Day: September 20, 2022

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. Category: pyrazoles-derivatives.

Goi, Takashi;Fukase, Koichi research published 《 Highly Efficient Coupling of Unstable Bicyclic Pyrimidines and Pyrazoles under Basic Conditions, and its Application to the Synthesis of Pharmaceutical Compounds》, the research content is summarized as follows. The efficient Pd-catalyzed coupling of unstable bicyclic pyrimidines and pyrazoles under basic conditions was established for the first time. The reactions proceeded with excellent yields without hydrolysis using Pd₂(dba)₃, ^tBuXPhos, and K₃PO₄.

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. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-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. Application In Synthesis of 2075-46-9.

Goi, Takashi;Fukase, Koichi research published 《 Highly Efficient Coupling of Unstable Bicyclic Pyrimidines and Pyrazoles under Basic Conditions, and its Application to the Synthesis of Pharmaceutical Compounds》, the research content is summarized as follows. The efficient Pd-catalyzed coupling of unstable bicyclic pyrimidines and pyrazoles under basic conditions was established for the first time. The reactions proceeded with excellent yields without hydrolysis using Pd₂(dba)₃, ^tBuXPhos, and K₃PO₄.

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

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. Related Products of 37622-90-5.

Goi, Takashi;Matsudaira, Tetsuji;Fukase, Koichi research published 《 Practical synthesis of 1-substituted 5-aminopyrazolo[4,3-d]pyrimidin-7-ones using intramolecular friedel-crafts type cyclization and its application to the synthesis of pharmaceutically active compounds》, the research content is summarized as follows. Intramol. Friedel-Crafts type cyclization is known as an efficient method of synthesizing fused bicyclic pyrimidones. However, the synthesis of 1-substituted pyrazolo[4,3-d]pyrimidin-7-ones using this cyclization method has not been achieved. Herein, authors describe the synthesis of various 1-substituted pyrazolo[4,3-d]pyrimidin-7-ones using practical intramol. Friedel-Crafts type cyclization, which was carried out in N,N-dimethylformamide in the presence of chlorotrimethylsilane. A hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD) inhibitor I was efficiently synthesized by this method.

Related Products of 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, 37622-90-5.

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. Product Details of C6H8N2O2.

Goi, Takashi;Nakajima, Tatsuo;Komatsu, Yoshiyuki;Kawata, Atsushi;Yamakoshi, Shuhei;Okada, Okimasa;Sugahara, Masakatsu;Umeda, Asami;Takada, Yoko;Murakami, Jun;Ohashi, Rikiya;Watanabe, Tomoko;Fukase, Koichi research published 《 Pyrazolo[4,3-d]pyrimidine Derivatives as a Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Domain Inhibitor for the Treatment of Anemia》, the research content is summarized as follows. Inhibition of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD) promotes erythropoietin (EPO) production by stabilizing the HIFα subunit. Thieno[2,3-d]pyrimidine 8 identified based on X-ray crystal structure anal. was optimized to lead to the discovery of pyrazolo[4,3-d]pyrimidine 13 as the lead compound of orally bioavailable HIF-PHD inhibitors. Conversion of the benzyl moiety in 13 gave pyrazolopyrimidine 19(I) with high solubility and bioavailability, which increased Hb levels in anemic model rats after repeated oral administration. It was shown that pyrazolo[4,3-d]pyrimidine derivatives are promising therapeutic agents for renal anemia through the inhibition of HIF-PHD.

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, Product Details of C6H8N2O2

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. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 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. Formula: C3H3N3O2.

Glinkerman, Christopher M.;Boger, Dale L. research published 《 Synthesis, Characterization, and Rapid Cycloadditions of 5-Nitro-1,2,3-triazine》, the research content is summarized as follows. The synthesis, characterization, and a study of the cycloaddition reactions of 5-nitro-1,2,3-triazine (I) are reported. The electron-deficient nature of I permits rapid cycloaddition with a variety of electron-rich dienophiles, including amidines, enamines, enol ethers, ynamines, and ketene acetals in high to moderate yields. ¹H NMR studies of a representative cycloaddition reaction between I and an amidine revealed a remarkable reaction rate and efficiency (1 mM, <60 s, CD₃CN, 23°, >95%).

