Category: pyrazoles-derivatives

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. Product Details of C9H15BN2O2.

Abdelsamie, Ahmed S.;Salah, Mohamed;Siebenbuerger, Lorenz;Hamed, Mostafa M.;Boerger, Carsten;van Koppen, Chris J.;Frotscher, Martin;Hartmann, Rolf W. research published 《 Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17β-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation》, the research content is summarized as follows. Estrogens are the major female sex steroid hormones, estradiol (E2) being the most potent form in humans. Disturbing the balance between E2 and its weakly active oxidized form estrone (E1) leads to diverse types of estrogen-dependent diseases such as endometriosis or osteoporosis. 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the biosynthesis of E2 by reduction of E1 while the type 2 enzyme catalyzes the reverse reaction. Thus, 17β-HSD1 and 17β-HSD2 are attractive targets for treatment of estrogen-dependent diseases. Recently, we reported the first proof-of-principle study of a 17β-HSD2 inhibitor in a bone fracture mouse model, using s.c. administration. In the present study, our aim was to improve the in vitro ADME profile of the most potent 17β-HSD1 and 17β-HSD2 inhibitors described so far. The optimized compounds show strong and selective inhibition of both the human enzymes and their murine orthologs. In addition, they display good metabolic stability in human liver microsomes (S9 fraction), low in vitro cytotoxicity as well as better aqueous solubility and physicochem. properties compared to the lead compounds These achievements make the compounds eligible for testing in preclin. in vivo animal model studies on the effects of inhibition of 17β-HSD1 and 17β-HSD2.

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., Product Details of C9H15BN2O2

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. Quality Control of 761446-44-0.

Adlington, Neil K.;Agnew, Lauren R.;Campbell, Andrew D.;Cox, Robert J.;Dobson, Andrew;Barrat, Cristina Fernandez;Gall, Malcolm A. Y.;Hicks, William;Howell, Gareth P.;Jawor-Baczynska, Anna;Miller-Potucka, Lucie;Pilling, Michael;Shepherd, Katy;Tassone, Ross;Taylor, Brian A.;Williams, Aled research published 《 Process Design and Optimization in the Pharmaceutical Industry: A Suzuki-Miyaura Procedure for the Synthesis of Savolitinib》, the research content is summarized as follows. A process for the Suzuki-Miyaura coupling reaction on multihundred kilogram scale as the final step in the preparation of the potential antitumor agent savolitinib I is developed. The optimization of catalyst and solvent for the process, the kinetics of the Suzuki-Miyaura coupling, the dependence of byproduct formation on solvent, temperature, and catalyst loading, and the development of procedures for the removal of palladium residues from the product and for the recrystallization of the unsolvated product as the desired form I are discussed. The requirements for and constraints on the large scale preparation of an active pharmaceutical ingredient are discussed.

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%., Quality Control of 761446-44-0

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

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (1H-Imidazol-2-yl)methanamine dihydrochloride( cas:22600-77-7 ) is researched.Computed Properties of C4H9Cl2N3.Casagrande, Manolo; Barteselli, Anna; Basilico, Nicoletta; Parapini, Silvia; Taramelli, Donatella; Sparatore, Anna published the article 《Synthesis and antiplasmodial activity of new heteroaryl derivatives of 7-chloro-4-aminoquinoline》 about this compound( cas:22600-77-7 ) in Bioorganic & Medicinal Chemistry. Keywords: quinoline heteroarylmethylamino heteroarylamino preparation antiplasmodial activity; antimalarial aminoquinoline chloro preparation. Let’s learn more about this compound (cas:22600-77-7).

