Category: 67914-60-7

On July 15, 2008, Irie, Osamu; Ehara, Takeru; Iwasaki, Atsuko; Yokokawa, Fumiaki; Sakaki, Junichi; Hirao, Hajime; Kanazawa, Takanori; Teno, Naoki; Horiuchi, Miyuki; Umemura, Ichiro; Gunji, Hiroki; Masuya, Keiichi; Hitomi, Yuko; Iwasaki, Genji; Nonomura, Kazuhiko; Tanabe, Keiko; Fukaya, Hiroaki; Kosaka, Takatoshi; Snell, Christopher R.; Hallett, Allan published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Discovery of selective and nonpeptidic cathepsin S inhibitors. And the article contained the following:

Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an inhouse pyrrolopyrimidine cathepsin K inhibitor by modification of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanomolar inhibition of cathepsin S with over 100-fold selectivity against other cysteine proteases, including cathepsin K and L. Some of the inhibitors showed cellular activities in mouse splenocytes as well as oral bioavailabilities in rats. 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 arylmethylpyrrolopyrimidinecarbonitrile preparation cathepsin s inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On February 8, 2018, Hou, Jinqiang; Kovacs, Michael S.; Dhanvantari, Savita; Luyt, Leonard G. published an article.HPLC of Formula: 67914-60-7 The title of the article was Development of Candidates for Positron Emission Tomography (PET) Imaging of Ghrelin Receptor in Disease: Design, Synthesis, and Evaluation of Fluorine-Bearing Quinazolinone Derivatives. And the article contained the following:

Mol. imaging with positron emission tomog. (PET) is an attractive platform for noninvasive detection and assessment of disease. The development of a PET imaging agent targeting the ghrelin receptor (growth hormone secretagogue receptor type 1a or GHS-R1a) has the potential to lead to the detection and assessment of the higher than normal expression of GHS-R1a in diseases such as prostate, breast, and ovarian cancer. To enable the development of 18F radiopharmaceuticals, we have designed and synthesized three series of quinazolinone derivatives, resulting in the identification of two compound with subnanomolar binding affinity and one fluorine-bearing compound I with picomolar binding affinity (20 pM), representing the highest binding affinity for GHS-R1a reported to date. Two lead compounds (II, IC50 = 20.6 nM; III, IC50 = 9.3 nM) were successfully 18F-radiolabeled with radiochem. purity of greater than 99%. Mol. modeling studies were performed to shed light on ligand-receptor interactions. 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 quinazolinone fluorine bearing preparation ghrelin receptor pet imaging, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 67914-60-7

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

On March 15, 2007, Silverman, Lisa S.; Caldwell, John P.; Greenlee, William J.; Kiselgof, Eugenia; Matasi, Julius J.; Tulshian, Deen B.; Arik, Leyla; Foster, Carolyn; Bertorelli, Rosalia; Monopoli, Angela; Ongini, Ennio published an article.Formula: C12H16N2O2 The title of the article was 3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists. And the article contained the following:

A novel series of 3-substituted-8-aryl-[1,2,4]triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A2A receptor antagonists with improved selectivity over the A1 receptor, physiochem. properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound I (R = MeOCH2CH2O) displayed both superior in vitro and highly promising in vivo profiles. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to triazolopurinamine preparation adenosine a2a antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C12H16N2O2

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

On December 31, 1995, Li, Lu; Tong, Zengshou; Gan, Guizhi published an article.Product Details of 67914-60-7 The title of the article was Synthesis of ketoconazole derivatives. And the article contained the following:

Title compounds I [R = Ac, P(O)(OEt)2, P(O)(OCHMe2)2] were prepared E.g., reaction of I (R = H) with di-Et phosphite, Et3N, and CCl4 in N,N-dimethylacetamide, CH2Cl2, and benzene gave 86% I [R = P(O)(OEt)2]. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Product Details of 67914-60-7

The Article related to ketoconazole derivative preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Product Details of 67914-60-7

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

Yang, Jiqiu; Liu, Lilin; Wang, Xiaoyan; Lu, Jiaguo; Sun, Changsheng; Zhang, Huanxiang; Zhou, Youjun; Zhang, Zhong published an article in 1984, the title of the article was Synthesis of an antifungal drug ketoconazole.Formula: C12H16N2O2 And the article contains the following content:

The title compound [I, R = p-(4-acetylpiperazin-1-yl)phenyl] was prepared by condensation of I (R = MeSO2) with piperazine II which was prepared starting from piperazine. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to ketoconazole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C12H16N2O2

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

Heeres, J.; Backx, L. J. J.; Van Cutsem, J. published an article in 1984, the title of the article was Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones.Computed Properties of 67914-60-7 And the article contains the following content:

The antifungal triazolone derivatives I [R = H, Me, Q (X = N, CH); R1 = H, alkyl; R2 = H, Me) were prepared by a multistep sequence from 1-(p-methoxyphenyl)piperazine or MeSO3Q via piperazines III (R3 = H, Bz) and cyclization of III [R3 = C(:NH)NH2] with R2C(:NH)NH2. In vitro and in vivo antifungal properties of I are reported. Compound I [R = Q (X = N), R1 = MeEtCH, R2 = H], which displays a pronounced oral activity against vaginal candidosis in rats and against microsporosis in guinea pigs, was selected for clin. evaluation. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Computed Properties of 67914-60-7

The Article related to triazolone phenylpiperazinophenyl preparation fungicide, fungicide phenylpiperazinophenyltriazolone, piperazinophenyltriazolone phenyl, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Computed Properties of 67914-60-7

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

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