Heterocyclic Building Blocks-piperazine

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

Kumar, J. Ranjith; Nissankararao, Srinath; Ushasri, S.; Rehaman, Sk. A. published an article in 2014, the title of the article was Synthesis and antimicrobial activity of new series of piperazine containing chalcone derivatives.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone And the article contains the following content:

Treatment of 1-acetyl-4-(4-hydroxyphenyl)piperazine with aromatic or substituted aromatic aldehydes in presence of methanol and potassium hydroxide, formed 3-substituted phenyl-1-(4-(4-hydroxylphenyl)piperzin-1-yl)-prop-2-en-1-one derivatives I (R = Ph, 4-ClC6H4, 4-FC6H4, etc.). These are assayed for their antibacterial activity against Bacillus pumilus, Bacillus subtilis, Escherichia coli, Proteus vulgaris and for antifungal activity against Aspergillus niger, Candida albicans strains. Antibacterial assay revealed that Bacillus subtilis and Proteus vulgaris were the most sensitive bacterial strains to compounds I (R = 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, 2,4-di-MeOC6H3, 2,4-Cl2C6H3) and in the antifungal assay, compounds I (R = Ph, 4-FC6H4, 2,4-Cl2C6H3) were highly effective against Aspergillus niger when compared to other other investigated strains. 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 piperazine chalcone preparation antibacterial antifungal, 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, 1988, Lin, HanFen; Yue, Xiang; Chen, WenBin published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Improved preparation of 1-acetyl-4-(4-hydroxyphenyl)piperazine. And the article contained the following:

The title compound (I) was prepared in 4 steps in 26.4% overall yield starting from diethanolamine. 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 acetylhydroxyphenylpiperazine, piperazine acetylhydroxyphenyl, 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 April 20, 2003, Ryu, Jae Chun; Lee, Kwang Jae; Lee, Sang Hee published an article.HPLC of Formula: 67914-60-7 The title of the article was Synthesis of ketoconazole derivatives. And the article contained the following:

For the drug master file (DMF) of ketoconazole, four impurities contained in ketoconazole were synthesized. During the synthesis of I, a new synthetic method of 1,4-dihydropyrazine was established. To oxidize the aminoalc. of I to the aminal I, the standard Swern oxidation condition was modified to mask the nucleophilicity of the amino group temporarily using one equivalent of acetic acid. Derivative II was synthesized via regioselective bromination at the I position of the 4-aminophenol derivative of II using Br2 in the presence of p-TsOH. The etherification of aryl bromide with a phenol derivative compound was accomplished by a modification of the general Cu-mediated reaction condition using excess of the phenol derivative itself as a solvent at elevated temperature (190 °C). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).HPLC of Formula: 67914-60-7

The Article related to ketoconazole derivative drug master file impurity preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 67914-60-7

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

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