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., Formula: C3H3N3O2

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.

Gimeno-Fonquernie, Pol;Liang, Weibin;Albalad, Jorge;Kuznicki, Andrew;Price, Jason R.;Bloch, Eric D.;Doonan, Christian J.;Sumby, Christopher J. research published 《 Templated synthesis of zirconium(IV)-based metal-organic layers (MOLs) with accessible chelating sites》, the research content is summarized as follows. Metal-organic layers (MOLs) are of great interest in heterogeneous catalysis, particularly materials that can accommodate extraneous metal centers. Here, the authors demonstrate a two-step preorganisation/delamination synthetic strategy using CuI as a template to prepare Zr-based MOLs with accessible ‘syn’ bis-pyrazolyl chelating sites (named UAM-2·ns) that are poised for quant. post-synthetic metalation with late transition metals.

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 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. SDS of cas: 269410-08-4.

Gilles, Philippe;Kashyap, Rudra S.;Freitas, Maria Joao;Ceusters, Sam;Van Asch, Koen;Janssens, Anke;De Jonghe, Steven;Persoons, Leentje;Cobbaut, Mathias;Daelemans, Dirk;Van Lint, Johan;Voet, Arnout R. D.;De Borggraeve, Wim M. research published 《 Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors》, the research content is summarized as follows. Novel pyrazolo[3,4-d]pyrimidine based pan-PKD inhibitors I [R¹ = tBu, 3,3-dimethylbutyl, Bn, etc.; R² = pyrrol-3-yl, indol-3-yl, naphthalen-1-yl, etc.] with structural variety at position 1 were synthesized and evaluated for biol. activity. Compounds I were evaluated for PKD inhibition against full length PKD using Promega’s ADP-Glo^TM kinase activity assay and syntide-2 as a substrate. Starting from compound I [R¹ = tBu; R² = indol-3-yl] a known PKD inhibitor with IC₅₀ values in the range of 94-108 nM, compound I [R¹ = (piperidin-4-yl)methyl; R² = indol-3-yl] was identified with an improved biochem. inhibitory activity against PKD (IC₅₀ = 17-35 nM). Subsequent cellular assays demonstrated that compounds I [R¹ = tBu, (piperidin-4-yl)methyl; R² = indol-3-yl] inhibited PKD-dependent cortactin phosphorylation. Furthermore, the biochem. inhibitory activity of I [R¹ = tBu; R² = indol-3-yl] and 1-NM-PP1 against CAMKIIα and PKCδ was investigated and no notable inhibition was observed at compound concentrations of 1 and 10μM. Some of the synthesized PKD inhibitor compounds I [R¹ = tBu, (piperidin-4-yl)methyl, 2,2-dimethyl-propan-1-ol, (1-Me-piperidin-4-yl)methyl; R² = indol-3-yl, 1-Me-indol-3-yl, 2-ethoxyquinolin-6-yl] and some known PKD inhibitors (CRT0066101, 1-NM-PP1) were evaluated for their antitumor activity in a panel of eight different cancer cell lines. A screening against different cancer cell lines demonstrated that compound I [R¹ = tBu; R² = indol-3-yl] was potent and versatile antitumoral agent.

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., SDS of cas: 269410-08-4

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

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Electric Literature of 2075-46-9.

