Category: 215610-30-3

On February 10, 2010, Janin, Yves; Guillou, Sandrine published a patent.Application In Synthesis of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of alkoxypyrazoles. And the patent contained the following:

The present invention relates to a process for the preparation of alkoxypyrazoles and new alkoxypyrazole compounds The invention relates to a process for the preparation of alkoxypyrazoles I and their isomers, wherein R1 is (un)substituted alkyl, alkenyl, or alkynyl, etc.; R2 is H, halo, substituted alkyl, alkenyl, or alkynyl; R3 is H, halo, (un)substituted alkyl, or aryl, etc.; R4 is H, (un)substituted alkyl, aryl, or heteroaryl, etc. For instance, heterocyclization of diethylethoxymethylenemalonate with NH2NH2 gave Et 3-ethoxy-1H-pyrazole-4-carboxylate (41%) and 2,3-dihydro-3-oxo-1H-pyrazole-4-carboxylic acid Et ester (37%). 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 alkoxypyrazole preparation, 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, 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, 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

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

On March 3, 2022, Grall-Ulsemer, Sandra; Guba, Wolfgang; Lerner, Christian; Li, Mingming; Liu, Yongqiang; Rudolph, Markus; Schmitt, Sebastien; Urner, Lorenz; Wang, Yongguang; Wang, Min; Wang, Jianhua; Yang, Song; Zhou, Chengang; Mattei, Patrizio published a patent.Formula: C4H6N2O The title of the patent was Imidazole-pyrazole derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazole-pyrazole derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases. Compounds of formula I wherein R1R2 are taken together to form substituted nitrogen-containing heterocyclyl; R1 is (un)substituted 3- to 14-membered heterocyclyl, (un)substituted 3- to 14-membered heterocyclyl-CO and (un)substituted 3- to 14-membered heterocyclyl-C1-6 alkyl; R2 is H and C1-6 alkyl; R3 is H, halo, C1-6 alkyl and C1-6 alkoxy; R4 and R6 are independently H, C1-6 alkyl, C1-6 alkoxy, CN, etc.; R5a, R5b and R5c are independently H, halo, OH, C1-6 alkyl, C1-6 alkoxy, etc.; R7 is H, C1-6 alkyl and C1-6 haloalkyl; A is 5- to 14-membered heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by methylation of N-(3-chloro-4-(4-(piperidine-4-carbonyl)piperazine-1-carbonyl)phenyl)-5-(1-(5-methoxypyridin-2-yl)-3-(trifluoromethyl)-pyrazol-4-yl)-1-methyl-imidazole-2-carboxamide with Me iodide. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.095μM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Formula: C4H6N2O

The Article related to imidazole pyrazole preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Formula: C4H6N2O

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

On March 10, 2022, Lerner, Christian; Li, Mingming; Liu, Yongqiang; Schmitt, Sebastien; Wang, Jianhua; Wang, Min; Wang, Yongguang; Yang, Song; Zhou, Chengang published a patent.COA of Formula: C4H6N2O The title of the patent was Preparation of imidazole-pyrazole derivatives with anti-bacterial properties. And the patent contained the following:

The invention provides imidazole pyrazole derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases. Compounds of formula I wherein R1R2 may be taken together to form substituted nitrogen-containing heterocycle; R1 is C1-6 alkyl, amino-C1-6 alkyl, amino-C1-6 alkoxy-C1-6 alkyl, etc.; R2 is H and C1-6 alkyl; R3 is H, halo, C1-6 alkyl and C1-6 alkoxy; R4 and R6 are independently H, C1-6 alkyl, C1-6 alkoxy, CN, etc.; R5a, R5b and R5c are H, halo, OH, C1-6 alkyl, C1-6 alkoxy, etc.; A is 5- to 14- membered heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II•HCO2H was prepared by arylation of tert-Bu 4-(4-(2-chloro-4-(1-methyl-5-(3-(trifluoromethyl)-1H-pyrazol-4-yl)-imidazole-2-carboxamido)benzoyl)piperazine-1-carbonyl)piperidine-1-carboxylate with 2-chloropyrimidine; the resulting tert-Bu 4-(4-(2-chloro-4-(1-methyl-5-(1-(pyrimidin-2-yl)-3-(trifluoromethyl)-pyrazol-4-yl)-imidazole-2-carboxamido)benzoyl)piperazine-1- carbonyl)piperidine-1-carboxylate underwent hydrolysis to give compound II•HCO2H. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.69μM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).COA of Formula: C4H6N2O

The Article related to imidazole pyrazole preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of Formula: C4H6N2O

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

On June 7, 2012, Crew, Andrew P.; Dong, Hanqing; Ferraro, Caterina; Sherman, Dan; Siu, Kam W. published a patent.Recommanded Product: 215610-30-3 The title of the patent was Macrocyclic phosphonates and phosphinates, fused with five- and six-membered nitrogen heterocycles as specific focal adhesion kinase inhibitors in cancer therapy. And the patent contained the following:

Macrocyclic phosphonates or phosphinates I, II [1, X = N, CH; A1 = C6H4, heteroarylene; A3 = heteroarylene, preferably, A3 = pyrazolediyl, triazolediyl, imidazolediyl; L2 = O, bond; L3 = C2-6 alkylene; L4 = C1-2 alkylene; Q1-Q4 = N, N-oxide, optionally substituted CH, Q1-Q4 may form a fused (hetero)cycle; R1-R3 = H, organyl, preferably, R1 = Cl, CN, NO2, CF3; R4 = OH, C1-4 alkyl, C3-6 cycloalkyl, C4-6 heterocyclyl, alkoxy], including resolved enantiomers thereof, and a pharmaceutically acceptable salts thereof, useful as selective focal adhesion kinase (FAK) inhibitors, beneficial in therapy of aggressive tumors, were prepared by intramol. esterification of acyclic phosphonate or phosphinate group with OH-containing linker A3 or by Suzuki coupling of pinacolboronate-containing linker A3 with halo-substituted (hetero)aryl ring. The prepared compounds 1 were tested for inhibition of phospho-FAK Y397 in the presence of human plasma, showing IC50 values, in general, less than 0.4 μM. In an example, the phosphonate II (1a, X = N, R1 = CF3, R2 = R3 = H, R4 = Et, R5 = OMe; L3 = (CH2)3, X1+X2 = CH2NMeCO) was prepared by esterification of 0.07 mmol of the acyclic phosphonate, sodium Et [4-[4-[[7-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-2-methyl-3-oxo-2,3-dihydro-1H-isoindol-4-yl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-3-methoxybenzylphosphonate in the presence of 0.3684 mmol of PYBOP and 0.4 mmol of DIPEA in 50 mL of 1,2-dichloroethane and 10 mL of DMF for 3 h at 20° with a 12% yield. In another example, the phosphonate 1a exhibited inhibitory activity towards phospho-FAK Y397 at a concentration <0.4 μM both in the plasma-free conditions and in the presence of human or murine plasma. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Recommanded Product: 215610-30-3

The Article related to phosphonate cyclic macrocyclic preparation focal adhesion kinase inhibition, antitumor agent macrocyclic phosphonate phosphinate focal adhesion kinase inhibition, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Recommanded Product: 215610-30-3

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

On August 11, 2016, Moussy, Alain; Benjahad, Abdellah; Pez, Didier; Sandrinelli, Franck; Martin, Jason; Picoul, Willy; Chevenier, Emmanuel published a patent.Computed Properties of 215610-30-3 The title of the patent was Preparation of phenylamino-oxazole or phenylamino-thiazole compounds with antitumor activity. And the patent contained the following:

The invention relates to compounds of formula I and pharmaceutical compositions thereof, useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases. I [wherein A = an optionally substituted heterocyclyl; B = aryl or heteroaryl; X = N, C-R6; R1, R2, R4, R5, and R6 independently = H, CN, CF3, etc.; R3 = H] or a pharmaceutically acceptable salt thereof, which are claimed and exemplified. Reaction of N-(5-methoxy-2-methylphenyl)acetamide with 5-[6-(1H-pyrazol-1-yl)pyridin-3-yl]-2-chlorooxazole provided example compound II in 68% yield. Candidate compounds of I were evaluated for antitumor activity in solid and hematol. tumor cells using CellTiter-Blue cell-based survival proliferation assay (data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Computed Properties of 215610-30-3

The Article related to phenylaminothiazole phenylaminooxazle antitumor malignancy, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Computed Properties of 215610-30-3

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

On December 6, 2007, Blom, Petra; Defert, Olivier; Kaletta, Titus; Leysen, Dirk Casimir Maria published a patent.Name: 5-Methoxy-1H-pyrazole The title of the patent was Preparation of thiazole and pyridinyl carboxamides and related heterocyclic analogs that interact with ion channels. And the patent contained the following:

Title compounds I [X = substituted thiazole, pyridine, oxopiperidine, etc.; R1 = H, halo, OH, NO2, alkyl, etc.; L1 = alkylene, cycloalkylene, pyrrolidinlenealkylene, etc.; m = 0-4], and their pharmaceutically acceptable salts, are prepared and disclosed as being capable of interacting with ion channels, in particular ion channels from the kv family. Thus, e.g., II was prepared by coupling of the corresponding 4-bromothiazole derivative (preparation given) with Ph boronic acid. Inhibition assays of the kv4.3 ion channel are described, e.g., II provided above 50% inhibition. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Name: 5-Methoxy-1H-pyrazole

The Article related to thiazole carboxamide derivative preparation ion channel modulator kv, pyridine carboxamide derivative preparation ion channel modulator kv, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: 5-Methoxy-1H-pyrazole

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

On April 1, 2022, Huang, Liye; Li, Hua; Liu, Huabin; Wang, Zhiyuan; Li, Tao; Ouyang, Feiyan; Zhang, Xinmiao published a patent.Quality Control of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of N-(3-(2-((1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)pyrrolidine-2-carboxamide derivatives as Jak1 kinase inhibitors. And the patent contained the following:

The invention discloses the preparation of N-(3-(2-((1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)pyrrolidine-2-carboxamide derivatives with general formula I as Jak1 kinase inhibitors wherein R1=H, halogen, substituted or unsubstituted C1-C6 linear or branched alkyl, substituted or unsubstituted C3-C6 cycloalkyl or ORa; R2=H, substituted or unsubstituted C1-C6 straight or branched chain alkyl, substituted or unsubstituted C3-C10 cycloalkyl, substituted or unsubstituted C2-C10 heterocycloalkyl; R3=H, halogen, cyano radical, unsubstituted or halogenated C1-C6 straight or branched chain alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl; R4=SO2Ra2, CORa2, COORa2, substituted or unsubstituted C3-C10 cycloalkyl, substituted or unsubstituted C2-C10 heterocycloalkyl; R5=F, cyano, C1-C6 straight or branched chain alkyl, C3-C6 cycloalkyl or ORa5; Ra, Ra2, Ra5=H, substituted or unsubstituted C1-C10 straight or branched chain alkyl, substituted or unsubstituted C2-C10 alkenyl, substituted or unsubstituted C2-C10 alkynyl, substituted or unsubstituted C3 -C10 cycloalkyl, substituted or unsubstituted C2-C10 heterocycloalkyl; R6=D, halogen, cyano, hydroxyl, unsubstituted or halogenated C1-C6 straight or branched chain alkyl, C2-C6 alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, C2-C6heterocycloalkyl, ORa6, SRa6, NRb6Rc6, CORa6, CONRb6Rc6, COORd6, SO2Ra6, SO2NRb6Rc6, NRb6CORa6, NRd6CONRb6Rc6, NRb6SO2Ra6, NRd6SO2NRb6Rc6 or SORa. For example, (S)-N-(3-(5-fluoro-2-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)-1-(methylsulfonyl)pyrrolidine-2-carboxamide was prepared from Me 3-methoxy-1H-pyrazole-4-carboxylate by hydrolysis, nitration, reduction, substitution reaction, amidation and so on. The title compounds have good inhibitory activity against Jak1 kinase and can be used to prepare drugs for the treatment of inflammation, autoimmune diseases or cancer. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Quality Control of 5-Methoxy-1H-pyrazole

The Article related to amidation preparation pyrimidine treatment human inflammation autoimmune disease cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 5-Methoxy-1H-pyrazole

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