With the aim to investigate the effect of different heterocyclic rings linked to the 4-aminoquinoline nucleus on the antimalarial activity, a set of 7-chloro-4-(heteroarylmethylamino)quinoline and 7-chloro-4-(heteroarylamino)quinoline derivatives was synthesized and tested in vitro against D-10 (CQ-S) and W-2 (CQ-R) strains of Plasmodium falciparum. All compounds exhibited from moderate to high antiplasmodial activities. The activity was strongly influenced both by the presence of a methylenic group, as a spacer between the 4-aminoquinoline and the heterocyclic ring, and by the presence of a basic head. The most potent mols. inhibited the growth of both CQ-S and CQ-R strains of P. falciparum with IC50 < 30 nM and were not toxic against human endothelial cells. These results confirm that the presence of an heteroaryl moiety in the side chain of 7-chloro-4-aminoquinoline is useful for the design and development of new powerful antimalarial agents. This compound((1H-Imidazol-2-yl)methanamine dihydrochloride)Computed Properties of C4H9Cl2N3 was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

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

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Sodium 6-hydroxy-5-((2-methoxy-5-methyl-4-sulfonatophenyl)diazenyl)naphthalene-2-sulfonate( cas:25956-17-6 ) is researched.Related Products of 25956-17-6.Cotes, Sandra; LLinas, Humberto; Arrieta, Julio; Espinosa, Alberto published the article 《Evaluation of FD&C Red Number 40 dye concentration and type of gelatin in the dissolution of gelatin sheets》 about this compound( cas:25956-17-6 ) in Journal of Pharmaceutical Sciences and Research. Keywords: gelatin red dye dissolution crosslinking. Let’s learn more about this compound (cas:25956-17-6).

To study the relationship between the type of gelatin and dye concentration in relation to crosslinking in soft capsules. Two types of gelatin, bovine RXL type B 130 Bloom and pig NF type B 150 Bloom, and three concentrations of FD&C Red 40 dye were used in six pre-formulations in six replicates, each for a total of thirty-six trials. Each pre-formulation was analyzed by a sample dissolution test under conditions of natural stability and of 21 days. Using the logistic regression model, it was found that the type of gelatin and dye concentration were statistically significant, while the interactions between them showed no significance. The use of the RXL type B 130 Bloom gelatin in pre-formulation of soft gelatin capsules increases the probability of success with non-crosslinking.

《Evaluation of FD&C Red Number 40 dye concentration and type of gelatin in the dissolution of gelatin sheets》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(Sodium 6-hydroxy-5-((2-methoxy-5-methyl-4-sulfonatophenyl)diazenyl)naphthalene-2-sulfonate)Related Products of 25956-17-6.

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

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Chemistry of Bifunctional Photoprobes. 6. Synthesis and Characterization of High Specific Activity Metalated Photochemical Probes: Development of Novel Rhenium Photoconjugates of Human Serum Albumin and Fab Fragments, published in 2002-09-20, which mentions a compound: 22600-77-7, mainly applied to azathiaalkaneone azidofluorophenyl functionalized preparation; rhenium triazathiaalkanetrione azidofluorophenyl functionalized complex preparation photolysis amine; human serum albumin labeling rhenium triazathiaalkanetrione azidofluorophenyl functionalized complex; antibody labeling rhenium triazathiaalkanetrione azidofluorophenyl functionalized complex, Computed Properties of C4H9Cl2N3.

Functionalization of perfluoro aryl azides by bifunctional chelating agents (BFCAs) capable of forming high specific activity complexes with 99mTc (for γ-imaging) and 188Re (for radiotherapy) is described. The synthesis of multidonor BFCAs containing N2S2, N4, and N3S donor groups containing imidazole, pyridine, and pyrazine functionalities that may be important for tuning the pharmacokinetic parameters is also described. Functionalization of perfluoro aryl azides at various sites on BFCAs yields novel bifunctional photolabile chelating agents (BFPCAs) that are useful for covalent attachment to biomols. A representative Re-BFPCA I as the Me4N+ salt in a model solvent, diethylamine, proceeded to give a high yield of intermol. NH insertion product without the decomplexation of the metal ion from I. All products originated from the photolysis of I in diethylamine were characterized by anal. techniques, and a plausible mechanism of formation of different photolytic products is suggested. The high yield of intermol. NH insertion of I is extended to labeling of human serum albumin (HSA) and Fab fragments under aqueous conditions. The photolabeling technol. developed here offers a new way to attach diagnostically and therapeutically useful radiotracers (e.g., 99mTc, 188Re) to Fab fragments for potential noninvasive imaging and therapy of cancer.

