pyrazoles-derivatives

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Reference of 761446-44-0.

Ji, Zhiqin;Clark, Richard F.;Bhat, Vikram;Matthew Hansen, T.;Lasko, Loren M.;Bromberg, Kenneth D.;Manaves, Vlasios;Algire, Mikkel;Martin, Ruth;Qiu, Wei;Torrent, Maricel;Jakob, Clarissa G.;Liu, Hong;Cole, Philip A.;Marmorstein, Ronen;Kesicki, Edward A.;Lai, Albert;Michaelides, Michael R. research published 《 Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases》, the research content is summarized as follows. P300 and CREB-binding protein (CBP) are essential for a multitude of cellular processes. Dysregulation of p300/CBP histone acetyltransferase activity is linked to a broad spectrum of human diseases including cancers. A novel drug-like spirohydantoin (21) has been discovered as a selective orally bioavailable inhibitor of p300/CBP histone acetyltransferase. Lead compound 21 is more potent than the first-in-class lead A-485 in both enzymic and cellular assays and lacks the off-target inhibition of dopamine and serotonin transporters, that was observed with A-485.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Reference of 761446-44-0

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

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Electric Literature of 269410-08-4.

Ji, Hong;Wu, Li-Yang;Cai, Jiang-Hong;Li, Guo-Rong;Gan, Na-Na;Wang, Zhao-Hua research published 《 Room-temperature borylation and one-pot two-step borylation/Suzuki-Miyaura cross-coupling reaction of aryl chlorides》, the research content is summarized as follows. A highly efficient room-temperature borylation strategy of aryl chlorides is described. Utilizing Buchwald’s second-generation preformed catalyst, boronate esters were obtained for a wide range of substrates in high yield. The method was also applied to Suzuki-Miyaura cross-coupling reaction in a one-pot two-step sequential manner, providing a facile and convenient access to the direct synthesis of biaryl compounds from aryl chlorides.

269410-08-4, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, also known as 4-Pyrazoleboronic acid pinacol ester , is a useful research compound. Its molecular formula is C9H15BN2O2 and its molecular weight is 194.04 g/mol. The purity is usually 95%.

4-Pyrazoleboronic acid pinacol ester is a useful reagent for Suzuki-Miyaura cross-couplings as well as Ruthenium-catalyzed asymmetric hydrogenation. 4-Pyrazoleboronic acid pinacol ester is also a useful reagent for preparing VEGF, Aurora, RHO (ROCK), Janus Kinase 2, c-MET, ALK, S-nitrsoflutathione reductase, CDC7, Acetyl-CoA carboxylase inhibitors.

4-Pyrazoleboronic acid pinacol ester is used in the preparation of Rho kinase (ROCK) inhibitors as wella s other biologically active compounds.

4-Pyrazoleboronic acid pinacol ester is an organic compound that is the product of a bifunctional coupling reaction between 4-pyrazolecarboxylic acid and pinacol. It has been shown to inhibit protein S6 kinase, which is involved in the regulation of cell growth and proliferation. This compound has also been shown to be effective against cancer cells, including those that are resistant to conventional chemotherapeutic drugs. 4-Pyrazoleboronic acid pinacol ester may also be used as a precursor for other compounds with pharmaceutical activity., Electric Literature of 269410-08-4

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Application of C9H15BN2O2.

Ji, Hong;Cai, Jianghong;Gan, Nana;Wang, Zhaohua;Wu, Liyang;Li, Guorong;Yi, Tao research published 《 Palladium-catalyzed borylation of aryl (pseudo)halides and its applications in biaryl synthesis》, the research content is summarized as follows. A facile and efficient palladium-catalyzed borylation of aryl (pseudo)halides at room temperature has been developed. Arylboronic esters were expeditiously assembled in good yields and with a broad substrate scope and good functional group compatibility. This approach has been successfully applied to the one-pot two-step borylation/ Suzuki-Miyaura cross-coupling reaction, providing a concise access to biaryl compounds from readily available aryl halides. Furthermore, a parallel synthesis of biaryl analogs is accomplished at room temperature using the strategy, which enhances the practical usefulness of this method.

Application of C9H15BN2O2, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, also known as 4-Pyrazoleboronic acid pinacol ester , is a useful research compound. Its molecular formula is C9H15BN2O2 and its molecular weight is 194.04 g/mol. The purity is usually 95%.

4-Pyrazoleboronic acid pinacol ester is a useful reagent for Suzuki-Miyaura cross-couplings as well as Ruthenium-catalyzed asymmetric hydrogenation. 4-Pyrazoleboronic acid pinacol ester is also a useful reagent for preparing VEGF, Aurora, RHO (ROCK), Janus Kinase 2, c-MET, ALK, S-nitrsoflutathione reductase, CDC7, Acetyl-CoA carboxylase inhibitors.

