Day: November 24, 2022

Avinesh, P. published the artcileFacile Synthesis of Fully Decorated Imidazo[4,5-b] and Imidazo[4,5-c] Pyridines in Aqueous DMF via C-H Activation under Microwave Irradiation, HPLC of Formula: 1190875-39-8, the publication is ChemistrySelect (2016), 1(10), 2265-2270, database is CAplus.

Catalytic C-H bond activation of heteroarenes has gained tremendous potential in recent years due to their environmentally and economically benign nature. In this paper, the regioisomeric synthesis of fully decorated imidazopyridines, e.g., I employing a C-H activation protocol with a wide range of aryl/hetero aryl/alkyl boronic acids, e.g., II in aqueous DMF is reported. The use of inexpensive copper catalyst and bathophenanthroline as ligand were found to be instrumental in driving these reactions to completion. This optimized protocol was further extended to alkyl/aryl/heteroaryl potassium organo trifluoroborates such as potassium trifluoro(4-methoxyphenyl)boranuide, potassium trifluoro[4-(trifluoromethyl)phenyl]boranuide, potassium trifluoro(3,4,5-trimethylphenyl)boranuide, etc. A wide range of diversely substituted imidazo pyridine analogs which are known for their potential therapeutic applications have been synthesized using this highly efficient and atom economical protocol.

ChemistrySelect published new progress about 1190875-39-8. 1190875-39-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Piperidine,Boronic acid and ester,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, and the molecular formula is C13H22BN3O4, HPLC of Formula: 1190875-39-8.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Srivastava, Manish Kumar published the artcileCoordination propensity of N-protected amino acids and sterically congested heterocyclic 尾-diketones toward BuSnCl₃: preparation and structural features of some new seven coordinated organic-inorganic hybrid formulations of monobutyltin(IV), COA of Formula: C17H14N2O2, the publication is Main Group Metal Chemistry (2014), 37(3-4), 75-83, database is CAplus.

Organotin carboxylate complexes I (1–4; 1, X = CH₂CH, R = H, R¹ = Ph; 2, X = CH₂CH, R = H, R¹ = Me; 3, X = CH, R = s-Bu, R¹ = Ph; 4, X = CH, R = s-Bu, R¹ = 4-ClC₆H₄) and II (5–8; 5, X = CH₂CH, R = H, R¹ = P h; 6, X = CH, R = s-Bu, R¹ = Ph; 7, X = CH, R = s-Bu, R¹ = 4-ClC₆H₄; 8, X = CH, R = s-Bu, R¹ = Me), derived from phthaloyl-protected amino acids, were prepared by the reactions of monobutyltin(IV) chloride with sodium salts of N-protected amino acids and sterically congested heterocyclic 尾-diketones in 1:1:1 and 1:2:1 molar ratios in refluxing dry THF and characterized by spectral methods. Plausible structures of these N-protected amino acids and sterically congested heterocyclic 尾-diketones-modified BuSnCl₃ formulations were suggested on the basis of physicochem. and spectral studies. These newly prepared organic-inorganic hybrid complexes of monobutyltin(IV) contain seven coordinated tin centers as revealed by ¹¹⁹Sn NMR spectral data.

Main Group Metal Chemistry published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C6H8N2, COA of Formula: C17H14N2O2.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Sanjeev, R. published the artcileStudy on associative and non-associative behavior of some 5-membered heterocycles with two and one hetero atoms and their N-methylated derivatives from surface tension data, Recommanded Product: 1-Methylpyrazole, the publication is Research Journal of Chemistry and Environment (2015), 19(2), 26-29, database is CAplus.

Simple 5-membered heterocycles and two of their Nmethylated derivatives with two hetero atoms viz. pyrazole, isoxazole isothiozole and 1-methylpyrazole and with one hetero atom viz. pyrrole, furan, thiophene and N-methylpyrrole have shown a discriminative behavior toward surface tension, E脰TV脰S constants (k), order of association (x). This was explained in terms of associative and nonassociative behavior of these eight compounds Trouton’s rule had negligible significance on the associative and non-associative behavior.

Research Journal of Chemistry and Environment published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Recommanded Product: 1-Methylpyrazole.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Iida, Keisuke published the artcileDisulfide-Catalyzed Iodination of Electron-Rich Aromatic Compounds, Recommanded Product: 1-Methylpyrazole, the publication is Journal of Organic Chemistry (2019), 84(11), 7411-7417, database is CAplus and MEDLINE.