《Chemistry of Bifunctional Photoprobes. 6. Synthesis and Characterization of High Specific Activity Metalated Photochemical Probes: Development of Novel Rhenium Photoconjugates of Human Serum Albumin and Fab Fragments》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound((1H-Imidazol-2-yl)methanamine dihydrochloride)Computed Properties of C4H9Cl2N3.

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

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Treatment of the Allura Red food colorant contaminated water by a novel cyanobacterium Desertifilum tharense》. Authors are Gul, Ulkuye Dudu; Senol, Zeynep Mine; Tasstan, Burcu Ertit.The article about the compound:Sodium 6-hydroxy-5-((2-methoxy-5-methyl-4-sulfonatophenyl)diazenyl)naphthalene-2-sulfonatecas:25956-17-6,SMILESS:O=S(C1=CC=C2C(/N=N/C3=CC(C)=C(S(=O)([O-])=O)C=C3OC)=C(O)C=CC2=C1)([O-])=O.[Na+].[Na+]).Synthetic Route of C18H14N2Na2O8S2. Through the article, more information about this compound (cas:25956-17-6) is conveyed.

The biosorption properties of a newly isolated and identified cyanobacterium called Desertifilum tharense were investigated in the current study. Following morphol. and mol. identification (16S rRNA sequencing anal.), the food colorant removal potential of this new isolate was determined Moreover, the isotherm, kinetic, and thermodn. studies were performed, and also the biosorbent characterization was studied after and before colorant biosorption with Fourier transform IR and SEM anal. Addnl., the changes in chlorophyll content of the biosorbent were examined after and before colorant treatment. The newly isolated cyanobacterial biosorbent removed 97% of Allura Red food colorant/dye at 1,500 mg L-1 initial dye concentration successfully at optimal conditions. Langmuir isotherm and pseudo-second-order kinetic models were fitted with the biosorption of the dye. The D-R model showed that the biosorption process occurred phys. The chlorophyll-a content of the biosorbent was neg. affected by the biosorption. The newly isolated and identified cyanobacterium seems to be a successful candidate for use to treat highly dye concentrated wastewaters.

《Treatment of the Allura Red food colorant contaminated water by a novel cyanobacterium Desertifilum tharense》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(Sodium 6-hydroxy-5-((2-methoxy-5-methyl-4-sulfonatophenyl)diazenyl)naphthalene-2-sulfonate)Synthetic Route of C18H14N2Na2O8S2.

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

Application In Synthesis of 4-Fluoro-1H-indole-3-carboxylic acid. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 4-Fluoro-1H-indole-3-carboxylic acid, is researched, Molecular C9H6FNO2, CAS is 23077-42-1, about Synthesis of cyclic chiral α-amino boronates by copper-catalyzed asymmetric dearomative borylation of indoles. Author is Chen, Lili; Shen, Jun-Jian; Gao, Qian; Xu, Senmiao.

A copper(I)-catalyzed dearomative borylation of N-alkoxycarbonyl protected indole-3-carboxylates has been developed. The boron addition in this reaction occurred regioselectively at the 2-position of indoles followed by diastereoselective protonation, affording the corresponding stable cyclic chiral α-amino boronates (2-borylindolines) in moderate to good yields with excellent diastereo- and enantioselectivities. The product 2c could be used as a versatile precursor to undergo subsequent stereoselective transformations, delivering highly functionalized 2,3,3-trisubstituted chiral indolines.

《Synthesis of cyclic chiral α-amino boronates by copper-catalyzed asymmetric dearomative borylation of indoles》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(4-Fluoro-1H-indole-3-carboxylic acid)Application In Synthesis of 4-Fluoro-1H-indole-3-carboxylic acid.

