Month: November 2022

On December 20, 2019, Xu, Zichen; Wei, Wanguo; Fang, Xianjie; Liu, Rufeng; Yi, Mingyue; Zhou, Chenglong; Liu, Jie published a patent.Computed Properties of 1187582-58-6 The title of the patent was Preparation method of N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide as androgen receptor antagonist. And the patent contained the following:

The invention relates to a process for the preparation of N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide as androgen receptor antagonist. For instance, Suzuki reaction of 2-chloro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-benzonitrile with 5-bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole followed by deprotection, N-alkylation with N-Boc-L-alaninol, amidation with 5-acetyl-1H-pyrazole-3-carboxylic acid Et ester, and reduction to give N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Computed Properties of 1187582-58-6

The Article related to chlorocyanophenyl pyrazolylmethylethylhydroxyethyl pyrazolecarboxamide preparation suzuki alkylation amidation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 1187582-58-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 30, 2002, Vovk, M. V.; Mel’nichenko, N. V.; Chornous, V. A.; Bratenko, M. K. published an article.Formula: C20H14N2O The title of the article was Intramolecular cyclization of 4-isocyanato-3-(2-naphthyl)-1-phenylpyrazole under friedel-crafts reaction conditions. And the article contained the following:

4-Isocyanato-3-(2-naphthyl)-1-phenylpyrazole cyclized under the influence of AlCl3 to give 2H-benzo-[h]pyrazolo[4,3-c]isoquinoline. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Formula: C20H14N2O

The Article related to isocyanatonaphthylphenylpyrazole intramol cyclization friedel crafts condition, benzopyrazoloisoquinoline preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Formula: C20H14N2O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 30, 2016, Diamanti, Eleonora; Bottegoni, Giovanni; Goldoni, Luca; Realini, Natalia; Pagliuca, Chiara; Bertozzi, Fabio; Piomelli, Daniele; Pizzirani, Daniela published an article.Application In Synthesis of 5-Methoxy-1H-pyrazole The title of the article was Pyrazole-Based Acid Ceramidase Inhibitors: Design, Synthesis, and Structure-Activity Relationships. And the article contained the following:

Acid ceramidase (a.c.) is a lysosomal cysteine amidase responsible for the cleavage of ceramide into sphingosine, which is then phosphorylated to sphingosine 1-phosphate. AC regulates the intracellular levels of ceramide and sphingosine, and a.c. inhibition may be useful in the treatment of disorders, such as cancer, in which ceramide-mediated signaling may be dysfunctional. Despite their potential exptl. and therapeutic value, the number of available small-mol. inhibitors of a.c. activity remains limited. In the present study is described the discovery of a class of potent pyrazole carboxamide-based a.c. inhibitors, which were identified using the at. property field (APF) approach and developed through systematic SAR studies and in vitro pharmacol. characterization. The best compound of this series inhibits a.c. with nanomolar potency and causes ceramide accumulation and sphingosine depletion in intact G361 proliferative melanoma cells. By expanding the current armamentarium of a.c. inhibitors, these results should facilitate future efforts to unravel the biol. of a.c. and the therapeutic potential of its inhibition. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Application In Synthesis of 5-Methoxy-1H-pyrazole

The Article related to alkyl isocyanate coupling reaction pyrazole, pyrazole carboxamide derivative preparation potent acid ceramidase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application In Synthesis of 5-Methoxy-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 30, 2014, Ashok, D.; Ganesh, Arram; Ravi, S.; Lakshmi, B. Vijaya published an article.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Solvent-free microwave assisted synthesis and antimicrobial activity of new 2-{4-[3-(1-phenyl-3-aryl-1H-pyrazol-4-yl)-acryloyl]-phenyl}-isoindole-1,3-diones. And the article contained the following:

A series of new 2-(4-(3-(1-phenyl-3-aryl-1H-pyrazol-4-yl)-acryloyl)-phenyl)-isoindole-1,3-diones I (Ar = C6H5, 4-MeC6H4, 4-MeOC6H4, 4-BrC6H4, 2-naphthyl, etc.) have been synthesized by Claisen-Schmidt condensation of 2-(4-acetylphenyl)-isoindole-1,3-dione with 1-phenyl-3-aryl-1H-pyrazole-4-carbaldehydes in the presence of basic alumina under solvent-free microwave irradiation and conventional heating methods. All the synthesized compounds were screened for their antimicrobial activity. The activity was determined using cup plate agar diffusion method by measuring the zone of inhibition in mm. From the screening studies it is evident that the synthesized compounds I (Ar = Ph, 4-MeC6H4, 2-naphthyl) showed good antibacterial activity and compounds I (Ar = 4-MeOC6H4, 2-naphthyl) showed good antifungal activity against all the tested organisms. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazolyl acryloyl phenylisoindoledione preparation green chem microwave irradiation, solvent free antibacterial antifungal, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 30, 1998, Bau, Bernarde; Hofmann, Thorsten; Kloss, Juergen; Neunhoeffer, Hans published an article.Recommanded Product: 5-Methoxy-1H-pyrazole The title of the article was 1,2,3-Triazines. Part 5. Lithiation of 1,2,3-triazines. And the article contained the following:

5-Ethoxy-1,2,3-triazine is mono- and dilithiated and the resulting 4-lithio- and 4,6-dilithio-1,2,3-triazines, were reacted with aromatic aldehydes to give α-hydroxybenzylated derivatives The latter are oxidized to give benzoyl-1,2,3-triazines. Condensation of 4,6-bis(4-methylbenzoyl)-5-ethoxy-1,2,3-triazine, with N2H4 afforded a pyrazolo[4.3-d][1,2,3]triazine, and reaction of benzoyl-1,2,3-triazines with (CH2NH2)2 afforded the 1,2,3-triazino[5,4-e][1,4]diazepines. 4-Methoxy-1,2,3-triazine forms 5- and 6-lithio-4-methoxy-1,2,3-triazine, whose reaction with PhCHO gave 5- and 6-(α-hydroxybenzyl)-4-methoxy-1,2,3-triazine, resp. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Recommanded Product: 5-Methoxy-1H-pyrazole

The Article related to triazine preparation lithiation alkylation, benzoyltriazine preparation, pyrazolotriazine preparation, triazinodiazepine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Recommanded Product: 5-Methoxy-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Arbaciauskiene, Egle; Martynaitis, Vytas; Krikstolaityte, Sonata; Holzer, Wolfgang; Sackusa, Algirdas published an article in 2011, the title of the article was Synthesis of 3-substituted 1-phenyl-1H-pyrazole-4-carbaldehydes and the corresponding ethanones by Pd-catalyzed cross-coupling reactions.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde And the article contains the following content:

An efficient synthetic route to construct substituted 1-phenyl-1H-pyrazole-4-carboxaldehydes and the corresponding ethanones was described and the synthesis of the target compounds was achieved using 1-phenyl-1H-pyrazol-3-ol as a starting material. Carbon-carbon bond-forming palladium-catalyzed cross-coupling reactions were applied for the functionalization of the intermediate pyrazole triflates [i.e., trifluoromethanesulfonic acid 1-phenyl-1H-pyrazol-3-yl ester derivatives]. The target compounds thus formed included imidazo[4,3-c]pyridine derivatives, 1,3-diphenyl-1H-pyrazole-4-carboxaldehyde, 1-phenyl-3-(3-thienyl)-1H-pyrazole-4-carboxaldehyde, 1-(1,3-diphenyl-1H-pyrazol-4-yl)ethanone, etc. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazolol triflate preparation palladium catalyzed cross coupling, pyrazolecarboxaldehyde preparation, ethanone pyrazolyl preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Xu, Li-Li; Zheng, Chang-Ji; Sun, Liang-Peng; Miao, Jing; Piao, Hu-Ri published an article in 2012, the title of the article was Synthesis of novel 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties as potential antibacterial agents.Electric Literature of 36640-53-6 And the article contains the following content:

In the present study, a series of 1,3-diarylpyrazole derivatives I [R = (un)substituted Ph, n = 1-5] bearing rhodanine-3-fatty acid moieties were synthesized and their antimicrobial activities were tested against various Gram-pos. and Gram-neg. bacteria. 1,3-Diaryl-4-formylpyrazoles were synthesized as key intermediates following a Vilsmeier-Haack strategy. Several compounds with an MIC of 2 μg/mL exhibited stronger antibacterial activity against the methicillin-resistant Staphylococcus aureus (MRSA) than the controls. None of the compounds showed any activity against Gram-neg. bacteria. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Electric Literature of 36640-53-6

The Article related to pyrazole aryl rhodanine derivative preparation antibacterial, thiazolidinone thioxodiarylpyrazolylmethylene preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Electric Literature of 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On December 31, 2014, Goel, Neelima; Drabu, Sushma; Afzal, Obaid; Bawa, Sandhya published an article.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Antimicrobial screening and one-pot synthesis of 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives. And the article contained the following:

A series of 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives (4a-4k) were synthesized through direct reductive amination of 3-(naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde with various substituted aromatic amines using NaBH4 in the presence of I2 as reducing agent. The reaction was carried out in anhydrous methanol under neutral conditions at room temperature All 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives (4a-4k) were tested in vitro for antifungal and antibacterial activities against different fungal and bacterial strains. Most of the compounds exhibited considerable antifungal activity, but poor antibacterial activity against the test strains. In the series compound 4e, 4g, 4j, and 4k, showed excellent antifungal activity against the fungal strain Aspergillus niger (MTCC) 281 and Aspergillus flavus MTCC 277 (% inhibition in the range of 47.7-58.9). The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazole naphthyl anilinomethyl preparation antibacterial antifungal, antimicrobial activity, naphthalene, pyrazole, reductive amination, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On June 6, 2008, McLaughlin, Mark; Marcantonio, Karen; Chen, Cheng-yi; Davies, Ian W. published an article.Quality Control of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The title of the article was A Simple, Modular Method for the Synthesis of 3,4,5-Trisubstituted Pyrazoles. And the article contained the following:

A modular approach for the regiocontrolled preparation of pyrazoles bearing substituents on all three carbon atoms is described. Central to this method is the use of a switchable metal-directing group to enable sequential direct lithiation of the 3- and 5-positions of the pyrazole ring. Pyrazole boronic esters obtained from these lithiated intermediates can undergo efficient Suzuki cross-coupling under the developed nonaqueous conditions, which minimize undesirable protolytic deboronation. Halogenation of the 4-position provides the means for substitution at the remaining carbon atom. The experimental process involved the reaction of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 1028092-65-0).Quality Control of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

The Article related to aryl pyrazole regioselective synthesis, pyrazole tetrahydropyranyl regioselective lithiation suzuki coupling aryl halide, tetrahydropyranyl metal directing group, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Salanouve, Elise; Retailleau, Pascal; Janin, Yves L. published an article in 2012, the title of the article was Few unexpected results from a Suzuki-Miyaura reaction.Recommanded Product: 215610-30-3 And the article contains the following content:

In the course of the synthesis of original anti-infectious compounds, we focused on the palladium-catalyzed Suzuki-Miyaura aryl-aryl coupling reaction between 2-(3-ethoxy-5-iodo-1H-pyrazol-1-yl)pyridine and phenylboronic acid. A study of the reaction products obtained under different conditions (various ligands and solvents) not only provided us with insights to optimize this reaction but also with a few side compounds, resulting from CH activation, along with the unexpected bis(3-ethoxy-1-(pyridin-2-yl)-1H-pyrazol-5-yl)palladium. Stoichiometric experiments with this remarkably stable biscyclopalladated reagent and Ph halides pointed out the occurrence of aryl-aryl coupling, possibly via palladium IV intermediates. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Recommanded Product: 215610-30-3

The Article related to bispyridinylpyrazolylpalladium preparation reaction aryl halide, palladium bispyridinylpyrazolyl preparation reaction aryl halide, side product suzuki miyaura reaction, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 215610-30-3

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics