Tag: 200-300

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 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 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 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

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 April 30, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmermann, Kurt published a patent.Related Products of 1211568-27-2 The title of the patent was Bifunctional heterocycles, their use in targeted degradation of rapidly accelerated fibrosarcoma polypeptides and their preparation. And the patent contained the following:

The present disclosure relates bifunctional compounds of formula ULM-L-PTM, their use in modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein) and treatment of diseases that result from aggregation or accumulation of the target protein. and their preparation Compounds of formula ULM-L-PTM, wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. comprising a RAF protein targeting moiety; L is a bond or chem. linking moiety connecting ULM and PTM; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorph and prodrug thereof, are claimed. Compound I was prepared using a multistep procedure (procedure given). The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given). 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 bifunctional heterocycle preparation raf modulator, 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, 1995, Camps, Pelayo; Farres, Xavier; Garcia, M. Luisa; Ginesta, Joan; Pascual, James; Mauleon, David; Carganico, Germano published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Stereoselective syntheses of both enantiomers of ketoconazole from (R)- and (S)-epichlorohydrin. And the article contained the following:

Stereoselective syntheses of both enantiomers of ketoconazole (I) from com. available (R)- or (S)-epichlorohydrin has been developed. The key step of these syntheses involves the selective substitution of the methylene chlorine atom by benzoate on a mixture of (2S,4R)-II and (2R,4R)-II or of their enantiomers, followed by crystallization of the corresponding cis-benzoates, from which (+)- or (-)-I were obtained as described for (±)-I. The ee’s of (+)- and (-)-ketoconazole were determined by HPLC on the CSP Chiralcel OD-H. 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 enantiomer stereoselective synthesis, 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 October 15, 2010, Zheng, Chun-zhi; Zhang, Guo-hua; Jiang, Da-feng published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was New process for synthesis of 1-acetyl-4-(4-hydroxyphenyl)piperazine. And the article contained the following:

The synthesis of the target compound was achieved (37.5% overall yield) by a sequence involving a chlorination, cyclization and acylation using bis(2-chloroethyl)amine hydrochloride and aminophenol as reactants. The product thus obtained [i.e., 1-[4-(4-Hydroxyphenyl)-1-piperazinyl]ethanone] was confirmed by IR, 1H-NMR. 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 ethanone hydroxyphenyl piperazine preparation, 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 July 14, 2011, Aissaoui, Hamed; Boss, Christoph; Corminboeuf, Olivier; Heidmann, Bibia; Siegrist, Romain published a patent.Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde The title of the patent was Preparation of piperazines as antimalarial agents. And the patent contained the following:

The invention relates to piperazine derivatives of Formula I (wherein X is CH or N; R1 is -NO2, -NMe2, H, CN, etc.; and R2 is H, Me, CN, halo, etc.), and their use as active ingredients in the preparation of pharmaceutical compositions The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria. Synthetic procedures for preparing I are exemplified. Example compound II, prepared by reacting the corresponding cinnamic acid derivative with amine intermediate III, was very effective in both in vivo and in vitro antimalarial assays. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde

The Article related to piperazine compound preparation antimalarial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde

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

On December 13, 2012, Aissaoui, Hamed; Boss, Christoph; Corminboeuf, Olivier; Heidmann, Bibia; Siegrist, Romain published a patent.Synthetic Route of 890092-19-0 The title of the patent was Piperazines as antimalarial agents. And the patent contained the following:

The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Synthetic Route of 890092-19-0

The Article related to piperazine compound preparation antimalarial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Synthetic Route of 890092-19-0

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