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

Recommanded Product: 6-Bromo-2,3-dihydrobenzo[b][1,4]dioxine. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 6-Bromo-2,3-dihydrobenzo[b][1,4]dioxine, is researched, Molecular C8H7BrO2, CAS is 52287-51-1, about Synthesis and some transformations of 2- and 2,2′-substituted bis(ethylenedioxy)biphenyls containing cyclopropane fragments. Author is Mochalov, S. S.; Puretskii, N. A.; Fedotov, A. N.; Trofimova, E. V.; Tafeenko, V. A.; Aslanov, L. A.; Zefirov, N. S..

3,4:3′,4′-Bis(ethylenedioxy)biphenyl undergoes bromination, nitration, and cyclopropylcarbonylation only at the 2-position. Analogous reactions with 2-substituted bis(ethylenedioxy)biphenyls occur regioselectively at the 2′-position. The reactions of 2-cyclopropylcarbonyl- and 2,2′-bis(cyclopropylcarbonyl)bis(ethylenedioxy)biphenyls with complex metal hydrides afforded the corresponding arylcyclopropylcarbinols which tended to undergo intramol. alkylation of the aromatic ring with conservation of the cyclopropane fragment (monosubstituted derivatives) and formation of cyclopropyl-containing cyclic ethers (disubstituted ethylenedioxybiphenyls). The reduction of the nitro group in 2′-cyclopropylcarbonyl-2-nitro-4,5:4′,5′-bis(ethylenedioxy)biphenyl was accompanied by intramol. cyclization involving spatially close functional groups, the cyclopropane fragment remaining intact.

《Synthesis and some transformations of 2- and 2,2′-substituted bis(ethylenedioxy)biphenyls containing cyclopropane fragments》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(6-Bromo-2,3-dihydrobenzo[b][1,4]dioxine)Recommanded Product: 6-Bromo-2,3-dihydrobenzo[b][1,4]dioxine.

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

Product Details of 17190-29-3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 3-Hydroxy-3-phenylpropanenitrile, is researched, Molecular C9H9NO, CAS is 17190-29-3, about P(i-PrNCH2CH2)3N as a Lewis Base Catalyst for the Synthesis of β-Hydroxynitriles Using TMSAN. Author is Wadhwa, Kuldeep; Verkade, John G..

The title proazaphosphatrane was found to be an efficient catalyst for synthesis of β-hydroxynitriles via the reaction of trimethylsilylacetonitrile (TMSAN) with aldehydes under mild reaction conditions and typically low catalyst loading (ca. 2 mol %). A variety of functional groups were tolerated, and good to excellent product yields were obtained.

《P(i-PrNCH2CH2)3N as a Lewis Base Catalyst for the Synthesis of β-Hydroxynitriles Using TMSAN》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(3-Hydroxy-3-phenylpropanenitrile)Product Details of 17190-29-3.

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

Kawano, Yoshikazu; Kaneko, Nobuya; Mukaiyama, Teruaki published the article 《Lewis base-catalyzed cyanomethylation of carbonyl compounds with (trimethylsilyl)acetonitrile》. Keywords: Lewis base catalyzed cyanomethylation carbonyl compound trimethylsilyl acetonitrile; lithium acetate catalyzed cyanomethylation carbonyl compound silyl acetonitrile.They researched the compound: 3-Hydroxy-3-phenylpropanenitrile( cas:17190-29-3 ).Category: pyrazoles-derivatives. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:17190-29-3) here.

Catalytic cyanomethylation of various carbonyl compounds with (trimethylsilyl)acetonitrile (TMSCH2CN) in the presence of Lewis bases such as cesium or lithium acetate proceeded smoothly to afford the corresponding cyanomethylated adducts in good yields. Thus, AcOLi catalyzed cyanomethylation of PhCHO with Me3SiCH2CN in DMF at 0° to room temperature followed by acid hydrolysis gave 98% PhCHOHCH2CN.

《Lewis base-catalyzed cyanomethylation of carbonyl compounds with (trimethylsilyl)acetonitrile》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(3-Hydroxy-3-phenylpropanenitrile)Category: pyrazoles-derivatives.

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