Ghosh, Tubai;Maity, Pintu;Ranu, Brindaban C. research published 《 Cobalt-Copper Catalyzed C(sp2) – N Cross Coupling of Amides or Nitrogenated Heterocycles with Styrenyl or Aryl Halides》, the research content is summarized as follows. An efficient C(sp2)-N-cross coupling of cyclic and acyclic amides with styrenyl/aryl/heteroaryl halides catalyzed by cobalt acetylacetonate in combination with copper(I) iodide was achieved. A library of diversely substituted cyclic and acyclic enamides were obtained in high yields by this procedure. The reaction was stereoselective producing (E)-enamides from trans-styrenyl halides and (Z)-products from cis-halides. This procedure was successfully employed for the coupling of other N-heterocycles such as pyrazole, imidazole and triazole with aryl/styrenyl/heteroaryl halides to produce the corresponding N-coupled products. A probable mechanism was suggested.

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., Electric Literature of 2075-46-9

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

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. Name: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Ghosh, Prithwish;Byun, Youjung;Kwon, Na Yeon;Kang, Ju Young;Mishra, Neeraj Kumar;Park, Jung Su;Kim, In Su research published 《 Reactivity of triplet diradical intermediates in aqueous media for transition-metal-free Csp²-H alkylation》, the research content is summarized as follows. Herein, a distinct reaction pathway involving triplet diradical intermediates in the coupling reaction between alkyl pyridinium ylides and electrophilic N-heterocyclic mols. was reported. Alkyl pyridinium ylides generated from alkyl pyridinium salts under basic aqueous conditions underwent addition into iminoamido N-heterocycles, generating triplet diradical intermediates lead to C-H alkylated N-heterocycles I [R = Me, Bn, 2-pyridyl, etc.; R¹ = Br, Ph, 2-thienyl, etc.; R² = Bn, CH₂-2-FC₆H₄, CH₂-2-naphthyl, etc.], II [R³ = Me, allyl, iPr, etc.; R⁴ = H, Cl; R⁵ = Bn, CH₂-4-MeOC₆H₄, CH₂-2-furyl, etc.; X = CH, N] and III [R⁶ = Me, 3-MeC₆H₄; R⁷ = Ph, Bn, 4-EtOC₆H₄, etc.]. The proposed reaction mechanism was supported by ESR and radical scavenging experiments Notably, a wide substrate scope and excellent level of functional group tolerance were attained under cost-effective and straightforward conditions, which revealed the amenability of this protocol in the pharmaceutical and chem. industries. These results were of significant relevance to the organic and medicinal chemists because of the handling simplicity, broad substrate scope, high efficiency, excellent chemoselectivity and the environmentally friendly conditions of the developed methodol.

Name: 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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. 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. Application In Synthesis of 761446-44-0.

Gerstenberger, Brian S.;Ambler, Catherine;Arnold, Eric P.;Banker, Mary-Ellen;Brown, Matthew F.;Clark, James D.;Dermenci, Alpay;Dowty, Martin E.;Fensome, Andrew;Fish, Susan;Hayward, Matthew M.;Hegen, Martin;Hollingshead, Brett D.;Knafels, John D.;Lin, David W.;Lin, Tsung H.;Owen, Dafydd R.;Saiah, Eddine;Sharma, Raman;Vajdos, Felix F.;Xing, Li;Yang, Xiaojing;Yang, Xin;Wright, Stephen W. research published 《 Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases》, the research content is summarized as follows. Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal transduction downstream of receptors for the IL-23/IL-12 pathways and type I interferon family, where it pairs with JAK2 or JAK1, resp. On the basis of human genetic and emerging clin. data, a selective TYK2 inhibitor provides an opportunity to treat autoimmune diseases delivering a potentially differentiated clin. profile compared to currently approved JAK inhibitors. The discovery of an ATP-competitive pyrazolopyrazinyl series of TYK2 inhibitors was accomplished through computational and structurally enabled design starting from a known kinase hinge binding motif. With understanding of PK/PD relationships, a target profile balancing TYK2 potency and selectivity over off-target JAK2 was established. Lead optimization involved modulating potency, selectivity, and ADME properties which led to the identification of the clin. candidate PF-06826647 (22).

Application In Synthesis of 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%., 761446-44-0.

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