Herein, a disulfide-catalyzed electrophilic iodination of aromatic compounds using 1,3-diiodo-5,5-dimethylhydantoin (DIH) has been developed. The disulfide activates DIH as a Lewis base to promote the iodination reaction in acetonitrile under mild conditions. This system is applicable to a wide range of electron-rich aromatic compounds, including acetanilide, anisole, imidazole, and pyrazole derivatives

Journal of Organic Chemistry published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Recommanded Product: 1-Methylpyrazole.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Seki, Kunio published the artcileStudies on hypolipidemic agents. II. Synthesis and pharmacological properties of alkylpyrazole derivatives, Application of 3-Isopropyl-1H-pyrazole-5-carboxylic acid, the publication is Chemical & Pharmaceutical Bulletin (1984), 32(4), 1568-77, database is CAplus and MEDLINE.

Claisen condensation of MeCOR (R = C₁-C₁₇ alkyl) with (CO₂Et)₂ gave enolates RCOCH:C(ONa)CO₂Et, which underwent cyclocondensation with R¹NHNH₂[R¹ = H, Me, (CH₂)_nMe, C₆H₄R²-4; R² = H, Me, Cl, OMe, NH₂; n = 7, 9, 11] to give pyrazoles I (R³ = CO₂H, CO₂Et). Reduction of I (same R, R¹ = H, R² = CO₂Et) gave I (R³ = CH₂OH) and hydrolysis of I (R³ = CO₂Et) gave I (R = CO₂H). The latter compounds were chlorinated and amidated to give I [same R, R¹ = H, R³ = CONHR⁴, R⁴ = CH₂CH₂OH, CH₂CO₂Et, CH(CHMeEt)CO₂Et, H, Bu, decyl]. These pyrazoles (46 compounds) were evaluated for hypolipidemic activity in rats. Homologation of the C-5 alkyl chain led to marked increase in activity, but introduction of other substituents at other sites on the pyrazole ring failed to enhance the activity. The replacement of the pyrazole ring with an isoxazole ring resulted in a marked decrease in activity. I (R = tridecyl, R¹ = H, R² = CO₂H) was as effective as clofibrate in lowering serum triglycerides and cholesterol in rats and showed fairly low toxicity with LD₅₀ = 10.0 g/kg orally in mice.

Chemical & Pharmaceutical Bulletin published new progress about 890590-91-7. 890590-91-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid, name is 3-Isopropyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C48H47FeP, Application of 3-Isopropyl-1H-pyrazole-5-carboxylic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Beaulieu, Christian published the artcileIdentification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(24), 7444-7449, database is CAplus and MEDLINE.

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease is described. The identified inhibitors bearing an amino nitrile warhead in P1 exhibit low nanomolar in vitro potency against cruzipain. Further SAR in P2 portion led to the identification of compounds, such as 26 (I), that have a unique selectivity profile against other cysteine proteases and offering new opportunities for safer treatment of Chagas disease.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Zainul, Rahadian published the artcileEnhanced electrochemical sensor for electrocatalytic glucose analysis in orange juices and milk by the integration of the electron-withdrawing substituents on graphene/glassy carbon electrode, Computed Properties of 4551-69-3, the publication is Journal of Analytical Methods in Chemistry (2022), 5029036, database is CAplus and MEDLINE.

In this work, a novel electrochem. sensor was developed by electron-withdrawing substituent modification of 1-phenyl-3-methyl-4-(4-fluorobenzoyl)-5-pyrazolone on a graphene-modified glassy carbon electrode (HPMpFP-graphene/GCE) for glucose detection. The results of characterizations using a scanning electron microscope, Fourier transform IR spectroscopy, Raman spectroscopy, and NMR spectroscopy showed the successful fabrication of HPMpFP-graphene nanocomposite, which served as an electroactive probe for glucose detection. The electron transfer ability of HPMpFBP-graphene/GCE has been successfully revealed using cyclic voltammetry and electrochem. impedance spectroscopy results. The good electrochem. performance was shown by well-defined peak currents of square wave voltammetry under various parameters, including pH, HPMpFP and graphene composition, and scan rate effect. A high electrochem. evaluated surface area using chronoamperometry suggested that the present glucose detection response was intensified. The chronoamperometry results at a work potential of 0.4 V presented a wide linear range of 1 x 10³-90渭M and 88-1渭M with 0.74渭M (S/N = 3) as the detection limit. An acceptable recovery has been revealed in the real sample anal. The electrochem. sensing behavior of the composite indicates that it may be a promising candidate for a glucose sensor and it significantly extends the range of applications in the electrochem. field.

