; Kim, Jang-Woo; Bauer, Ludwig; Doss, George published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis of 1,2,4-triazole and thiazole analogs of ketoconazole. And the article contained the following:

The synthesis of 1,2,4-triazole and thiazole analogs of ketoconazole is described in which one of the α azole ring carbons is linked to C-2 of the ketal by means of a three methylene tether. Lithiation of 1-methyl-1,2,4-triazole and thiazole and subsequent alkylation with 2-(2,4-dichlorophenyl)-2-(3-iodopropyl)-1,3-dioxolane produced, after an aqueous acidic workup, 2,4-dichlorophenyl 3-[5-(1-methyl-1,2,4-triazolyl) and 2-thiazolyl]propyl ketones, resp. Ketalization with glycerol furnished the corresponding diastereomeric pairs of cis- and trans-1,3-dioxolanes. The reaction of 2,4-dichlorophenyl 3-[5-(1-methyl-1,2,4-triazolyl)]propyl ketone with 3-mercapto-1,2-propanediol produced the corresponding diastereomeric cis- and trans-hydroxymethyl-1,3-oxathiolanes. The diastereomeric racemates were separated by column chromatog. and their stereochem. established by NOE NMR experiments Some of these racmic cis ketal alcs. were converted by benzyl bromide to the corresponding benzyl ethers. Several of these racemic cis-ketals were reacted, first with methanesulfonyl chloride, then with 1-acetyl-4-(4-hydroxyphenyl)piperazine, to furnish the title compounds 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 ketoconazole triazole thiazole analog preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On August 31, 2008, Chen, Yonghao; Long, Shengjing published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis of ketoconazole by phase-transfer catalysis. And the article contained the following:

Antifungal drug ketoconazole was synthesized by utilization of phase-transfer catalysis from [2-bromomethyl-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl]methanol via acylation, N-alkylation with imidazole and hydrolysis, formation the active ester with methanesulfonyl chloride, and then condensation with the side chain 1-acetyl-4-(4-hydroxyphenyl)piperazine. The overall yield was about 30%. 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 ketoconazole synthesis antifungal drug bromomethyldichlorophenyl dioxolanylmethanol, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Recommanded Product: 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 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 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 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 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

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 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