Category: pyrazoles-derivatives

On June 24, 2021, Liu, Bo; Cotesta, Simona; Gerspacher, Marc; Leblanc, Catherine; Lorthiois, Edwige Liliane Jeanne; Machauer, Rainer; Mah, Robert; Mura, Christophe; Rigollier, Pascal; Schneider, Nadine; Stutz, Stefan; Vaupel, Andrea; Warin, Nicolas; Wilcken, Rainer published a patent.Product Details of 2089292-88-4 The title of the patent was Pyrazole derivatives as anti-cancer agents and preparation. And the patent contained the following:

The invention relates compounds of formula I, us as anti-cancer agents in the ability to inhibit KRASG12C and their preparation Compound I, wherein A is (un)substituted C5-7, (un)substituted C5-10, (un)substituted 5- to 7-membered unsaturated heterocyclyl containing one carbon-carbon double bond and one oxygen, etc.; B selected from the group of B1 and B2; B1 is (un)substituted C6-10 with 1, 2, 3 and 4 RBa; B2 is 6- to 13-membered heteroaryl containing 1, 2 and 3 nitrogen atoms and is (un)substituted 1, 2, 3 and 4 RBb; each RBa is independently hydroxy, C1-4 alkyl, halo, etc.; each RBb is independently C1-4 alkyl; cyclopropyl, halo, etc.; C is hydrogen, C1-3 alkyl, C3-5 cycloalkyl, etc.; L is (un)substituted 2-azaspiro[3.3]heptanyl, (un)substituted 2-azaspiro[3.4]heptanyl, pyrrolidine, etc.; D is (un)substituted prop-2-en-1-one, (un)substituted prop-2-yn-1-one, etc.; and stereoisomers, atropisomers, pharmaceutically acceptable salts, thereof, are claimed. Conmpound II was prepared using a multistep procedure (procedure given). Compound II was evaluated for KRAS G12C inhibitory activity yielding an IC50 of 0.017μM. Compounds of the invention were evaluated for KRAS G12C inhibitory activity (data given). The experimental process involved the reaction of 5-Bromo-2-methyl-2H-pyrazolo[3,4-c]pyridine(cas: 2089292-88-4).Product Details of 2089292-88-4

The Article related to pyrazole preparation cancer kras inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Product Details of 2089292-88-4

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

On April 21, 2011, Bretschneider, Thomas; Voerste, Arnd; Fuesslein, Martin; Koehler, Adeline; Goergens, Ulrich published a patent.Reference of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Amides and thioamides as pesticides and their preparation. And the patent contained the following:

The invention relates to amides and thioamides of formula I, to a method for the production thereof, and to the use thereof for combating pests. Compounds of formula I wherein G is N, CH, C-halo, C-NO2, C-CN, etc.; R1 is H, alkyl, haloalkyl, cycloalkyl, halo, etc.; X is O and S; R2 is H, alkyl, haloalkyl, alkoxy, etc.; R3 is H, alkyl, haloalkyl, cyanoalkyl, alkenyl, etc.; and their salts and N-oxides thereof, are claimed. Example compound II was prepared by N-arylation of pyrazole-4-carbonitrile with 3-bromopyridine; the resulting 1-(pyridin-3-yl)-1H-pyrazole-4-carbonitrile underwent hydrolysis to give the corresponding carboxylic acid, which underwent chlorination to give the corresponding carboxylic acid chloride hydrochloride, which underwent amidation with ethylamine to give compound II. All the invention compounds were evaluated for their pesticidal activity (some data given). The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Reference of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

The Article related to amide thioamide preparation pesticide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

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

On January 6, 2016, Lian, Lei; Zheng, Yurong; He, Bin; Peng, Xuegang; Jin, Tao; Cui, Qi published a patent.Safety of 5-Methoxy-1H-pyrazole The title of the patent was Pyrazole ketone compound or salt thereof, preparation method, herbicidal composition and application. And the patent contained the following:

The inventive pyrazole ketone compound has structure shown as general formula I, wherein R1R2N represents (un)substituted 3-8 membered nitrogen-containing heterocyclic group containing 1-3 hetero atoms, or R1 and R2 are independently H, alkyl, heteroalkyl, etc.; R3 is H, alkyl, alkenyl, alkynyl, cycloalkyl or alkyl substituted cycloalkyl; R4 is Me, Et, Pr, iso-Pr, or cyclopropyl; X is H, S(O)nR6, R7, or (substituted) 3-8 membered heterocyclic group containing 1-4 hetero atoms, n is 1, 2 or 3; R6 is (un)substituted alkyl or aryl, R7 is (un)substituted alkyl, aryl, alkanoyl or aroyl. Compounds of the invention were prepared and evluated for their herbicidal activity on various crops (data given). The pyrazole ketone compound has good herbicidal effect, convenient application, low cost, and high com. value. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Safety of 5-Methoxy-1H-pyrazole

The Article related to pyrazole ketone preparation herbicide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Safety of 5-Methoxy-1H-pyrazole

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

On May 11, 2017, Lian, Lei; Zheng, Yurong; He, Bin; Peng, Xuegang; Jin, Tao; Cui, Qi published a patent.Computed Properties of 215610-30-3 The title of the patent was Pyrazole ketone compound or salt thereof, preparation method, herbicidal composition and application. And the patent contained the following:

The inventive pyrazole ketone compound has structure shown as general formula I, wherein R1R2N represents (un)substituted 3-8 membered nitrogen-containing heterocyclic group containing 1-3 hetero atoms, or R1 and R2 are independently H, alkyl, heteroalkyl, etc.; R3 is H, alkyl, alkenyl, alkynyl, cycloalkyl or alkyl substituted cycloalkyl; R4 is Me, Et, Pr, iso-Pr, or cyclopropyl; X is H, S(O)nR6, R7, or (substituted) 3-8 membered heterocyclic group containing 1-4 hetero atoms, n is 1, 2 or 3; R6 is (un)substituted alkyl or aryl, R7 is (un)substituted alkyl, aryl, alkanoyl or aroyl. Compounds of the invention were prepared and evaluated for their herbicidal activity on various crops (data given). The pyrazole ketone compound has good herbicidal effect, convenient application, low cost, and high com. value. 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 pyrazole ketone preparation herbicide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 215610-30-3

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

On February 11, 2010, Janin, Yves; Guillou, Sandrine published a patent.Computed Properties of 215610-30-3 The title of the patent was Preparation of alkoxypyrazoles. And the patent contained the following:

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).Computed Properties of 215610-30-3

The Article related to alkoxypyrazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 215610-30-3

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

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

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

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

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, 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