Journal of Analytical Methods in Chemistry published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C18H35NO, Computed Properties of 4551-69-3.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Koike, Eiji published the artcileOrganic pigments. II. Syntheses of 1-phenyl-3-methyl-5-pyrazolone and its derivatives, Application In Synthesis of 14580-22-4, the publication is Nippon Kagaku Kaishi (1921-47) (1954), 56-8, database is CAplus.

cf. C.A. 48, 6388d, 11079a. Phenylhydrazine (I) (24 g.) was added within 30 min. to a mixture of 12 g. 60% EtOH and 29.2 g. AcCH₂CO₂Et (II) below 50掳, stirred for 2 hrs., then refluxed 4 hrs. and filtered to yield 35.5 g. of 1-phenyl-3-methyl-5-pyrazolone, m. 125.0-126.5掳. The treatment of 6.5 g. p-ClC₆H₄NHNH₂.HCl in H₂O, acidified with AcOH with 4.8 g. II gave 84% 1-(p-chlorophenyl)-3-methyl-5-pyrazolone, m. 165-6掳. Similarly were prepared the following analogs of III (1-substituent, m.p., % yield given): 慰-ClC₆H₄, 182-3掳, 68.6; m-ClC₆H₄, 124-5.5掳, 93.6; 慰-MeC₆H₄, 180-1掳, 26.6; m-MeC₆H₄, 104.7-5.0掳, 48; p-MeC₆H₄, 91.5-3.5掳, 43.6; p-MeOC₆H₄, 122-3掳, 36.7; m-O₂NC₆H₄, 185掳, 68.5; p-O₂NC₆H₄, 220掳, 80; m-HO₃SC₆H₄, 200掳, 90.8. AcCH₂CN (42 g.) in 54 cc. H₃O and 16 cc. concentrated HCl treated with 54 g. I in 200 cc. H₂O and 41 cc. HCl at 35-40掳, and further addition of 30 cc. concentrated HCl at 90掳 gave 62.5 g. of 1-phenyl-3-methyl-5-aminopyrazole, m. 110-111.5掳.

Nippon Kagaku Kaishi (1921-47) published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Application In Synthesis of 14580-22-4.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Rani, Pooja published the artcileCoordination Polymers as a Functional Material for the Selective Molecular Recognition of Nitroaromatics and ipso-Hydroxylation of Arylboronic Acids, Computed Properties of 763120-58-7, the publication is Chemistry – An Asian Journal (2022), 17(2), e202101204, database is CAplus and MEDLINE.

We report the synthesis and structural characterization of two coordination polymers (CPs), namely; [{Zn(L)(DMF)₄} 路 2BF₄]_伪 (1) and [{Cd(L)₂(Cl)₂} 路 2H₂O]_伪 (2) (where L=N²,N⁶-di(pyridin-4-yl)naphthalene-2,6-dicarboxamide). Crystal packing of 1 reveals the existence of channels running along the b- and c-axis filled by the ligated DMF and lattice anions, resp. Whereas, crystal packing of 2 reveals that the metallacycles of each 1D chain are intercalating into the groove of adjacent metallacycles resulting in the stacking of 1D loop-chains to form a sheet-like architecture. In addition, both 1 and 2 were exploited as multifunctional materials for the detection of nitroarom. compounds (NACs) as well as a catalyst in the ipso-hydroxylation of aryl/heteroarylboronic acids. Remarkably, 1 and 2 showed high fluorescence stability in an aqueous medium and displayed a maximum 88% and 97% quenching efficiency for 4-NPH, resp. among all the investigated NACs. The mechanistic investigation of NACs recognition suggested that the fluorescence quenching occurred via electron as well as energy transfer process. Furthermore, the ipso-hydroxylation of aryl/heteroarylboronic acids in presence of 1 and 2 gave up to 99% desired product yield within 15 min in our established protocol. In both cases, 1 and 2 are recyclable upto five cycles without any significant loss in their efficiency.

Chemistry – An Asian Journal published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Computed Properties of 763120-58-7.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Cheung, Atwood K. published the artcileDiscovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA), HPLC of Formula: 763120-58-7, the publication is Journal of Medicinal Chemistry (2018), 61(24), 11021-11036, database is CAplus and MEDLINE.

Spinal muscular atrophy (SMA), a rare neuromuscular disorder, is the leading genetic cause of death in infants and toddlers. SMA is caused by the deletion or a loss of function mutation of the survival motor neuron 1 (SMN1) gene. In humans, a second closely related gene SMN2 exists, however it codes for a less stable SMN protein. In recent years, significant progress has been made toward disease modifying treatments for SMA by modulating SMN2 pre-mRNA splicing. Herein, we describe the discovery of LMI070/branaplam, a small mol. that stabilizes the interaction between the spliceosome and SMN2 pre-mRNA. Branaplam (1) originated from a high-throughput phenotypic screening hit, pyridazine 2, and evolved via multi-parameter lead optimization. In a severe mouse SMA model, branaplam treatment increased full-length SMN RNA and protein levels, and extended survival. Currently, branaplam is in clin. studies for SMA.

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, HPLC of Formula: 763120-58-7.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics