Category: pyrazoles-derivatives

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 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 August 12, 1975, Wikel, James H. published a patent.COA of Formula: C11H9N3O4 The title of the patent was 5-(2-Aminophenyl)pyrazole-3-carboxylic acids and esters. And the patent contained the following:

MeO2CCO2Me was treated with MeCOC6H4NO2-2 and the o-O2NC6H4COCH2COCO2Et cyclized with H2NNH2 to give I (R = NO2), which was reduced to I (R = NH2). At 1-200 mg/kg I (R = NH2) was a complement inhibitor. The experimental process involved the reaction of Methyl 3-(2-nitrophenyl)-1H-pyrazole-5-carboxylate(cas: 57446-04-5).COA of Formula: C11H9N3O4

The Article related to complement inhibitor aminophenylpyrazolecarboxylate, pyrazolecarboxylate aminophenyl complement inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.COA of Formula: C11H9N3O4

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

On March 1, 2007, Arora, Nidhi; Billedeau, Roland Joseph; Dewdney, Nolan James; Gabriel, Tobias; Goldstein, David Michael; O’Yang, Counde; Soth, Michael; Trejo-Martin, Teresa Alejandra published a patent.Recommanded Product: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the patent was Preparation of fused pyrazole derivatives as P38 MAP kinase inhibitors. And the patent contained the following:

The title fused pyrazole derivatives are prepared as p38 MAP kinase inhibitors for the treatment of p38-mediated diseases. For example, the compound I was prepared in a multi-step synthesis. I inhibited p38 MAP kinase with IC50 of 0.001 μM in vitro. Formulations containing the title compound as an active ingredient were also described. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Recommanded Product: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to preparation pyrazolo pyrimidine pyridine p38 map kinase inhibitor, formulation treatment arthritis human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

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

On September 30, 2012, Siddhartha, Tarun; Mithilesh; Sharma, Raju; Chawla, Pooja; Saraf, S. K. published an article.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Syntheses and antioxidant screening of pyrazole-4-carboxaldehyde derivatives. And the article contained the following:

Pyrazole-4-carboxaldehydes were synthesized by AcOH-mediated condensation of aryl Me ketones with phenylhydrazines in EtOH to afford the corresponding phenylhydrazones. Subsequent reaction with 2 equiv DMF-POCl3 adduct (Vilsmeier Haack reagent) in DMF at 60-70° for 6 h afforded immonium perchlorates. Further, alk. hydrolysis (NaOH) afforded pyrazole-4-carboxaldehydes. All the synthesized compounds were screened for antioxidant activity. In a ferric reducing power assay, increased absorbance of the compounds with concentration indicates increased reducing power. Compounds with higher concentrations showed a higher reducing power. The reducing power showed good linear relation (R2) in both standard as well as in the newly prepared compounds Thus, the compounds have antioxidant activity. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to phenylhydrazone vilsmeier haack cyclization formylation, pyrazolecarboxaldehyde preparation antioxidant, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

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

Kendall, Jackie D.; O’Connor, Patrick D.; Marshall, Andrew J.; Frederick, Raphael; Marshall, Elaine S.; Lill, Claire L.; Lee, Woo-Jeong; Kolekar, Sharada; Chao, Mindy; Malik, Alisha; Yu, Shuqiao; Chaussade, Claire; Buchanan, Christina; Rewcastle, Gordon W.; Baguley, Bruce C.; Flanagan, Jack U.; Jamieson, Stephen M. F.; Denny, William A.; Shepherd, Peter R. published an article in 2012, the title of the article was Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid And the article contains the following content:

A novel series of pyrazolo[1,5-a]pyridines were prepared as PI3 kinase inhibitors, and their selectivity for the p110α isoform over the other Class Ia PI3 kinases was demonstrated. The SAR around the pyrazolo[1,5-a]pyridine ring system was investigated, and N’-[(5-cyanopyrazolo[1,5-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonic acid hydrazide was shown to be a particularly potent example (p110α IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid

The Article related to pyrazolopyrazinylmethylene benzenesulfonylhydrazine preparation pi3 kinase inhibitor anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid

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

Verma, Anil; Kumar, Vinod; Kataria, Ramesh; Singh, Joginder published an article in 2019, the title of the article was Novel acetohydrazide pyrazole derivatives, design, synthesis, characterization and antimicrobial activity.Computed Properties of 36640-53-6 And the article contains the following content:

Eleven acetohydrazide linked pyrazole derivatives I [R = Ph, thiophen-2-yl, 1-naphthyl, etc.] were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds I were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds I were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. I [R = 4-fluorophenyl, 4-chlorophenyl, 4-bromophenyl] were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives I as compared to other groups present in the ring. Hence, among compounds I [R = 4-fluorophenyl, 4-chlorophenyl, 4-bromophenyl] could be explored further against other microbes to prove its vitality. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Computed Properties of 36640-53-6

The Article related to diphenyl pyrazolylmethylene acetohydrazide preparation antibacterial antifungal activity sar, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 36640-53-6

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

On March 27, 1979, Rainer, Georg published a patent.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the patent was 4-Pyrazoleacetic acid derivatives. And the patent contained the following:

Pyrazoleacetic acid derivatives I (R = CO2H, alkoxycarbonyl, CONH2; R1, R2 = optionally substituted Ph, furyl, thienyl, naphthyl; R3 = H, Ph, furyl) were prepared Thus, CH2Ac2 was treated with BrCH2CO2Et to give Ac2CHCH2CO2Et which was cyclized with PhNHNH2 to give I (R = CO2Et, R1 = Ph, R2 = R3 = Me), which was hydrolyzed to the acid. I had antiinflammatory and analgesic activity. Thus, I (R = CO2H, R1 = Ph, R2 = R3 = 2-furyl) had antiinflammatory ED50 in the UV erythema test of 1.5 mg/kg orally and then analgesic ED40 50 mg/kg orally. 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 pyrazoleacetic acid, antiinflammatory pyrazoleacetic acid, analgesic pyrazoleacetic acid, 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 19, 2014, Vankayalapati, Hariprasad; Yerramreddy, Venkatakrishnareddy; Ganipisetty, Venu Babu; Talluri, Sureshkumar; Appalaneni, Rajendra P. published a patent.Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol The title of the patent was Preparation of substituted 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors. And the patent contained the following:

The present invention relates to compounds I-III [X = N or CH; L1 = H, F, (un)substituted Ph, etc.; Q = direct bond, thienyl, thiazolyl, Ph, etc.; R1 = H, halo, CN, etc.; Z = direct bond, thienyl, thiazolyl, Ph, etc.; R2 = H, halo, CN, etc.; n = 0-2; m = 0-2; with the provisos], to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes. Over two-hundred compounds I were prepared and/or claimed. E.g., a multi-step synthesis of IV, starting from 2,2-dimethyl-1,3-dioxane-4,6-dione and 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, was described. Exemplified compounds I were tested against SIK2 (data given for representative compounds I). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

The Article related to pyrrolopyridine pyrazolopyridine preparation salt inducible kinase 2 sik2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

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

On September 11, 2014, Vankayalapati, Hariprasad; Yerramreddy, Venkatakrishnareddy; Ganipisetty, Venu Babu; Talluri, Sureshkumar; Appalaneni, Rajendra P. published a patent.HPLC of Formula: 924909-16-0 The title of the patent was Preparation of substituted 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors. And the patent contained the following:

The present invention relates to compounds I-III [X = N or CH; L1 = H, F, (un)substituted Ph, etc.; Q = direct bond, thienyl, thiazolyl, Ph, etc.; R1 = H, halo, CN, etc.; Z = direct bond, thienyl, thiazolyl, Ph, etc.; R2 = H, halo, CN, etc.; n = 0-2; m = 0-2; with the provisos], to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes. Over two-hundred compounds I were prepared and/or claimed. E.g., a multi-step synthesis of IV, starting from 2,2-dimethyl-1,3-dioxane-4,6-dione and 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, was described. Exemplified compounds I were tested against SIK2 (data given for representative compounds I). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).HPLC of Formula: 924909-16-0

The Article related to pyrrolopyridine pyrazolopyridine preparation salt inducible kinase 2 sik2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.HPLC of Formula: 924909-16-0

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