4-Pyrazoleboronic acid pinacol ester is used in the preparation of Rho kinase (ROCK) inhibitors as wella s other biologically active compounds.

4-Pyrazoleboronic acid pinacol ester is an organic compound that is the product of a bifunctional coupling reaction between 4-pyrazolecarboxylic acid and pinacol. It has been shown to inhibit protein S6 kinase, which is involved in the regulation of cell growth and proliferation. This compound has also been shown to be effective against cancer cells, including those that are resistant to conventional chemotherapeutic drugs. 4-Pyrazoleboronic acid pinacol ester may also be used as a precursor for other compounds with pharmaceutical activity., 269410-08-4.

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Application In Synthesis of 2075-46-9.

Jakubczyk, Michal;Mkrtchyan, Satenik;Madura, Izabela D.;Marek, Paulina H.;Iaroshenko, Viktor O. research published 《 Copper-catalyzed direct C-H arylselenation of 4-nitro-pyrazoles and other heterocycles with selenium powder and aryl iodides. Access to unsymmetrical heteroaryl selenides》, the research content is summarized as follows. A one-pot, Cu-catalyzed direct C-H arylselenation protocol using elemental Se and aryl iodides was developed for nitro-substituted, N-alkylated pyrazoles, imidazoles and other heterocycles including 4H-chromen-4-one. This general and concise method allows one to obtain a large number of unsym. heteroaryl selenides bearing a variety of substituents. The presence of the nitro group was confirmed to be essential for the C-H activation and can also be used for further functionalisation and manipulation. Several examples of heteroannulated benzoselenazines were also synthesized using the developed synthetic protocol.

Application In Synthesis of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Formula: C6H8N2O2.

Iskauskiene, Monika;Ragaite, Greta;Sloek, Frank A.;Sackus, Algirdas research published 《 Facile synthesis of novel amino acid-like building blocks by N-alkylation of heterocyclic carboxylates with N-Boc-3-iodoazetidine》, the research content is summarized as follows. An efficient protocol providing easy access to highly functionalized heterocyclic compounds as novel organic building blocks was developed by coupling alkyl pyrazole-, indazole- and indolecarboxylates with N-Boc-3-iodoazetidine. The synthesized compounds were representatives of constrained non-chiral synthetic azole carboxylates in their N-Boc protected ester forms. Diversification of the prepared heterocyclic building blocks was achieved via application of palladium-catalyzed Suzuki-Miyaura cross-coupling reactions. In total, 34 building blocks were obtained to form a highly diversified small mol. collection. The structure of the novel heterocyclic compounds was investigated and verified by advanced NMR spectroscopy methods.

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Formula: C6H8N2O2

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

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Recommanded Product: Ethyl 4-pyrazolecarboxylate.

Ichikawa, Masanori;Ohtsuka, Masami;Ohki, Hitoshi;Ota, Masahiro;Haginoya, Noriyasu;Itoh, Masao;Shibata, Yoshihiro;Ishigai, Yutaka;Terayama, Koji;Kanda, Akira;Sugita, Kazuyuki research published 《 Discovery of DF-461, a Potent Squalene Synthase Inhibitor [Erratum to document cited in CA159:478473]》, the research content is summarized as follows. The authors present a corrected author list based on reconsideration and re-evaluation of each author’s contribution.

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Recommanded Product: Ethyl 4-pyrazolecarboxylate

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Category: pyrazoles-derivatives.

Ichikawa, Masanori;Ohtsuka, Masami;Ohki, Hitoshi;Ota, Masahiro;Haginoya, Noriyasu;Itoh, Masao;Shibata, Yoshihiro;Ishigai, Yutaka;Terayama, Koji;Kanda, Akira;Sugita, Kazuyuki research published 《 Discovery of DF-461, a Potent Squalene Synthase Inhibitor》, the research content is summarized as follows. We report the development of a new trifluoromethyltriazolobenzoxazepine series of squalene synthase inhibitors. Structure-activity studies and pharmacokinetics optimization on this series led to the identification of compound 23 (DF-461), which exhibited potent squalene synthase inhibitory activity, high hepatic selectivity, excellent rat hepatic cholesterol synthesis inhibitory activity, and plasma lipid lowering efficacy in nonrodent repeated dose studies.

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Category: pyrazoles-derivatives

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Category: pyrazoles-derivatives.

Hunter, James H.;Prendergast, Lisa;Valente, Louis F.;Madin, Andrew;Pairaudeau, Garry;Waring, Michael J. research published 《 High Fidelity Suzuki-Miyaura Coupling for the Synthesis of DNA Encoded Libraries Enabled by Micelle Forming Surfactants》, the research content is summarized as follows. DNA encoded chem. libraries provide a highly efficient means of screening vast numbers of small mols. against an immobilized protein target. Their potential is currently restricted by the constraints of carrying out library synthesis in the presence of attached DNA tags, for which a limited number of reactions and substrates can be used. Even established reactions, such as Suzuki-Miyaura couplings, do not give efficient coupling reactions across a wide range of substrates and can lead to significant DNA degradation We developed an efficient protocol for carrying out Suzuki-Miyaura couplings on DNA tagged substrates that proceeds with unprecedented efficiency to the desired biaryl products (>98% on average with no detectable DNA degradation) across a wide range of drug-like substrates using a micellar promoted process with com. TPGS-750-M surfactant. We have demonstrated the applicability of this method in DEL synthesis by preparing a prototypical two-dimensional 36-member library employing the Suzuki-Miyaura coupling methodol. as the final library synthesis step. This work shows, for the first time, that standard micellar surfactants can promote reactions for encoded library synthesis, leading to libraries of exceptional fidelity, and demonstrates the potential to expand the range of accessible DNA compatible chem.

Category: pyrazoles-derivatives, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, also known as 4-Pyrazoleboronic acid pinacol ester , is a useful research compound. Its molecular formula is C9H15BN2O2 and its molecular weight is 194.04 g/mol. The purity is usually 95%.

4-Pyrazoleboronic acid pinacol ester is a useful reagent for Suzuki-Miyaura cross-couplings as well as Ruthenium-catalyzed asymmetric hydrogenation. 4-Pyrazoleboronic acid pinacol ester is also a useful reagent for preparing VEGF, Aurora, RHO (ROCK), Janus Kinase 2, c-MET, ALK, S-nitrsoflutathione reductase, CDC7, Acetyl-CoA carboxylase inhibitors.

4-Pyrazoleboronic acid pinacol ester is used in the preparation of Rho kinase (ROCK) inhibitors as wella s other biologically active compounds.

4-Pyrazoleboronic acid pinacol ester is an organic compound that is the product of a bifunctional coupling reaction between 4-pyrazolecarboxylic acid and pinacol. It has been shown to inhibit protein S6 kinase, which is involved in the regulation of cell growth and proliferation. This compound has also been shown to be effective against cancer cells, including those that are resistant to conventional chemotherapeutic drugs. 4-Pyrazoleboronic acid pinacol ester may also be used as a precursor for other compounds with pharmaceutical activity., 269410-08-4.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Recommanded Product: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Huhn, Annissa J.;Gardberg, Anna S.;Poy, Florence;Brucelle, Francois;Vivat, Valerie;Cantone, Nico;Patel, Gaurav;Patel, Chirag;Cummings, Richard;Sims, Robert;Levell, Julian;Audia, James E.;Bommi-Reddy, Archana;Wilson, Jonathan E. research published 《 Early Drug-Discovery Efforts towards the Identification of EP300/CBP Histone Acetyltransferase (HAT) Inhibitors》, the research content is summarized as follows. EP300 and CBP (KAT3A/3B) are two highly homologous, multidomain, epigenetic coregulators that play central roles in transcription through the acetylation of lysine residues on histones and other proteins. Both enzymes have been implicated in human diseases, especially cancer. From a high-throughput screen of 191 000 compounds searching for EP300/CBP histone acetyltransferase (HAT) inhibitors, 18 compounds were characterized by a suite of biochem. enzymic assays and biophys. methods, including X-ray crystallog. and native mass spectrometry. This work resulted in the discovery of three distinct mechanistic classes of EP300/CBP HAT inhibitors, including two classes not previously described. The profiles of an example of each class of inhibitor are described in detail. A subsequent medicinal chem. effort led to the development of a novel class of orally bioavailable AcCoA-competitive EP300/CBP HAT inhibitors with in vivo activity. We believe that this work will prove to be a useful guide for other groups interested in the development of HAT inhibitors.

Recommanded Product: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Recommanded Product: Ethyl 4-pyrazolecarboxylate.

Huang, Qi;Tran, Gael;Gomez Pardo, Domingo;Tsuchiya, Tomoki;Hillebrand, Stefan;Vors, Jean-Pierre;Cossy, Janine research published 《 Palladium-catalyzed phosphonylation of pyrazoles substituted by electron-withdrawing groups》, the research content is summarized as follows. A series of bromopyrazoles substituted by electron-withdrawing groups such as an ester, a trifluoromethyl group or a cyano group was involved in Pd-catalyzed phosphonylation. Moderate to good yields were obtained in the corresponding phosphonylated pyrazoles.

Recommanded Product: Ethyl 4-pyrazolecarboxylate, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, 37622-90-5.

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