Category: 67914-60-7

Schiaffella, Fausto published the artcileNovel ketoconazole analogues based on the replacement of 2,4-dichlorophenyl group with 1,4-benzothiazine moiety: Design, synthesis, and microbiological evaluation, Category: piperazines, the publication is Bioorganic & Medicinal Chemistry (2006), 14(15), 5196-5203, database is CAplus and MEDLINE.

As a part of a program to develop novel antifungal agents, new compounds which incorporate the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared These compounds were computationally investigated to assess whether the 1,4-benzothiazine moiety was a suitable bioisosteric replacement for the 2,4-dichlorophenyl group of KTZ in order to obtain a more potent inhibition of CYP51 enzyme of Candida albicans. Results of preliminary microbiol. studies show that the racemic cis-7 analog has a good in vivo activity, comparable to that of KTZ, but the best activity was observed in the racemic trans-7 analog.

Bioorganic & Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Beyzavi, Hudson published the artcile¹⁸F-Deoxyfluorination of Phenols via Ru ¦Ð-Complexes, COA of Formula: C12H16N2O2, the publication is ACS Central Science (2017), 3(9), 944-948, database is CAplus and MEDLINE.

The deficiency of robust and practical methods for ¹⁸F-radiofluorination is a bottleneck for positron emission tomog. (PET) tracer development. Here, we report the first transition-metal-assisted ¹⁸F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atm., large substrate scope, and translatability to generate doses appropriate for PET imaging.

ACS Central Science published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, COA of Formula: C12H16N2O2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Tang, Yan-feng published the artcileSynthesis of preladenant, COA of Formula: C12H16N2O2, the publication is Jingxi Huagong (2014), 31(10), 1250-1254, database is CAplus.

An intermediate, 1-(4′-methoxyethoxyl phenyl) piperazine (III), was synthesized from 1-(4′-hydroxylphenyl)-piperazinyl ethanone (I) via etherification and hydrolysis. Another intermediate (VII) with a nitrogen condensed ring was prepared from Me furan-2-carboxylate (IV) by acylation, ring-closure and halogenation. Finally, Preladenant was prepared from the two intermediates by condensation reaction. FTIR, ¹HNMR and ESI-MS were employed to characterize these intermediates and the target compound Through common synthetic method, the yields of these 6 steps are 99.0%, 95.4%, 98.0%, 78.9%, 86.9% (calculated by Cl) and 52.5%, resp. To obtain a higher total yield, ultrasonic was used in the last condensation reaction. The results show that the condensation yield reached 85.4% when the reaction conditions were as follows: the ultrasonic power (150 W), the molar ratio of intermediate III to VII (1.2: 1), solvent (DMSO), acid-bonding agent (Na₂CO₃), reaction temperature (90¡ãC) and reaction time (1.5 h). The yield of the condensation is greatly increased by ultrasonic method.

Jingxi Huagong published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C11H12O4, COA of Formula: C12H16N2O2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Komami, Narumi published the artcilePalladium-Catalyzed Germylation of Aryl Bromides and Aryl Triflates Using Hexamethyldigermane, Computed Properties of 67914-60-7, the publication is Synthesis (2018), 50(10), 2067-2075, database is CAplus.

Pd-catalyzed germylation of aryl bromides and aryl triflates using com. available hexamethyldigermane is described. Optimized reaction conditions afforded various functionalized aryltrimethylgermanes, including drug-like mols., in moderate to good yields, demonstrating the versatility of the presented protocols.

Synthesis published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Computed Properties of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Schiaffella, Fausto published the artcileNovel ketoconazole analogues based on the replacement of 2,4-dichlorophenyl group with 1,4-benzothiazine moiety: Design, synthesis, and microbiological evaluation, Category: piperazines, the publication is Bioorganic & Medicinal Chemistry (2006), 14(15), 5196-5203, database is CAplus and MEDLINE.

As a part of a program to develop novel antifungal agents, new compounds which incorporate the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared These compounds were computationally investigated to assess whether the 1,4-benzothiazine moiety was a suitable bioisosteric replacement for the 2,4-dichlorophenyl group of KTZ in order to obtain a more potent inhibition of CYP51 enzyme of Candida albicans. Results of preliminary microbiol. studies show that the racemic cis-7 analog has a good in vivo activity, comparable to that of KTZ, but the best activity was observed in the racemic trans-7 analog.

Bioorganic & Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Beyzavi, Hudson published the artcile¹⁸F-Deoxyfluorination of Phenols via Ru π-Complexes, COA of Formula: C12H16N2O2, the publication is ACS Central Science (2017), 3(9), 944-948, database is CAplus and MEDLINE.

The deficiency of robust and practical methods for ¹⁸F-radiofluorination is a bottleneck for positron emission tomog. (PET) tracer development. Here, we report the first transition-metal-assisted ¹⁸F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atm., large substrate scope, and translatability to generate doses appropriate for PET imaging.

ACS Central Science published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, COA of Formula: C12H16N2O2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Tang, Yan-feng published the artcileSynthesis of preladenant, COA of Formula: C12H16N2O2, the publication is Jingxi Huagong (2014), 31(10), 1250-1254, database is CAplus.

An intermediate, 1-(4′-methoxyethoxyl phenyl) piperazine (III), was synthesized from 1-(4′-hydroxylphenyl)-piperazinyl ethanone (I) via etherification and hydrolysis. Another intermediate (VII) with a nitrogen condensed ring was prepared from Me furan-2-carboxylate (IV) by acylation, ring-closure and halogenation. Finally, Preladenant was prepared from the two intermediates by condensation reaction. FTIR, ¹HNMR and ESI-MS were employed to characterize these intermediates and the target compound Through common synthetic method, the yields of these 6 steps are 99.0%, 95.4%, 98.0%, 78.9%, 86.9% (calculated by Cl) and 52.5%, resp. To obtain a higher total yield, ultrasonic was used in the last condensation reaction. The results show that the condensation yield reached 85.4% when the reaction conditions were as follows: the ultrasonic power (150 W), the molar ratio of intermediate III to VII (1.2: 1), solvent (DMSO), acid-bonding agent (Na₂CO₃), reaction temperature (90°C) and reaction time (1.5 h). The yield of the condensation is greatly increased by ultrasonic method.

Jingxi Huagong published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C11H12O4, COA of Formula: C12H16N2O2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Komami, Narumi published the artcilePalladium-Catalyzed Germylation of Aryl Bromides and Aryl Triflates Using Hexamethyldigermane, Computed Properties of 67914-60-7, the publication is Synthesis (2018), 50(10), 2067-2075, database is CAplus.

Pd-catalyzed germylation of aryl bromides and aryl triflates using com. available hexamethyldigermane is described. Optimized reaction conditions afforded various functionalized aryltrimethylgermanes, including drug-like mols., in moderate to good yields, demonstrating the versatility of the presented protocols.

Synthesis published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Computed Properties of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

He, Qiuqin published the artcileSynthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-y1)-2-(2,4-difluorophenyl)-3-[(4-substituted)-piperazin-1-y1]-2-propanol, Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Zhongguo Yaowu Huaxue Zazhi (2007), 17(1), 8-12, database is CAplus.

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.

Zhongguo Yaowu Huaxue Zazhi published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Liang, Shuang published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted)-1-piperazinyl]-2-propanols, Category: piperazines, the publication is Zhongguo Yaowu Huaxue Zazhi (2004), 14(2), 71-75, database is CAplus.

The effect of the side chain in (4-substituted)-1-piperazinyl on the antifungal activity of fluconazole compounds was studied. Thirteen title compounds were synthesized and confirmed by the elementary anal., ¹H-NMR and IR spectra. The MICs of all the title compounds were determined by the method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using the RPMI1640 test medium. The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities. The activities of the eight compounds thus prepared were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro. The lipid/water distribution coefficient and stereochem. have important influence on the antifungal activities of the title compounds

Zhongguo Yaowu Huaxue Zazhi published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics